Chemicals

Showing 19201–19350 of 41137 results

  • Eupenifeldin is a pentacyclic bistropolone fungal metabolite originally isolated from E. brefeldianum ATCC 74184.{39755} It is cytotoxic against HCT116 and HCTVM46 colon carcinoma cells in vitro (IC50s = 0.005 and 0.002 μg/ml, respectively). In vivo, eupenifeldin (0.3-2 mg/kg per day) increases median survival time in a mouse model of P388 leukemia.  

     

    Brand:
    Cayman
    SKU:25114 - 500 µg

    Available on backorder

  • Euphol acetate is a triterpenoid that has been found in Euphorbia species and has diverse biological activities.{48815,48816,48817} It reduces sodium fluorescein uptake by CHO cells expressing organic anion-transporting polypeptide 1B1 (OATP1B1) and OATP1B3 to 29.2 and 40.2% of controls, respectively, when used at a concentration of 10 μM.{48817} Euphol acetate (50 and 100 μg/ml) induces mortality in 40% of B. glabrata snails.{48816}  

     

    Brand:
    Cayman
    SKU:29646 - 1 mg

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  • Euphorbiasteroid is a tricyclic diterpene that has been found in the plant E. lathyris.{48442} It inhibits early-stage adipogenesis of 3T3-L1 cells, decreasing intracellular triglyceride accumulation when used at concentrations of 25 and 50 µM.{48443} It decreases the expression of Fas, C/EBPα, PPARγ, and SREBP-1c and increases phosphorylation of AMP-activated protein kinase (AMPK) and acetyl-coenzyme A carboxylase (ACC) in 3T3-L1 cells. Euphorbiasteroid inhibits proliferation of HL-60 cells in a concentration-dependent manner, as well as induces apoptosis and increases the expression of Fas and Fas ligand (FasL) and the activity of caspase-3 and caspase-8 in HL-60 cells.{48444} It increases P-glycoprotein activity, reverses multi-drug resistance, and restores cytotoxicity of the anticancer agents vinblastine (Item No. 11762), paclitaxel (Item No. 10461), and doxorubicin (Item No. 15007) to MES-SA/Dx5 sarcoma cells.{48445}  

     

    Brand:
    Cayman
    SKU:27822 - 100 mg

    Available on backorder

  • Euphorbiasteroid is a tricyclic diterpene that has been found in the plant E. lathyris.{48442} It inhibits early-stage adipogenesis of 3T3-L1 cells, decreasing intracellular triglyceride accumulation when used at concentrations of 25 and 50 µM.{48443} It decreases the expression of Fas, C/EBPα, PPARγ, and SREBP-1c and increases phosphorylation of AMP-activated protein kinase (AMPK) and acetyl-coenzyme A carboxylase (ACC) in 3T3-L1 cells. Euphorbiasteroid inhibits proliferation of HL-60 cells in a concentration-dependent manner, as well as induces apoptosis and increases the expression of Fas and Fas ligand (FasL) and the activity of caspase-3 and caspase-8 in HL-60 cells.{48444} It increases P-glycoprotein activity, reverses multi-drug resistance, and restores cytotoxicity of the anticancer agents vinblastine (Item No. 11762), paclitaxel (Item No. 10461), and doxorubicin (Item No. 15007) to MES-SA/Dx5 sarcoma cells.{48445}  

     

    Brand:
    Cayman
    SKU:27822 - 25 mg

    Available on backorder

  • Euphorbiasteroid is a tricyclic diterpene that has been found in the plant E. lathyris.{48442} It inhibits early-stage adipogenesis of 3T3-L1 cells, decreasing intracellular triglyceride accumulation when used at concentrations of 25 and 50 µM.{48443} It decreases the expression of Fas, C/EBPα, PPARγ, and SREBP-1c and increases phosphorylation of AMP-activated protein kinase (AMPK) and acetyl-coenzyme A carboxylase (ACC) in 3T3-L1 cells. Euphorbiasteroid inhibits proliferation of HL-60 cells in a concentration-dependent manner, as well as induces apoptosis and increases the expression of Fas and Fas ligand (FasL) and the activity of caspase-3 and caspase-8 in HL-60 cells.{48444} It increases P-glycoprotein activity, reverses multi-drug resistance, and restores cytotoxicity of the anticancer agents vinblastine (Item No. 11762), paclitaxel (Item No. 10461), and doxorubicin (Item No. 15007) to MES-SA/Dx5 sarcoma cells.{48445}  

     

    Brand:
    Cayman
    SKU:27822 - 250 mg

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  • Euphorbiasteroid is a tricyclic diterpene that has been found in the plant E. lathyris.{48442} It inhibits early-stage adipogenesis of 3T3-L1 cells, decreasing intracellular triglyceride accumulation when used at concentrations of 25 and 50 µM.{48443} It decreases the expression of Fas, C/EBPα, PPARγ, and SREBP-1c and increases phosphorylation of AMP-activated protein kinase (AMPK) and acetyl-coenzyme A carboxylase (ACC) in 3T3-L1 cells. Euphorbiasteroid inhibits proliferation of HL-60 cells in a concentration-dependent manner, as well as induces apoptosis and increases the expression of Fas and Fas ligand (FasL) and the activity of caspase-3 and caspase-8 in HL-60 cells.{48444} It increases P-glycoprotein activity, reverses multi-drug resistance, and restores cytotoxicity of the anticancer agents vinblastine (Item No. 11762), paclitaxel (Item No. 10461), and doxorubicin (Item No. 15007) to MES-SA/Dx5 sarcoma cells.{48445}  

     

    Brand:
    Cayman
    SKU:27822 - 50 mg

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  • Eurycomanone is a quassinoid originally isolated from E. longifolia that has diverse biological activities.{59000} It is active against the W2 and D6 clones of P. falciparum (IC50s = 0.015 and 0.026 µg/ml, respectively).{59002} Eurycomanone induces lipolysis in 3T3-L1 adipocytes with an EC50 value of 14.6 µM, an effect that can be blocked by the protein kinase A (PKA) inhibitor H-89 (Item No. 10010556).{59001} It induces cell cycle arrest at the G2/M phase and apoptosis in HepG2 cells when used at a concentration of 5 µg/ml.{59003} It reduces estrogen release and increases testosterone release in isolated rat Leydig cell-rich testicular interstitial cell preparations when used at concentrations of 1 and 10 µM.{59004} Eurycomanone (1 mg/kg, i.p.) decreases gastric acid secretion and lesion size in rat models of indomethacin-, water immersion stress-, or pyloric ligation-induced ulcer formation.{59005}  

     

    Brand:
    Cayman
    SKU:30896 - 1 mg

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  • Eurycomanone is a quassinoid originally isolated from E. longifolia that has diverse biological activities.{59000} It is active against the W2 and D6 clones of P. falciparum (IC50s = 0.015 and 0.026 µg/ml, respectively).{59002} Eurycomanone induces lipolysis in 3T3-L1 adipocytes with an EC50 value of 14.6 µM, an effect that can be blocked by the protein kinase A (PKA) inhibitor H-89 (Item No. 10010556).{59001} It induces cell cycle arrest at the G2/M phase and apoptosis in HepG2 cells when used at a concentration of 5 µg/ml.{59003} It reduces estrogen release and increases testosterone release in isolated rat Leydig cell-rich testicular interstitial cell preparations when used at concentrations of 1 and 10 µM.{59004} Eurycomanone (1 mg/kg, i.p.) decreases gastric acid secretion and lesion size in rat models of indomethacin-, water immersion stress-, or pyloric ligation-induced ulcer formation.{59005}  

     

    Brand:
    Cayman
    SKU:30896 - 10 mg

    Available on backorder

  • Eurycomanone is a quassinoid originally isolated from E. longifolia that has diverse biological activities.{59000} It is active against the W2 and D6 clones of P. falciparum (IC50s = 0.015 and 0.026 µg/ml, respectively).{59002} Eurycomanone induces lipolysis in 3T3-L1 adipocytes with an EC50 value of 14.6 µM, an effect that can be blocked by the protein kinase A (PKA) inhibitor H-89 (Item No. 10010556).{59001} It induces cell cycle arrest at the G2/M phase and apoptosis in HepG2 cells when used at a concentration of 5 µg/ml.{59003} It reduces estrogen release and increases testosterone release in isolated rat Leydig cell-rich testicular interstitial cell preparations when used at concentrations of 1 and 10 µM.{59004} Eurycomanone (1 mg/kg, i.p.) decreases gastric acid secretion and lesion size in rat models of indomethacin-, water immersion stress-, or pyloric ligation-induced ulcer formation.{59005}  

     

    Brand:
    Cayman
    SKU:30896 - 25 mg

    Available on backorder

  • Eurycomanone is a quassinoid originally isolated from E. longifolia that has diverse biological activities.{59000} It is active against the W2 and D6 clones of P. falciparum (IC50s = 0.015 and 0.026 µg/ml, respectively).{59002} Eurycomanone induces lipolysis in 3T3-L1 adipocytes with an EC50 value of 14.6 µM, an effect that can be blocked by the protein kinase A (PKA) inhibitor H-89 (Item No. 10010556).{59001} It induces cell cycle arrest at the G2/M phase and apoptosis in HepG2 cells when used at a concentration of 5 µg/ml.{59003} It reduces estrogen release and increases testosterone release in isolated rat Leydig cell-rich testicular interstitial cell preparations when used at concentrations of 1 and 10 µM.{59004} Eurycomanone (1 mg/kg, i.p.) decreases gastric acid secretion and lesion size in rat models of indomethacin-, water immersion stress-, or pyloric ligation-induced ulcer formation.{59005}  

     

    Brand:
    Cayman
    SKU:30896 - 5 mg

    Available on backorder

  • Evacetrapib is a benzazepine inhibitor of cholesteryl ester transfer protein (CETP; IC50s = 5.5 and 26 nM for human recombinant and plasma-derived proteins, respectively).{41797} It is selective for CETP over a panel of cell surface and nuclear receptors with no significant inhibition at 1 µM. Evacetrapib (1-10 µM) reduces expression of the serine protease proprotein convertase subtilisin kexin 9 (PCSK9) and the LDL receptor (LDLR) in HepG2 cells in a dose-dependent manner with no effect on cell viability.{41798} It also reduces protein levels of LDLR, SREBF2-M, and PCSK9 in HepG2 lysates, nuclear extracts, and culture medium, respectively, in a dose-dependent manner. Oral administration of evacetrapib (30 mg/kg) inhibits CETP activity by 98.5, 98.6, and 18.4% after four, eight, and 24 hours, respectively, in serum from transgenic mice expressing human CETP and ApoA1.{41797} Evacetrapib increases HDL cholesterol levels in CETP/ApoA1 transgenic mice in a dose-dependent manner, including by 129.7% eight hours following administration of a 30 mg/kg dose.  

     

    Brand:
    Cayman
    SKU:23670 - 10 mg

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  • Evacetrapib is a benzazepine inhibitor of cholesteryl ester transfer protein (CETP; IC50s = 5.5 and 26 nM for human recombinant and plasma-derived proteins, respectively).{41797} It is selective for CETP over a panel of cell surface and nuclear receptors with no significant inhibition at 1 µM. Evacetrapib (1-10 µM) reduces expression of the serine protease proprotein convertase subtilisin kexin 9 (PCSK9) and the LDL receptor (LDLR) in HepG2 cells in a dose-dependent manner with no effect on cell viability.{41798} It also reduces protein levels of LDLR, SREBF2-M, and PCSK9 in HepG2 lysates, nuclear extracts, and culture medium, respectively, in a dose-dependent manner. Oral administration of evacetrapib (30 mg/kg) inhibits CETP activity by 98.5, 98.6, and 18.4% after four, eight, and 24 hours, respectively, in serum from transgenic mice expressing human CETP and ApoA1.{41797} Evacetrapib increases HDL cholesterol levels in CETP/ApoA1 transgenic mice in a dose-dependent manner, including by 129.7% eight hours following administration of a 30 mg/kg dose.  

     

    Brand:
    Cayman
    SKU:23670 - 100 mg

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  • Evacetrapib is a benzazepine inhibitor of cholesteryl ester transfer protein (CETP; IC50s = 5.5 and 26 nM for human recombinant and plasma-derived proteins, respectively).{41797} It is selective for CETP over a panel of cell surface and nuclear receptors with no significant inhibition at 1 µM. Evacetrapib (1-10 µM) reduces expression of the serine protease proprotein convertase subtilisin kexin 9 (PCSK9) and the LDL receptor (LDLR) in HepG2 cells in a dose-dependent manner with no effect on cell viability.{41798} It also reduces protein levels of LDLR, SREBF2-M, and PCSK9 in HepG2 lysates, nuclear extracts, and culture medium, respectively, in a dose-dependent manner. Oral administration of evacetrapib (30 mg/kg) inhibits CETP activity by 98.5, 98.6, and 18.4% after four, eight, and 24 hours, respectively, in serum from transgenic mice expressing human CETP and ApoA1.{41797} Evacetrapib increases HDL cholesterol levels in CETP/ApoA1 transgenic mice in a dose-dependent manner, including by 129.7% eight hours following administration of a 30 mg/kg dose.  

     

    Brand:
    Cayman
    SKU:23670 - 5 mg

    Available on backorder

  • Evacetrapib is a benzazepine inhibitor of cholesteryl ester transfer protein (CETP; IC50s = 5.5 and 26 nM for human recombinant and plasma-derived proteins, respectively).{41797} It is selective for CETP over a panel of cell surface and nuclear receptors with no significant inhibition at 1 µM. Evacetrapib (1-10 µM) reduces expression of the serine protease proprotein convertase subtilisin kexin 9 (PCSK9) and the LDL receptor (LDLR) in HepG2 cells in a dose-dependent manner with no effect on cell viability.{41798} It also reduces protein levels of LDLR, SREBF2-M, and PCSK9 in HepG2 lysates, nuclear extracts, and culture medium, respectively, in a dose-dependent manner. Oral administration of evacetrapib (30 mg/kg) inhibits CETP activity by 98.5, 98.6, and 18.4% after four, eight, and 24 hours, respectively, in serum from transgenic mice expressing human CETP and ApoA1.{41797} Evacetrapib increases HDL cholesterol levels in CETP/ApoA1 transgenic mice in a dose-dependent manner, including by 129.7% eight hours following administration of a 30 mg/kg dose.  

     

    Brand:
    Cayman
    SKU:23670 - 50 mg

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  • Evernic acid is a secondary metabolite produced by some species of lichen that can bind to allosteric sites on the protein surface of FAS-II enzymes and produce antibacterial and antiplasmodial effects.{28468} It inhibits two key plasmodial FAS-II enzymes PfFabZ and PfFabI (IC50 = 10.7 and 36.1 µM, respectively) but shows low efficacy against the malaria parasite P. berghei (IC50 = 77.3 µM).{28468}  

     

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    Cayman
    SKU:-

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  • Evernic acid is a secondary metabolite produced by some species of lichen that can bind to allosteric sites on the protein surface of FAS-II enzymes and produce antibacterial and antiplasmodial effects.{28468} It inhibits two key plasmodial FAS-II enzymes PfFabZ and PfFabI (IC50 = 10.7 and 36.1 µM, respectively) but shows low efficacy against the malaria parasite P. berghei (IC50 = 77.3 µM).{28468}  

     

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    Cayman
    SKU:-

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  • Evernic acid is a secondary metabolite produced by some species of lichen that can bind to allosteric sites on the protein surface of FAS-II enzymes and produce antibacterial and antiplasmodial effects.{28468} It inhibits two key plasmodial FAS-II enzymes PfFabZ and PfFabI (IC50 = 10.7 and 36.1 µM, respectively) but shows low efficacy against the malaria parasite P. berghei (IC50 = 77.3 µM).{28468}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • Evernic acid is a secondary metabolite produced by some species of lichen that can bind to allosteric sites on the protein surface of FAS-II enzymes and produce antibacterial and antiplasmodial effects.{28468} It inhibits two key plasmodial FAS-II enzymes PfFabZ and PfFabI (IC50 = 10.7 and 36.1 µM, respectively) but shows low efficacy against the malaria parasite P. berghei (IC50 = 77.3 µM).{28468}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • The mammalian target of rapamycin (mTOR) is a serine/threonine kinase that, as part of two distinct complexes (mTORC1 and mTORC2), plays pivotal roles in intracellular signaling.{15415,15559,24848} Everolimus is a hydroxyethyl ether rapamycin (Item No. 13346) derivative that inhibits mTOR signaling through both mTORC1 and mTORC2 when added to cells at 20 nM.{24850,24847} It is orally available and shows improved pharmacokinetics and pharmacodynamics over rapamycin.{24847} Through its inhibition of mTOR, everolimus inhibits cell proliferation, metabolism, and angiogenesis in certain types of cancer.{24847,24849} It also acts as an immunosuppressive agent in the context of organ transplantation.{24847,24846}  

     

    Brand:
    Cayman
    SKU:11597 - 10 mg

    Available on backorder

  • The mammalian target of rapamycin (mTOR) is a serine/threonine kinase that, as part of two distinct complexes (mTORC1 and mTORC2), plays pivotal roles in intracellular signaling.{15415,15559,24848} Everolimus is a hydroxyethyl ether rapamycin (Item No. 13346) derivative that inhibits mTOR signaling through both mTORC1 and mTORC2 when added to cells at 20 nM.{24850,24847} It is orally available and shows improved pharmacokinetics and pharmacodynamics over rapamycin.{24847} Through its inhibition of mTOR, everolimus inhibits cell proliferation, metabolism, and angiogenesis in certain types of cancer.{24847,24849} It also acts as an immunosuppressive agent in the context of organ transplantation.{24847,24846}  

     

    Brand:
    Cayman
    SKU:11597 - 25 mg

    Available on backorder

  • The mammalian target of rapamycin (mTOR) is a serine/threonine kinase that, as part of two distinct complexes (mTORC1 and mTORC2), plays pivotal roles in intracellular signaling.{15415,15559,24848} Everolimus is a hydroxyethyl ether rapamycin (Item No. 13346) derivative that inhibits mTOR signaling through both mTORC1 and mTORC2 when added to cells at 20 nM.{24850,24847} It is orally available and shows improved pharmacokinetics and pharmacodynamics over rapamycin.{24847} Through its inhibition of mTOR, everolimus inhibits cell proliferation, metabolism, and angiogenesis in certain types of cancer.{24847,24849} It also acts as an immunosuppressive agent in the context of organ transplantation.{24847,24846}  

     

    Brand:
    Cayman
    SKU:11597 - 5 mg

    Available on backorder

  • Everolimus-d4 is intended for use as an internal standard for the quantification of everolimus (Item No. 11597) by GC- or LC-MS. Everolimus is a hydroxyethyl ether form of rapamycin (Item No. 13346) that inhibits mTOR signaling through both mTORC1 and mTORC2 when added to cells at 20 nM.{24850,24847} It is orally available and shows improved pharmacokinetics and pharmacodynamics over rapamycin.{24847} Through its inhibition of mTOR, everolimus inhibits cell proliferation, metabolism, and angiogenesis in certain types of cancer.{24849,24846} It also acts as an immunosuppressive agent in the context of organ transplantation.  

     

    Brand:
    Cayman
    SKU:22559 -

    Out of stock

  • Everolimus-d4 is intended for use as an internal standard for the quantification of everolimus (Item No. 11597) by GC- or LC-MS. Everolimus is a hydroxyethyl ether form of rapamycin (Item No. 13346) that inhibits mTOR signaling through both mTORC1 and mTORC2 when added to cells at 20 nM.{24850,24847} It is orally available and shows improved pharmacokinetics and pharmacodynamics over rapamycin.{24847} Through its inhibition of mTOR, everolimus inhibits cell proliferation, metabolism, and angiogenesis in certain types of cancer.{24849,24846} It also acts as an immunosuppressive agent in the context of organ transplantation.  

     

    Brand:
    Cayman
    SKU:22559 -

    Out of stock

  • Evobrutinib is an inhibitor of Bruton’s tyrosine kinase (BTK; IC50 = 8.9 nM).{50414} It is selective for BTK over a panel of 233 kinases at 1 μM. It inhibits BTK in peripheral blood mononuclear cells (PBMCs; IC50 = 61 nM). Evobrutinib inhibits B cell activation and proliferation in vitro (IC50s = 18.4 and 10.9 nM, respectively).{46591} It inhibits mast cell degranulation in a mouse model of passive cutaneous anaphylaxis when administered at doses of 3.95, 19.8, and 39.5 mg/kg. Evobrutinib (1 and 3 mg/kg) reduces cartilage destruction in a rat model of collagen-induced arthritis. It also decreases proteinuria, interstitial inflammation, and the number of glomerular lesions and preserves kidney function in a mouse model of systemic lupus erythematosus (SLE).  

     

    Brand:
    Cayman
    SKU:29029 - 1 mg

    Available on backorder

  • Evobrutinib is an inhibitor of Bruton’s tyrosine kinase (BTK; IC50 = 8.9 nM).{50414} It is selective for BTK over a panel of 233 kinases at 1 μM. It inhibits BTK in peripheral blood mononuclear cells (PBMCs; IC50 = 61 nM). Evobrutinib inhibits B cell activation and proliferation in vitro (IC50s = 18.4 and 10.9 nM, respectively).{46591} It inhibits mast cell degranulation in a mouse model of passive cutaneous anaphylaxis when administered at doses of 3.95, 19.8, and 39.5 mg/kg. Evobrutinib (1 and 3 mg/kg) reduces cartilage destruction in a rat model of collagen-induced arthritis. It also decreases proteinuria, interstitial inflammation, and the number of glomerular lesions and preserves kidney function in a mouse model of systemic lupus erythematosus (SLE).  

     

    Brand:
    Cayman
    SKU:29029 - 10 mg

    Available on backorder

  • Evobrutinib is an inhibitor of Bruton’s tyrosine kinase (BTK; IC50 = 8.9 nM).{50414} It is selective for BTK over a panel of 233 kinases at 1 μM. It inhibits BTK in peripheral blood mononuclear cells (PBMCs; IC50 = 61 nM). Evobrutinib inhibits B cell activation and proliferation in vitro (IC50s = 18.4 and 10.9 nM, respectively).{46591} It inhibits mast cell degranulation in a mouse model of passive cutaneous anaphylaxis when administered at doses of 3.95, 19.8, and 39.5 mg/kg. Evobrutinib (1 and 3 mg/kg) reduces cartilage destruction in a rat model of collagen-induced arthritis. It also decreases proteinuria, interstitial inflammation, and the number of glomerular lesions and preserves kidney function in a mouse model of systemic lupus erythematosus (SLE).  

     

    Brand:
    Cayman
    SKU:29029 - 25 mg

    Available on backorder

  • Evobrutinib is an inhibitor of Bruton’s tyrosine kinase (BTK; IC50 = 8.9 nM).{50414} It is selective for BTK over a panel of 233 kinases at 1 μM. It inhibits BTK in peripheral blood mononuclear cells (PBMCs; IC50 = 61 nM). Evobrutinib inhibits B cell activation and proliferation in vitro (IC50s = 18.4 and 10.9 nM, respectively).{46591} It inhibits mast cell degranulation in a mouse model of passive cutaneous anaphylaxis when administered at doses of 3.95, 19.8, and 39.5 mg/kg. Evobrutinib (1 and 3 mg/kg) reduces cartilage destruction in a rat model of collagen-induced arthritis. It also decreases proteinuria, interstitial inflammation, and the number of glomerular lesions and preserves kidney function in a mouse model of systemic lupus erythematosus (SLE).  

     

    Brand:
    Cayman
    SKU:29029 - 5 mg

    Available on backorder

  • Evoxanthine is an alkaloid that has been found in O. renieri and has antimalarial and anticancer activities.{52172,52173} It is active against P. falciparum with an IC50 value of 67.6 µg/ml.{52172} Evoxanthine decreases proliferation of nine sensitive and drug-resistant cancer cell lines (IC50s = 6.11-80.99 µM).{52173}  

     

    Brand:
    Cayman
    SKU:29437 - 1 mg

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  • Evoxanthine is an alkaloid that has been found in O. renieri and has antimalarial and anticancer activities.{52172,52173} It is active against P. falciparum with an IC50 value of 67.6 µg/ml.{52172} Evoxanthine decreases proliferation of nine sensitive and drug-resistant cancer cell lines (IC50s = 6.11-80.99 µM).{52173}  

     

    Brand:
    Cayman
    SKU:29437 - 5 mg

    Available on backorder

  • EVP-6124 is a partial agonist of α7 subunit-containing nicotinic acetylcholine receptors (nAChRs; IC50 = 22.38 nM).{52384} It is 1,000-fold selective for α7 subunit-containing nAChRs over α4β2 subunit-containing nAChRs at 10 µM, as well as a panel of 60 peptide and nonpeptide receptors, ion channels, and transporters. EVP-6124 induces inward currents in Xenopus oocytes expressing human α7 subunit-containing nAChRs (EC50 = 0.16 µM). In vivo, EVP-6124 (0.1, 0.3, and 1 mg/kg) reverses scopolamine-induced deficits in the novel object recognition task and prevents natural forgetting of a familiar object in rats. It reduces premature responding, a measure of impulsivity, by low-attentive but not high-attentive female rats in the 5-choice serial reaction time test (5CSRTT).{52385}  

     

    Brand:
    Cayman
    SKU:30073 - 10 mg

    Available on backorder

  • EVP-6124 is a partial agonist of α7 subunit-containing nicotinic acetylcholine receptors (nAChRs; IC50 = 22.38 nM).{52384} It is 1,000-fold selective for α7 subunit-containing nAChRs over α4β2 subunit-containing nAChRs at 10 µM, as well as a panel of 60 peptide and nonpeptide receptors, ion channels, and transporters. EVP-6124 induces inward currents in Xenopus oocytes expressing human α7 subunit-containing nAChRs (EC50 = 0.16 µM). In vivo, EVP-6124 (0.1, 0.3, and 1 mg/kg) reverses scopolamine-induced deficits in the novel object recognition task and prevents natural forgetting of a familiar object in rats. It reduces premature responding, a measure of impulsivity, by low-attentive but not high-attentive female rats in the 5-choice serial reaction time test (5CSRTT).{52385}  

     

    Brand:
    Cayman
    SKU:30073 - 25 mg

    Available on backorder

  • EVP-6124 is a partial agonist of α7 subunit-containing nicotinic acetylcholine receptors (nAChRs; IC50 = 22.38 nM).{52384} It is 1,000-fold selective for α7 subunit-containing nAChRs over α4β2 subunit-containing nAChRs at 10 µM, as well as a panel of 60 peptide and nonpeptide receptors, ion channels, and transporters. EVP-6124 induces inward currents in Xenopus oocytes expressing human α7 subunit-containing nAChRs (EC50 = 0.16 µM). In vivo, EVP-6124 (0.1, 0.3, and 1 mg/kg) reverses scopolamine-induced deficits in the novel object recognition task and prevents natural forgetting of a familiar object in rats. It reduces premature responding, a measure of impulsivity, by low-attentive but not high-attentive female rats in the 5-choice serial reaction time test (5CSRTT).{52385}  

     

    Brand:
    Cayman
    SKU:30073 - 5 mg

    Available on backorder

  • EVP-6124 is a partial agonist of α7 subunit-containing nicotinic acetylcholine receptors (nAChRs; IC50 = 22.38 nM).{52384} It is 1,000-fold selective for α7 subunit-containing nAChRs over α4β2 subunit-containing nAChRs at 10 µM, as well as a panel of 60 peptide and nonpeptide receptors, ion channels, and transporters. EVP-6124 induces inward currents in Xenopus oocytes expressing human α7 subunit-containing nAChRs (EC50 = 0.16 µM). In vivo, EVP-6124 (0.1, 0.3, and 1 mg/kg) reverses scopolamine-induced deficits in the novel object recognition task and prevents natural forgetting of a familiar object in rats. It reduces premature responding, a measure of impulsivity, by low-attentive but not high-attentive female rats in the 5-choice serial reaction time test (5CSRTT).{52385}  

     

    Brand:
    Cayman
    SKU:30073 - 50 mg

    Available on backorder

  • EW-7197 is a potent inhibitor of activin receptor-like kinase 5 (ALK5, also known as TGF-β receptor type 1; IC50 = 12.9 nM).{34039,34042} It also inhibits ALK2 and ALK4 at nanomolar concentrations.{34042} EW-7197 blocks TGF-β/Smad signaling, cell migration, invasion, and lung metastasis in mouse mammary tumor virus/c-Neu mice and 4TI orthotopic-grafted mice.{34042} It also inhibits epithelial-to-mesenchymal transition (EMT) in TGF-β-treated breast cancer cells.{34042} EW-7197 is used to block TGF-β signaling and EMT in animal models of cancer and fibrosis.{34040,34041,34043}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • EW-7197 is a potent inhibitor of activin receptor-like kinase 5 (ALK5, also known as TGF-β receptor type 1; IC50 = 12.9 nM).{34039,34042} It also inhibits ALK2 and ALK4 at nanomolar concentrations.{34042} EW-7197 blocks TGF-β/Smad signaling, cell migration, invasion, and lung metastasis in mouse mammary tumor virus/c-Neu mice and 4TI orthotopic-grafted mice.{34042} It also inhibits epithelial-to-mesenchymal transition (EMT) in TGF-β-treated breast cancer cells.{34042} EW-7197 is used to block TGF-β signaling and EMT in animal models of cancer and fibrosis.{34040,34041,34043}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • EW-7197 is a potent inhibitor of activin receptor-like kinase 5 (ALK5, also known as TGF-β receptor type 1; IC50 = 12.9 nM).{34039,34042} It also inhibits ALK2 and ALK4 at nanomolar concentrations.{34042} EW-7197 blocks TGF-β/Smad signaling, cell migration, invasion, and lung metastasis in mouse mammary tumor virus/c-Neu mice and 4TI orthotopic-grafted mice.{34042} It also inhibits epithelial-to-mesenchymal transition (EMT) in TGF-β-treated breast cancer cells.{34042} EW-7197 is used to block TGF-β signaling and EMT in animal models of cancer and fibrosis.{34040,34041,34043}  

     

    Brand:
    Cayman
    SKU:-

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  • Exemestane is a third generation, irreversible steroidal aromatase inhibitor (Ki = 10.2 nM; Kinact = 26 nM) that induces aromatase degradation leading to a decrease in estrogen levels in plasma.{22655,22657} As an androgen analog, exemestane exhibits androgenic effects and has been shown to decrease total and HDL cholesterol, apo A1, and total triglyceride levels.{22656} Marketed under the trade name Aromasin™, exemestane has been used to treat estrogen receptor-positive breast cancers in post-menopausal women.{22655}  

     

    Brand:
    Cayman
    SKU:-
  • Exemestane is a third generation, irreversible steroidal aromatase inhibitor (Ki = 10.2 nM; Kinact = 26 nM) that induces aromatase degradation leading to a decrease in estrogen levels in plasma.{22655,22657} As an androgen analog, exemestane exhibits androgenic effects and has been shown to decrease total and HDL cholesterol, apo A1, and total triglyceride levels.{22656} Marketed under the trade name Aromasin™, exemestane has been used to treat estrogen receptor-positive breast cancers in post-menopausal women.{22655}  

     

    Brand:
    Cayman
    SKU:-
  • Exemestane is a third generation, irreversible steroidal aromatase inhibitor (Ki = 10.2 nM; Kinact = 26 nM) that induces aromatase degradation leading to a decrease in estrogen levels in plasma.{22655,22657} As an androgen analog, exemestane exhibits androgenic effects and has been shown to decrease total and HDL cholesterol, apo A1, and total triglyceride levels.{22656} Marketed under the trade name Aromasin™, exemestane has been used to treat estrogen receptor-positive breast cancers in post-menopausal women.{22655}  

     

    Brand:
    Cayman
    SKU:-
  • Exemestane is a third generation, irreversible steroidal aromatase inhibitor (Ki = 10.2 nM; Kinact = 26 nM) that induces aromatase degradation leading to a decrease in estrogen levels in plasma.{22655,22657} As an androgen analog, exemestane exhibits androgenic effects and has been shown to decrease total and HDL cholesterol, apo A1, and total triglyceride levels.{22656} Marketed under the trade name Aromasin™, exemestane has been used to treat estrogen receptor-positive breast cancers in post-menopausal women.{22655}  

     

    Brand:
    Cayman
    SKU:-
  • Exendin-3 (9-39) amide is a truncated form of the exendin-4 (Item No. 11096) peptide that acts as a potent competitive antagonist for the glucagon-like peptide 1 receptor (GLP-1R; Kd = 1.7 nM in CHL cells transfected with cloned human GLP-1).{27504} It inhibits exendin-3-induced increases in cAMP levels in guinea pig pancreas cells (IC50 = 20 nM).{34476} Exendin-3 (9-39) amide administration in the hypothalamus (10 and 100 µg, i.c.v.) reverses GLP-1 inhibition of feeding behavior in rats.{34477}  

     

    Brand:
    Cayman
    SKU:19890 -

    Available on backorder

  • Exendin-3 (9-39) amide is a truncated form of the exendin-4 (Item No. 11096) peptide that acts as a potent competitive antagonist for the glucagon-like peptide 1 receptor (GLP-1R; Kd = 1.7 nM in CHL cells transfected with cloned human GLP-1).{27504} It inhibits exendin-3-induced increases in cAMP levels in guinea pig pancreas cells (IC50 = 20 nM).{34476} Exendin-3 (9-39) amide administration in the hypothalamus (10 and 100 µg, i.c.v.) reverses GLP-1 inhibition of feeding behavior in rats.{34477}  

     

    Brand:
    Cayman
    SKU:19890 -

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  • Exendin-4 is a potent peptide agonist of the glucagon-like peptide 1 (GLP-1) receptor (Ki = 136 pM).{27501,27502,27504,24256} By activating the GLP-1 receptor, it stimulates glucose-induced insulin secretion in isolated rat islets and proinsulin expression in mouse insulinoma βTC-1 cells, supporting efficacy in type 2 diabetes.{27502} Exendin-4 was first isolated from the venom of H. horridum and consequently synthesized, with the recombinant peptide referred to as ‘exenatide.’ Exenatide protects hippocampal neurons against glutamate-induced apoptosis, suggesting utility in neuropathies associated with type 2 diabetes and in neurodegenerative diseases.{27503,27506} Exenatide also has anxiolytic and anti-depressant effects and induces satiety.{27506,27505}  

     

    Brand:
    Cayman
    SKU:11096 - 1 mg

    Available on backorder

  • Exendin-4 is a potent peptide agonist of the glucagon-like peptide 1 (GLP-1) receptor (Ki = 136 pM).{27501,27502,27504,24256} By activating the GLP-1 receptor, it stimulates glucose-induced insulin secretion in isolated rat islets and proinsulin expression in mouse insulinoma βTC-1 cells, supporting efficacy in type 2 diabetes.{27502} Exendin-4 was first isolated from the venom of H. horridum and consequently synthesized, with the recombinant peptide referred to as ‘exenatide.’ Exenatide protects hippocampal neurons against glutamate-induced apoptosis, suggesting utility in neuropathies associated with type 2 diabetes and in neurodegenerative diseases.{27503,27506} Exenatide also has anxiolytic and anti-depressant effects and induces satiety.{27506,27505}  

     

    Brand:
    Cayman
    SKU:11096 - 5 mg

    Available on backorder

  • Exendin-4 is a potent peptide agonist of the glucagon-like peptide 1 (GLP-1) receptor (Ki = 136 pM).{27501,27502,27504,24256} By activating the GLP-1 receptor, it stimulates glucose-induced insulin secretion in isolated rat islets and proinsulin expression in mouse insulinoma βTC-1 cells, supporting efficacy in type 2 diabetes.{27502} Exendin-4 was first isolated from the venom of H. horridum and consequently synthesized, with the recombinant peptide referred to as ‘exenatide.’ Exenatide protects hippocampal neurons against glutamate-induced apoptosis, suggesting utility in neuropathies associated with type 2 diabetes and in neurodegenerative diseases.{27503,27506} Exenatide also has anxiolytic and anti-depressant effects and induces satiety.{27506,27505}  

     

    Brand:
    Cayman
    SKU:11096 - 500 µg

    Available on backorder

  • Exo1 is a cell-permeable, reversible inhibitor of exocytosis (IC50 = 20 µM).{29668} It interferes with protein trafficking and secretion mediated by the Golgi apparatus and endoplasmic reticulum by dissociating the GTPase activator ADP-ribosylation factor (ARF1) from Golgi membranes, which leads to a consequent collapse of the Golgi apparatus.{29668}  

     

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    Cayman
    SKU:-

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  • Exo1 is a cell-permeable, reversible inhibitor of exocytosis (IC50 = 20 µM).{29668} It interferes with protein trafficking and secretion mediated by the Golgi apparatus and endoplasmic reticulum by dissociating the GTPase activator ADP-ribosylation factor (ARF1) from Golgi membranes, which leads to a consequent collapse of the Golgi apparatus.{29668}  

     

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    Cayman
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  • Programmed cell death in bacteria is dependent on a system of cell-to-cell communication termed quorum sensing. Extracellular death factor (EDF) is a linear pentapeptide that communicating cells produce and release, which upon reaching a sufficient concentration activates the cell death pathway in a subset of cells.{24994} It is sensitive to extreme pH, high temperatures, and other stressful conditions.{24994} At 2.5 ng/ml, EDF has been shown to facilitate mazEF-mediated cell death, significantly reducing population size in E. coli cultures.{24994}  

     

    Brand:
    Cayman
    SKU:-
  • Programmed cell death in bacteria is dependent on a system of cell-to-cell communication termed quorum sensing. Extracellular death factor (EDF) is a linear pentapeptide that communicating cells produce and release, which upon reaching a sufficient concentration activates the cell death pathway in a subset of cells.{24994} It is sensitive to extreme pH, high temperatures, and other stressful conditions.{24994} At 2.5 ng/ml, EDF has been shown to facilitate mazEF-mediated cell death, significantly reducing population size in E. coli cultures.{24994}  

     

    Brand:
    Cayman
    SKU:-
  • Glutathione S-transferases (GSTs) are ubiquitous multifunctional enzymes that play key roles in cellular detoxification and signal transduction by conjugating target substrates to glutathione. GSTP1-1, the most prevalent GST isozyme in nonhepatic tissues, binds to and inhibits the stress-activated c-Jun N-terminal kinase (JNK), an important regulator of cell proliferation, differentiation, and apoptosis.{27831} GSTP1-1 is overexpressed in many cancers and has been linked to drug resistance.{27832} Ezatiostat is a tripeptide analog of glutathione that can selectively inhibit GSTP1-1 catalytic activity (Ki = 400 nM) with minimal effect on the related GSTα and -µ families (Kis range from 20-75 µM).{27831} After intracellular de-esterification, the active form of ezatiostat, TLK117, binds to and inhibits GSTP1-1, restoring JNK-mediated cellular proliferation and differentiation signaling pathways.{27832,27833,27834} Ezatiostat has been shown to stimulate the proliferation of myeloid precursors in preclinical models and is under clinical examination for its potential prevention of myelosuppression in myelodysplastic syndrome.{27833,27834}  

     

    Brand:
    Cayman
    SKU:-
  • Glutathione S-transferases (GSTs) are ubiquitous multifunctional enzymes that play key roles in cellular detoxification and signal transduction by conjugating target substrates to glutathione. GSTP1-1, the most prevalent GST isozyme in nonhepatic tissues, binds to and inhibits the stress-activated c-Jun N-terminal kinase (JNK), an important regulator of cell proliferation, differentiation, and apoptosis.{27831} GSTP1-1 is overexpressed in many cancers and has been linked to drug resistance.{27832} Ezatiostat is a tripeptide analog of glutathione that can selectively inhibit GSTP1-1 catalytic activity (Ki = 400 nM) with minimal effect on the related GSTα and -µ families (Kis range from 20-75 µM).{27831} After intracellular de-esterification, the active form of ezatiostat, TLK117, binds to and inhibits GSTP1-1, restoring JNK-mediated cellular proliferation and differentiation signaling pathways.{27832,27833,27834} Ezatiostat has been shown to stimulate the proliferation of myeloid precursors in preclinical models and is under clinical examination for its potential prevention of myelosuppression in myelodysplastic syndrome.{27833,27834}  

     

    Brand:
    Cayman
    SKU:-
  • Glutathione S-transferases (GSTs) are ubiquitous multifunctional enzymes that play key roles in cellular detoxification and signal transduction by conjugating target substrates to glutathione. GSTP1-1, the most prevalent GST isozyme in nonhepatic tissues, binds to and inhibits the stress-activated c-Jun N-terminal kinase (JNK), an important regulator of cell proliferation, differentiation, and apoptosis.{27831} GSTP1-1 is overexpressed in many cancers and has been linked to drug resistance.{27832} Ezatiostat is a tripeptide analog of glutathione that can selectively inhibit GSTP1-1 catalytic activity (Ki = 400 nM) with minimal effect on the related GSTα and -µ families (Kis range from 20-75 µM).{27831} After intracellular de-esterification, the active form of ezatiostat, TLK117, binds to and inhibits GSTP1-1, restoring JNK-mediated cellular proliferation and differentiation signaling pathways.{27832,27833,27834} Ezatiostat has been shown to stimulate the proliferation of myeloid precursors in preclinical models and is under clinical examination for its potential prevention of myelosuppression in myelodysplastic syndrome.{27833,27834}  

     

    Brand:
    Cayman
    SKU:-
  • Glutathione S-transferases (GSTs) are ubiquitous multifunctional enzymes that play key roles in cellular detoxification and signal transduction by conjugating target substrates to glutathione. GSTP1-1, the most prevalent GST isozyme in nonhepatic tissues, binds to and inhibits the stress-activated c-Jun N-terminal kinase (JNK), an important regulator of cell proliferation, differentiation, and apoptosis.{27831} GSTP1-1 is overexpressed in many cancers and has been linked to drug resistance.{27832} Ezatiostat is a tripeptide analog of glutathione that can selectively inhibit GSTP1-1 catalytic activity (Ki = 400 nM) with minimal effect on the related GSTα and -µ families (Kis range from 20-75 µM).{27831} After intracellular de-esterification, the active form of ezatiostat, TLK117, binds to and inhibits GSTP1-1, restoring JNK-mediated cellular proliferation and differentiation signaling pathways.{27832,27833,27834} Ezatiostat has been shown to stimulate the proliferation of myeloid precursors in preclinical models and is under clinical examination for its potential prevention of myelosuppression in myelodysplastic syndrome.{27833,27834}  

     

    Brand:
    Cayman
    SKU:-
  • Ezetimibe inhibits intestinal cholesterol absorption by preventing cholesterol uptake by the Niemann-Pick C1-like 1 (NPC1L1) protein, a cholesterol transporter located in the apical membrane of enterocytes.{19679,15337,}Upon oral administration ezetimibe undergoes rapid glucuronidation in the intestine where its glucuronide binds NPC1L1.{19679,15337} Ezetimibe exhibits ED50 values of 0.0005-0.05 mg/kg in various animal models, selectively blocking cholesterol absorption without inhibiting pancreatic lipolytic enzyme activities in the intestinal lumen, affecting bile acid micelle solubilization of cholesterol, or interfering with the absorption of triglycerides, fatty acids, or bile acids.{19679,43023}  

     

    Brand:
    Cayman
    SKU:-

    Out of stock

  • Ezetimibe inhibits intestinal cholesterol absorption by preventing cholesterol uptake by the Niemann-Pick C1-like 1 (NPC1L1) protein, a cholesterol transporter located in the apical membrane of enterocytes.{19679,15337,}Upon oral administration ezetimibe undergoes rapid glucuronidation in the intestine where its glucuronide binds NPC1L1.{19679,15337} Ezetimibe exhibits ED50 values of 0.0005-0.05 mg/kg in various animal models, selectively blocking cholesterol absorption without inhibiting pancreatic lipolytic enzyme activities in the intestinal lumen, affecting bile acid micelle solubilization of cholesterol, or interfering with the absorption of triglycerides, fatty acids, or bile acids.{19679,43023}  

     

    Brand:
    Cayman
    SKU:-

    Out of stock

  • Ezetimibe inhibits intestinal cholesterol absorption by preventing cholesterol uptake by the Niemann-Pick C1-like 1 (NPC1L1) protein, a cholesterol transporter located in the apical membrane of enterocytes.{19679,15337,}Upon oral administration ezetimibe undergoes rapid glucuronidation in the intestine where its glucuronide binds NPC1L1.{19679,15337} Ezetimibe exhibits ED50 values of 0.0005-0.05 mg/kg in various animal models, selectively blocking cholesterol absorption without inhibiting pancreatic lipolytic enzyme activities in the intestinal lumen, affecting bile acid micelle solubilization of cholesterol, or interfering with the absorption of triglycerides, fatty acids, or bile acids.{19679,43023}  

     

    Brand:
    Cayman
    SKU:-

    Out of stock

  • Ezetimibe inhibits intestinal cholesterol absorption by preventing cholesterol uptake by the Niemann-Pick C1-like 1 (NPC1L1) protein, a cholesterol transporter located in the apical membrane of enterocytes.{19679,15337,}Upon oral administration ezetimibe undergoes rapid glucuronidation in the intestine where its glucuronide binds NPC1L1.{19679,15337} Ezetimibe exhibits ED50 values of 0.0005-0.05 mg/kg in various animal models, selectively blocking cholesterol absorption without inhibiting pancreatic lipolytic enzyme activities in the intestinal lumen, affecting bile acid micelle solubilization of cholesterol, or interfering with the absorption of triglycerides, fatty acids, or bile acids.{19679,43023}  

     

    Brand:
    Cayman
    SKU:-

    Out of stock

  • Ezetimibe hydroxy glucuronide is a minor phase II glucuronide metabolite of ezetimibe (Item No. 16331).{47182}  

     

    Brand:
    Cayman
    SKU:26602 - 1 mg

    Available on backorder

  • Ezetimibe hydroxy glucuronide is a minor phase II glucuronide metabolite of ezetimibe (Item No. 16331).{47182}  

     

    Brand:
    Cayman
    SKU:26602 - 500 µg

    Available on backorder

  • Ezetimibe-d4 is intended for use as an internal standard for the quantification of ezetimibe (Item No. 16331) by GC- or LC-MS. Ezetimibe inhibits intestinal cholesterol absorption by preventing cholesterol uptake by the Niemann-Pick C1-like 1 (NPC1L1) protein, a cholesterol transporter located in the apical membrane of enterocytes.{19679,15337} Upon oral administration ezetimibe undergoes rapid glucuronidation in the intestine where its glucuronide binds NPC1L1.{19679,15337} Ezetimibe exhibits ED50 values of 0.0005-0.05 mg/kg in various animal models, selectively blocking cholesterol absorption without inhibiting pancreatic lipolytic enzyme activities in the intestinal lumen, affecting bile acid micelle solubilization of cholesterol, or interfering with the absorption of triglycerides, fatty acids, or bile acids.{19679,43023}  

     

    Brand:
    Cayman
    SKU:25044 - 1 mg

    Available on backorder

  • EZM2302 is an inhibitor of protein arginine methyltransferase 4 (PRMT4; IC50 = 6 nM).{53436} It decreases asymmetric methylation of the PRMT4 substrate PABP1 (IC50 = 0.038 µM) and increases levels of demethylated SmB (EC50 = 0.018 µM) in RPMI-8226 multiple myeloma cells. EZM2302 inhibits proliferation in a panel of 36 hematopoietic cancer cell lines, with IC50 values of less than 100 μM for nine of the 15 multiple myeloma cell lines included in the panel. It reduces tumor growth and decreases asymmetric PABP1 methylation in tumor tissue in an RPMI-8226 mouse xenograft model when administered at doses of 75, 150, and 300 mg/kg twice per day. Intrathecal injection of EZM2302 (10 µg) reduces acute mechanical allodynia and thermal hyperalgesia in a mouse model of neuropathic pain induced by chronic constriction injury (CCI).{53437}  

     

    Brand:
    Cayman
    SKU:29954 - 1 mg

    Available on backorder

  • EZM2302 is an inhibitor of protein arginine methyltransferase 4 (PRMT4; IC50 = 6 nM).{53436} It decreases asymmetric methylation of the PRMT4 substrate PABP1 (IC50 = 0.038 µM) and increases levels of demethylated SmB (EC50 = 0.018 µM) in RPMI-8226 multiple myeloma cells. EZM2302 inhibits proliferation in a panel of 36 hematopoietic cancer cell lines, with IC50 values of less than 100 μM for nine of the 15 multiple myeloma cell lines included in the panel. It reduces tumor growth and decreases asymmetric PABP1 methylation in tumor tissue in an RPMI-8226 mouse xenograft model when administered at doses of 75, 150, and 300 mg/kg twice per day. Intrathecal injection of EZM2302 (10 µg) reduces acute mechanical allodynia and thermal hyperalgesia in a mouse model of neuropathic pain induced by chronic constriction injury (CCI).{53437}  

     

    Brand:
    Cayman
    SKU:29954 - 10 mg

    Available on backorder

  • EZM2302 is an inhibitor of protein arginine methyltransferase 4 (PRMT4; IC50 = 6 nM).{53436} It decreases asymmetric methylation of the PRMT4 substrate PABP1 (IC50 = 0.038 µM) and increases levels of demethylated SmB (EC50 = 0.018 µM) in RPMI-8226 multiple myeloma cells. EZM2302 inhibits proliferation in a panel of 36 hematopoietic cancer cell lines, with IC50 values of less than 100 μM for nine of the 15 multiple myeloma cell lines included in the panel. It reduces tumor growth and decreases asymmetric PABP1 methylation in tumor tissue in an RPMI-8226 mouse xenograft model when administered at doses of 75, 150, and 300 mg/kg twice per day. Intrathecal injection of EZM2302 (10 µg) reduces acute mechanical allodynia and thermal hyperalgesia in a mouse model of neuropathic pain induced by chronic constriction injury (CCI).{53437}  

     

    Brand:
    Cayman
    SKU:29954 - 5 mg

    Available on backorder

  • Ezutromid is an orally bioavailable small molecule that transcriptionally upregulates the utrophin gene, increasing both utrophin mRNA and protein.{32729} Through this action, ezutromid increases muscle function in dystrophin-deficient mdx mice, a mouse model of muscular dystrophy.{32729} A double-blind, placebo-controlled Phase I study demonstrated that ezutromid is safe and well tolerated in healthy volunteers.{32730}  

     

    Brand:
    Cayman
    SKU:20309 -

    Available on backorder

  • Ezutromid is an orally bioavailable small molecule that transcriptionally upregulates the utrophin gene, increasing both utrophin mRNA and protein.{32729} Through this action, ezutromid increases muscle function in dystrophin-deficient mdx mice, a mouse model of muscular dystrophy.{32729} A double-blind, placebo-controlled Phase I study demonstrated that ezutromid is safe and well tolerated in healthy volunteers.{32730}  

     

    Brand:
    Cayman
    SKU:20309 -

    Available on backorder

  • Ezutromid is an orally bioavailable small molecule that transcriptionally upregulates the utrophin gene, increasing both utrophin mRNA and protein.{32729} Through this action, ezutromid increases muscle function in dystrophin-deficient mdx mice, a mouse model of muscular dystrophy.{32729} A double-blind, placebo-controlled Phase I study demonstrated that ezutromid is safe and well tolerated in healthy volunteers.{32730}  

     

    Brand:
    Cayman
    SKU:20309 -

    Available on backorder

  • Ezutromid is an orally bioavailable small molecule that transcriptionally upregulates the utrophin gene, increasing both utrophin mRNA and protein.{32729} Through this action, ezutromid increases muscle function in dystrophin-deficient mdx mice, a mouse model of muscular dystrophy.{32729} A double-blind, placebo-controlled Phase I study demonstrated that ezutromid is safe and well tolerated in healthy volunteers.{32730}  

     

    Brand:
    Cayman
    SKU:20309 -

    Available on backorder

  • F-14329 is a tetramic acid fungal metabolite and a metal chelator that has been found in Chaunopycnis.{52470} It chelates iron, copper, magnesium, zinc, and aluminum ions in cell-free assays.  

     

    Brand:
    Cayman
    SKU:29999 - 1 mg

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  • F-amidine is an inhibitor of protein arginine deiminases (PADs) that is selective for PAD1 and PAD4 (IC50s = 29.5, 350, and 21.6 µM for PAD1, PAD3, and PAD4 in vitro, respectively).{18132,19982} It irreversibly inactivates all four PAD subtypes (kinact/KI = 2,800, 380, 170, and 3,000 M-1min-1 by covalently modifying an active site cysteine that is important for its catalytic activity.{18132,36047} F-amidine is cytotoxic to HL-60, MCF-7, and HT-29 cancer cell lines (IC50s = 0.5, 0.5 and 1 μM, respectively).{18529}  

     

    Brand:
    Cayman
    SKU:10610 - 1 mg

    Available on backorder

  • F-amidine is an inhibitor of protein arginine deiminases (PADs) that is selective for PAD1 and PAD4 (IC50s = 29.5, 350, and 21.6 µM for PAD1, PAD3, and PAD4 in vitro, respectively).{18132,19982} It irreversibly inactivates all four PAD subtypes (kinact/KI = 2,800, 380, 170, and 3,000 M-1min-1 by covalently modifying an active site cysteine that is important for its catalytic activity.{18132,36047} F-amidine is cytotoxic to HL-60, MCF-7, and HT-29 cancer cell lines (IC50s = 0.5, 0.5 and 1 μM, respectively).{18529}  

     

    Brand:
    Cayman
    SKU:10610 - 100 µg

    Available on backorder

  • F-amidine is an inhibitor of protein arginine deiminases (PADs) that is selective for PAD1 and PAD4 (IC50s = 29.5, 350, and 21.6 µM for PAD1, PAD3, and PAD4 in vitro, respectively).{18132,19982} It irreversibly inactivates all four PAD subtypes (kinact/KI = 2,800, 380, 170, and 3,000 M-1min-1 by covalently modifying an active site cysteine that is important for its catalytic activity.{18132,36047} F-amidine is cytotoxic to HL-60, MCF-7, and HT-29 cancer cell lines (IC50s = 0.5, 0.5 and 1 μM, respectively).{18529}  

     

    Brand:
    Cayman
    SKU:10610 - 250 µg

    Available on backorder

  • F-amidine is an inhibitor of protein arginine deiminases (PADs) that is selective for PAD1 and PAD4 (IC50s = 29.5, 350, and 21.6 µM for PAD1, PAD3, and PAD4 in vitro, respectively).{18132,19982} It irreversibly inactivates all four PAD subtypes (kinact/KI = 2,800, 380, 170, and 3,000 M-1min-1 by covalently modifying an active site cysteine that is important for its catalytic activity.{18132,36047} F-amidine is cytotoxic to HL-60, MCF-7, and HT-29 cancer cell lines (IC50s = 0.5, 0.5 and 1 μM, respectively).{18529}  

     

    Brand:
    Cayman
    SKU:10610 - 500 µg

    Available on backorder

  • F16 is a small, cationic, lipophilic molecule which binds preferentially to mitochondrial membranes and disrupts their function.{10295} F16 was discovered in high throughput screens for tumor inhibitors, where it was found to induce apoptosis in HER-1/EGFR-expressing breast carcinoma cell lines. In addition to being a potential antitumor agent, F16 is an easily visualized fluorescent molecule which can also be used to visualize mitochondria under confocal microscopy. The mechanism of apoptosis induction by F16 is believed to be through disruption of the mitochondrial transmembrane potential.{10295}  

     

    Brand:
    Cayman
    SKU:10022 - 1 mg

    Available on backorder

  • F16 is a small, cationic, lipophilic molecule which binds preferentially to mitochondrial membranes and disrupts their function.{10295} F16 was discovered in high throughput screens for tumor inhibitors, where it was found to induce apoptosis in HER-1/EGFR-expressing breast carcinoma cell lines. In addition to being a potential antitumor agent, F16 is an easily visualized fluorescent molecule which can also be used to visualize mitochondria under confocal microscopy. The mechanism of apoptosis induction by F16 is believed to be through disruption of the mitochondrial transmembrane potential.{10295}  

     

    Brand:
    Cayman
    SKU:10022 - 10 mg

    Available on backorder

  • F16 is a small, cationic, lipophilic molecule which binds preferentially to mitochondrial membranes and disrupts their function.{10295} F16 was discovered in high throughput screens for tumor inhibitors, where it was found to induce apoptosis in HER-1/EGFR-expressing breast carcinoma cell lines. In addition to being a potential antitumor agent, F16 is an easily visualized fluorescent molecule which can also be used to visualize mitochondria under confocal microscopy. The mechanism of apoptosis induction by F16 is believed to be through disruption of the mitochondrial transmembrane potential.{10295}  

     

    Brand:
    Cayman
    SKU:10022 - 5 mg

    Available on backorder

  • F16 is a small, cationic, lipophilic molecule which binds preferentially to mitochondrial membranes and disrupts their function.{10295} F16 was discovered in high throughput screens for tumor inhibitors, where it was found to induce apoptosis in HER-1/EGFR-expressing breast carcinoma cell lines. In addition to being a potential antitumor agent, F16 is an easily visualized fluorescent molecule which can also be used to visualize mitochondria under confocal microscopy. The mechanism of apoptosis induction by F16 is believed to be through disruption of the mitochondrial transmembrane potential.{10295}  

     

    Brand:
    Cayman
    SKU:10022 - 50 mg

    Available on backorder

  • AM2201 (Item No. 10707) is a potent synthetic cannabinoid (CB) that binds the CB1 and CB2 receptors with high affinity (Kis = 1.0 and 2.6 nM, respectively).{18696} F2201 is an analog of AM2201 with a fluorine at the 4 position of the naphthyl group. The physiological and toxicological properties of this compound have not been delineated. This product is intended for research and forensic purposes.  

     

    Brand:
    Cayman
    SKU:9001580 - 1 mg

    Available on backorder

  • AM2201 (Item No. 10707) is a potent synthetic cannabinoid (CB) that binds the CB1 and CB2 receptors with high affinity (Kis = 1.0 and 2.6 nM, respectively).{18696} F2201 is an analog of AM2201 with a fluorine at the 4 position of the naphthyl group. The physiological and toxicological properties of this compound have not been delineated. This product is intended for research and forensic purposes.  

     

    Brand:
    Cayman
    SKU:9001580 - 10 mg

    Available on backorder

  • AM2201 (Item No. 10707) is a potent synthetic cannabinoid (CB) that binds the CB1 and CB2 receptors with high affinity (Kis = 1.0 and 2.6 nM, respectively).{18696} F2201 is an analog of AM2201 with a fluorine at the 4 position of the naphthyl group. The physiological and toxicological properties of this compound have not been delineated. This product is intended for research and forensic purposes.  

     

    Brand:
    Cayman
    SKU:9001580 - 25 mg

    Available on backorder

  • AM2201 (Item No. 10707) is a potent synthetic cannabinoid (CB) that binds the CB1 and CB2 receptors with high affinity (Kis = 1.0 and 2.6 nM, respectively).{18696} F2201 is an analog of AM2201 with a fluorine at the 4 position of the naphthyl group. The physiological and toxicological properties of this compound have not been delineated. This product is intended for research and forensic purposes.  

     

    Brand:
    Cayman
    SKU:9001580 - 5 mg

    Available on backorder

  • FAD is a flavin dinucleotide that is synthesized when the AMP moiety from ATP is transferred onto riboflavin 5′-monophosphate (Item No. 18167).{38399} FAD functions as a coenzyme that facilitates the transfer of electrons by flavoenzymes in oxidation-reduction reactions in cells.{38400} FAD (0.0125-0.05% solution) reduces UV-B-induced death of human corneal epithelial cells in vitro.{38401}  

     

    Brand:
    Cayman
    SKU:23386 - 100 mg

    Available on backorder

  • FAD is a flavin dinucleotide that is synthesized when the AMP moiety from ATP is transferred onto riboflavin 5′-monophosphate (Item No. 18167).{38399} FAD functions as a coenzyme that facilitates the transfer of electrons by flavoenzymes in oxidation-reduction reactions in cells.{38400} FAD (0.0125-0.05% solution) reduces UV-B-induced death of human corneal epithelial cells in vitro.{38401}  

     

    Brand:
    Cayman
    SKU:23386 - 250 mg

    Available on backorder

  • FAD is a flavin dinucleotide that is synthesized when the AMP moiety from ATP is transferred onto riboflavin 5′-monophosphate (Item No. 18167).{38399} FAD functions as a coenzyme that facilitates the transfer of electrons by flavoenzymes in oxidation-reduction reactions in cells.{38400} FAD (0.0125-0.05% solution) reduces UV-B-induced death of human corneal epithelial cells in vitro.{38401}  

     

    Brand:
    Cayman
    SKU:23386 - 50 mg

    Available on backorder

  • FAD is a flavin dinucleotide that is synthesized when the AMP moiety from ATP is transferred onto riboflavin 5′-monophosphate (Item No. 18167).{38399} FAD functions as a coenzyme that facilitates the transfer of electrons by flavoenzymes in oxidation-reduction reactions in cells.{38400} FAD (0.0125-0.05% solution) reduces UV-B-induced death of human corneal epithelial cells in vitro.{38401}  

     

    Brand:
    Cayman
    SKU:23386 - 500 mg

    Available on backorder

  • Fadrozole is a non-steroidal aromatase inhibitor (IC50s = 5 and 1.4 nM for human placental and rat ovarian microsomal aromatase, respectively).{38819,38820} It selectively inhibits estrogen over progesterone production induced by luteinizing hormone (LH) in hamster ovarian tissue as well as corticosterone and aldosterone production induced by adrenocorticotropic hormone (ACTH; Item No. 24257) in rat adrenal tissue (IC50s = 0.03, 160, 100, and 1 μM, respectively).{38819} It also decreases ovarian estrogen levels in rats when administered at a dose of 0.26 mg/kg.{38820} Fadrozole inhibits conversion of cholesterol to 27-hydroxycholesterol by the cytochrome P450 (CYP) isomer 27A1 (Ki = 4.6 μM).{38821} It inhibits growth of androstenedione-stimulated mammary D2 cells implanted into thoracic mammary fat pads of mice by 95% when administered at a dose of 0.5 mg per animal per day.{38822}  

     

    Brand:
    Cayman
    SKU:24272 - 1 mg

    Available on backorder

  • Fadrozole is a non-steroidal aromatase inhibitor (IC50s = 5 and 1.4 nM for human placental and rat ovarian microsomal aromatase, respectively).{38819,38820} It selectively inhibits estrogen over progesterone production induced by luteinizing hormone (LH) in hamster ovarian tissue as well as corticosterone and aldosterone production induced by adrenocorticotropic hormone (ACTH; Item No. 24257) in rat adrenal tissue (IC50s = 0.03, 160, 100, and 1 μM, respectively).{38819} It also decreases ovarian estrogen levels in rats when administered at a dose of 0.26 mg/kg.{38820} Fadrozole inhibits conversion of cholesterol to 27-hydroxycholesterol by the cytochrome P450 (CYP) isomer 27A1 (Ki = 4.6 μM).{38821} It inhibits growth of androstenedione-stimulated mammary D2 cells implanted into thoracic mammary fat pads of mice by 95% when administered at a dose of 0.5 mg per animal per day.{38822}  

     

    Brand:
    Cayman
    SKU:24272 - 10 mg

    Available on backorder

  • Fadrozole is a non-steroidal aromatase inhibitor (IC50s = 5 and 1.4 nM for human placental and rat ovarian microsomal aromatase, respectively).{38819,38820} It selectively inhibits estrogen over progesterone production induced by luteinizing hormone (LH) in hamster ovarian tissue as well as corticosterone and aldosterone production induced by adrenocorticotropic hormone (ACTH; Item No. 24257) in rat adrenal tissue (IC50s = 0.03, 160, 100, and 1 μM, respectively).{38819} It also decreases ovarian estrogen levels in rats when administered at a dose of 0.26 mg/kg.{38820} Fadrozole inhibits conversion of cholesterol to 27-hydroxycholesterol by the cytochrome P450 (CYP) isomer 27A1 (Ki = 4.6 μM).{38821} It inhibits growth of androstenedione-stimulated mammary D2 cells implanted into thoracic mammary fat pads of mice by 95% when administered at a dose of 0.5 mg per animal per day.{38822}  

     

    Brand:
    Cayman
    SKU:24272 - 5 mg

    Available on backorder

  • FAI is a selective hydroxyl acylation analyzed by primer extension (SHAPE) electrophile reagent used to map RNA structures in vivo by forming stable 2’-hydroxy adducts with RNA, blocking reverse transcriptase elongation.{42234,42235} Its activity can be quenched by dithiothreitol (DTT) in vitro and in living cells.{42235} FAI has been used to probe the secondary structure of mouse embryonic stem cell 5S rRNA in vitro.{42234}  

     

    Brand:
    Cayman
    SKU:23429 - 1 mg

    Available on backorder

  • FAI is a selective hydroxyl acylation analyzed by primer extension (SHAPE) electrophile reagent used to map RNA structures in vivo by forming stable 2’-hydroxy adducts with RNA, blocking reverse transcriptase elongation.{42234,42235} Its activity can be quenched by dithiothreitol (DTT) in vitro and in living cells.{42235} FAI has been used to probe the secondary structure of mouse embryonic stem cell 5S rRNA in vitro.{42234}  

     

    Brand:
    Cayman
    SKU:23429 - 10 mg

    Available on backorder

  • FAI is a selective hydroxyl acylation analyzed by primer extension (SHAPE) electrophile reagent used to map RNA structures in vivo by forming stable 2’-hydroxy adducts with RNA, blocking reverse transcriptase elongation.{42234,42235} Its activity can be quenched by dithiothreitol (DTT) in vitro and in living cells.{42235} FAI has been used to probe the secondary structure of mouse embryonic stem cell 5S rRNA in vitro.{42234}  

     

    Brand:
    Cayman
    SKU:23429 - 25 mg

    Available on backorder

  • FAI is a selective hydroxyl acylation analyzed by primer extension (SHAPE) electrophile reagent used to map RNA structures in vivo by forming stable 2’-hydroxy adducts with RNA, blocking reverse transcriptase elongation.{42234,42235} Its activity can be quenched by dithiothreitol (DTT) in vitro and in living cells.{42235} FAI has been used to probe the secondary structure of mouse embryonic stem cell 5S rRNA in vitro.{42234}  

     

    Brand:
    Cayman
    SKU:23429 - 5 mg

    Available on backorder

  • Focal adhesion kinases (FAK) are non-receptor tyrosine kinases that play roles in regulating diverse processes, including cell adhesion, spreading, migration, proliferation, and apoptosis.{15630} They are over-expressed in many types of cancer. FAK inhibitor 14 is a direct inhibitor of FAK1 autophosphorylation, blocking phosphorylation of Y397 with an IC50 value of about 1 μM.{23133} There is no known significant effect on the activity of a range of other kinases. FAK inhibitor 14 promotes cell detachment and inhibits cell adhesion of cells in culture.{23133} Moreover, it blocks tumor growth in vivo.{23133,23132,23134} FAK inhibitor 14 has also been used to demonstrate a role for FAK in the regulation of aortic stiffness.{23131}  

     

    Brand:
    Cayman
    SKU:-
  • Focal adhesion kinases (FAK) are non-receptor tyrosine kinases that play roles in regulating diverse processes, including cell adhesion, spreading, migration, proliferation, and apoptosis.{15630} They are over-expressed in many types of cancer. FAK inhibitor 14 is a direct inhibitor of FAK1 autophosphorylation, blocking phosphorylation of Y397 with an IC50 value of about 1 μM.{23133} There is no known significant effect on the activity of a range of other kinases. FAK inhibitor 14 promotes cell detachment and inhibits cell adhesion of cells in culture.{23133} Moreover, it blocks tumor growth in vivo.{23133,23132,23134} FAK inhibitor 14 has also been used to demonstrate a role for FAK in the regulation of aortic stiffness.{23131}  

     

    Brand:
    Cayman
    SKU:-
  • Focal adhesion kinases (FAK) are non-receptor tyrosine kinases that play roles in regulating diverse processes, including cell adhesion, spreading, migration, proliferation, and apoptosis.{15630} They are over-expressed in many types of cancer. FAK inhibitor 14 is a direct inhibitor of FAK1 autophosphorylation, blocking phosphorylation of Y397 with an IC50 value of about 1 μM.{23133} There is no known significant effect on the activity of a range of other kinases. FAK inhibitor 14 promotes cell detachment and inhibits cell adhesion of cells in culture.{23133} Moreover, it blocks tumor growth in vivo.{23133,23132,23134} FAK inhibitor 14 has also been used to demonstrate a role for FAK in the regulation of aortic stiffness.{23131}  

     

    Brand:
    Cayman
    SKU:-
  • Focal adhesion kinases (FAK) are non-receptor tyrosine kinases that play roles in regulating diverse processes, including cell adhesion, spreading, migration, proliferation, and apoptosis.{15630} They are over-expressed in many types of cancer. FAK inhibitor 14 is a direct inhibitor of FAK1 autophosphorylation, blocking phosphorylation of Y397 with an IC50 value of about 1 μM.{23133} There is no known significant effect on the activity of a range of other kinases. FAK inhibitor 14 promotes cell detachment and inhibits cell adhesion of cells in culture.{23133} Moreover, it blocks tumor growth in vivo.{23133,23132,23134} FAK inhibitor 14 has also been used to demonstrate a role for FAK in the regulation of aortic stiffness.{23131}  

     

    Brand:
    Cayman
    SKU:-
  • Falcarinol is a C17-polyacetylene produced by the Apiaceae family that has antimicrobial properties due to its inhibition of fatty acid biosynthesis.{38102,38105} Falcarinol binds to the human recombinant cannabinoid (CB) receptors, CB1 and CB2, (Kis = 594 and 2,100 nM, respectively) in an [3H]anandamide displacement assay in HEK293 cells.{38104} It differentially modulates synaptic and extrasynaptic GABAA receptors in a recombinant HEK293 system.{38101} In vitro assays of ATPase activity demonstrate that falcarinol inhibits breast cancer resistance protein ATP-binding cassette sub-family G member 2 (ABCG2; IC50 = 79.3 μM), a drug efflux transporter and mediator of drug resistance.{38106} Falcarinol (6.88 μg/g feed) also inhibits aberrant crypt foci by 26.6% in azoxymethane-induced rats.{38103}  

     

    Brand:
    Cayman
    SKU:22407 -

    Out of stock

  • Falcarinol is a C17-polyacetylene produced by the Apiaceae family that has antimicrobial properties due to its inhibition of fatty acid biosynthesis.{38102,38105} Falcarinol binds to the human recombinant cannabinoid (CB) receptors, CB1 and CB2, (Kis = 594 and 2,100 nM, respectively) in an [3H]anandamide displacement assay in HEK293 cells.{38104} It differentially modulates synaptic and extrasynaptic GABAA receptors in a recombinant HEK293 system.{38101} In vitro assays of ATPase activity demonstrate that falcarinol inhibits breast cancer resistance protein ATP-binding cassette sub-family G member 2 (ABCG2; IC50 = 79.3 μM), a drug efflux transporter and mediator of drug resistance.{38106} Falcarinol (6.88 μg/g feed) also inhibits aberrant crypt foci by 26.6% in azoxymethane-induced rats.{38103}  

     

    Brand:
    Cayman
    SKU:22407 -

    Out of stock

  • Falcarinol is a C17-polyacetylene produced by the Apiaceae family that has antimicrobial properties due to its inhibition of fatty acid biosynthesis.{38102,38105} Falcarinol binds to the human recombinant cannabinoid (CB) receptors, CB1 and CB2, (Kis = 594 and 2,100 nM, respectively) in an [3H]anandamide displacement assay in HEK293 cells.{38104} It differentially modulates synaptic and extrasynaptic GABAA receptors in a recombinant HEK293 system.{38101} In vitro assays of ATPase activity demonstrate that falcarinol inhibits breast cancer resistance protein ATP-binding cassette sub-family G member 2 (ABCG2; IC50 = 79.3 μM), a drug efflux transporter and mediator of drug resistance.{38106} Falcarinol (6.88 μg/g feed) also inhibits aberrant crypt foci by 26.6% in azoxymethane-induced rats.{38103}  

     

    Brand:
    Cayman
    SKU:22407 -

    Out of stock

  • Falcarinol is a C17-polyacetylene produced by the Apiaceae family that has antimicrobial properties due to its inhibition of fatty acid biosynthesis.{38102,38105} Falcarinol binds to the human recombinant cannabinoid (CB) receptors, CB1 and CB2, (Kis = 594 and 2,100 nM, respectively) in an [3H]anandamide displacement assay in HEK293 cells.{38104} It differentially modulates synaptic and extrasynaptic GABAA receptors in a recombinant HEK293 system.{38101} In vitro assays of ATPase activity demonstrate that falcarinol inhibits breast cancer resistance protein ATP-binding cassette sub-family G member 2 (ABCG2; IC50 = 79.3 μM), a drug efflux transporter and mediator of drug resistance.{38106} Falcarinol (6.88 μg/g feed) also inhibits aberrant crypt foci by 26.6% in azoxymethane-induced rats.{38103}  

     

    Brand:
    Cayman
    SKU:22407 -

    Out of stock

  • Famciclovir is an orally bioavailable prodrug form of the antiviral guanosine analog penciclovir (Item No. 22918).{39519} Famciclovir is rapidly deacetylated and oxidized in vivo to form penciclovir, which is active against clinical isolates of herpes simplex virus 1 (HSV-1), HSV-2, and varicella-zoster virus (VZV) in a plaque reduction assay with IC50 values of 1.6, 6, and 12 μM, respectively. Both famciclovir and the product of its deacetylation, 6-deoxypenciclovir, are oxidized in vitro by human, guinea pig, and rat liver aldehyde oxidase, with 6-deoxypenciclovir being converted to penciclovir.{39520} Peak plasma concentrations of penciclovir (mean 3.5 μg/ml) are reached 0.5 hours after oral administration of famciclovir (40 mg/kg) in rats.{39521} Famciclovir (25 mg/kg) has a longer half-life in dogs, with peak concentrations of penciclovir (mean 4.4 μg/ml) in plasma occurring after 3 hours.  

     

    Brand:
    Cayman
    SKU:23834 - 100 mg

    Available on backorder

  • Famciclovir is an orally bioavailable prodrug form of the antiviral guanosine analog penciclovir (Item No. 22918).{39519} Famciclovir is rapidly deacetylated and oxidized in vivo to form penciclovir, which is active against clinical isolates of herpes simplex virus 1 (HSV-1), HSV-2, and varicella-zoster virus (VZV) in a plaque reduction assay with IC50 values of 1.6, 6, and 12 μM, respectively. Both famciclovir and the product of its deacetylation, 6-deoxypenciclovir, are oxidized in vitro by human, guinea pig, and rat liver aldehyde oxidase, with 6-deoxypenciclovir being converted to penciclovir.{39520} Peak plasma concentrations of penciclovir (mean 3.5 μg/ml) are reached 0.5 hours after oral administration of famciclovir (40 mg/kg) in rats.{39521} Famciclovir (25 mg/kg) has a longer half-life in dogs, with peak concentrations of penciclovir (mean 4.4 μg/ml) in plasma occurring after 3 hours.  

     

    Brand:
    Cayman
    SKU:23834 - 25 mg

    Available on backorder

  • Famciclovir is an orally bioavailable prodrug form of the antiviral guanosine analog penciclovir (Item No. 22918).{39519} Famciclovir is rapidly deacetylated and oxidized in vivo to form penciclovir, which is active against clinical isolates of herpes simplex virus 1 (HSV-1), HSV-2, and varicella-zoster virus (VZV) in a plaque reduction assay with IC50 values of 1.6, 6, and 12 μM, respectively. Both famciclovir and the product of its deacetylation, 6-deoxypenciclovir, are oxidized in vitro by human, guinea pig, and rat liver aldehyde oxidase, with 6-deoxypenciclovir being converted to penciclovir.{39520} Peak plasma concentrations of penciclovir (mean 3.5 μg/ml) are reached 0.5 hours after oral administration of famciclovir (40 mg/kg) in rats.{39521} Famciclovir (25 mg/kg) has a longer half-life in dogs, with peak concentrations of penciclovir (mean 4.4 μg/ml) in plasma occurring after 3 hours.  

     

    Brand:
    Cayman
    SKU:23834 - 250 mg

    Available on backorder

  • Famciclovir is an orally bioavailable prodrug form of the antiviral guanosine analog penciclovir (Item No. 22918).{39519} Famciclovir is rapidly deacetylated and oxidized in vivo to form penciclovir, which is active against clinical isolates of herpes simplex virus 1 (HSV-1), HSV-2, and varicella-zoster virus (VZV) in a plaque reduction assay with IC50 values of 1.6, 6, and 12 μM, respectively. Both famciclovir and the product of its deacetylation, 6-deoxypenciclovir, are oxidized in vitro by human, guinea pig, and rat liver aldehyde oxidase, with 6-deoxypenciclovir being converted to penciclovir.{39520} Peak plasma concentrations of penciclovir (mean 3.5 μg/ml) are reached 0.5 hours after oral administration of famciclovir (40 mg/kg) in rats.{39521} Famciclovir (25 mg/kg) has a longer half-life in dogs, with peak concentrations of penciclovir (mean 4.4 μg/ml) in plasma occurring after 3 hours.  

     

    Brand:
    Cayman
    SKU:23834 - 50 mg

    Available on backorder

  • Famotidine is a histamine H2 receptor antagonist with a Ki value of 12 nM in fractionated guinea pig cerebral cortex membranes.{36463} It is selective for H2 over H1 and muscarinic receptors (Kis = 4 and 28 µM, respectively, in bovine cerebral cortex).{23214} Famotidine inhibits histamine-induced acid secretion in isolated canine parietal cells (IC50 = 0.6 µM).{17620} It also suppresses histamine-induced gastric acid secretion in dogs when administered orally and in anesthetized rats when administered intraduodenally (ID50s = 10 and 400 µg/kg, respectively).{17620} Formulations containing famotidine have been used in the treatment of ulcers, gastroesophageal reflux disease (GERD), and heartburn, as well as to decrease the risk of gastrointestinal toxicity associated with non-steroidal anti-inflammatory drugs (NSAIDs).  

     

    Brand:
    Cayman
    SKU:23828 - 1 g

    Available on backorder

  • Famotidine is a histamine H2 receptor antagonist with a Ki value of 12 nM in fractionated guinea pig cerebral cortex membranes.{36463} It is selective for H2 over H1 and muscarinic receptors (Kis = 4 and 28 µM, respectively, in bovine cerebral cortex).{23214} Famotidine inhibits histamine-induced acid secretion in isolated canine parietal cells (IC50 = 0.6 µM).{17620} It also suppresses histamine-induced gastric acid secretion in dogs when administered orally and in anesthetized rats when administered intraduodenally (ID50s = 10 and 400 µg/kg, respectively).{17620} Formulations containing famotidine have been used in the treatment of ulcers, gastroesophageal reflux disease (GERD), and heartburn, as well as to decrease the risk of gastrointestinal toxicity associated with non-steroidal anti-inflammatory drugs (NSAIDs).  

     

    Brand:
    Cayman
    SKU:23828 - 10 g

    Available on backorder

  • Famotidine is a histamine H2 receptor antagonist with a Ki value of 12 nM in fractionated guinea pig cerebral cortex membranes.{36463} It is selective for H2 over H1 and muscarinic receptors (Kis = 4 and 28 µM, respectively, in bovine cerebral cortex).{23214} Famotidine inhibits histamine-induced acid secretion in isolated canine parietal cells (IC50 = 0.6 µM).{17620} It also suppresses histamine-induced gastric acid secretion in dogs when administered orally and in anesthetized rats when administered intraduodenally (ID50s = 10 and 400 µg/kg, respectively).{17620} Formulations containing famotidine have been used in the treatment of ulcers, gastroesophageal reflux disease (GERD), and heartburn, as well as to decrease the risk of gastrointestinal toxicity associated with non-steroidal anti-inflammatory drugs (NSAIDs).  

     

    Brand:
    Cayman
    SKU:23828 - 25 g

    Available on backorder

  • Famotidine is a histamine H2 receptor antagonist with a Ki value of 12 nM in fractionated guinea pig cerebral cortex membranes.{36463} It is selective for H2 over H1 and muscarinic receptors (Kis = 4 and 28 µM, respectively, in bovine cerebral cortex).{23214} Famotidine inhibits histamine-induced acid secretion in isolated canine parietal cells (IC50 = 0.6 µM).{17620} It also suppresses histamine-induced gastric acid secretion in dogs when administered orally and in anesthetized rats when administered intraduodenally (ID50s = 10 and 400 µg/kg, respectively).{17620} Formulations containing famotidine have been used in the treatment of ulcers, gastroesophageal reflux disease (GERD), and heartburn, as well as to decrease the risk of gastrointestinal toxicity associated with non-steroidal anti-inflammatory drugs (NSAIDs).  

     

    Brand:
    Cayman
    SKU:23828 - 5 g

    Available on backorder

  • Fangchinoline is an alkaloid that has been found in S. tetrandrae and has diverse biological activities, including anti-inflammatory, neuroprotective, and anticancer properties.{52160,52161,52162} It inhibits the activity of sheep COX and decreases IL-6-induced proliferation of MH60 mouse hybridoma cells with IC50 values of 129 and 3.7 µM, respectively.{52160} Fangchinoline (1 and 10 µM) reduces cyanide-induced increases in secreted glutamate levels and cell death in primary neonatal rat cerebellar granule neurons.{52161} It decreases proliferation of PC3 human prostate cancer cells by 63 and 86% when used at concentrations of 20 and 30 µM, respectively.{52162} Fangchinoline reduces tumor growth in a PC3 mouse xenograft model when administered at a dose of 5 mg/kg per day for 12 days.  

     

    Brand:
    Cayman
    SKU:29243 - 10 mg

    Available on backorder

  • Fangchinoline is an alkaloid that has been found in S. tetrandrae and has diverse biological activities, including anti-inflammatory, neuroprotective, and anticancer properties.{52160,52161,52162} It inhibits the activity of sheep COX and decreases IL-6-induced proliferation of MH60 mouse hybridoma cells with IC50 values of 129 and 3.7 µM, respectively.{52160} Fangchinoline (1 and 10 µM) reduces cyanide-induced increases in secreted glutamate levels and cell death in primary neonatal rat cerebellar granule neurons.{52161} It decreases proliferation of PC3 human prostate cancer cells by 63 and 86% when used at concentrations of 20 and 30 µM, respectively.{52162} Fangchinoline reduces tumor growth in a PC3 mouse xenograft model when administered at a dose of 5 mg/kg per day for 12 days.  

     

    Brand:
    Cayman
    SKU:29243 - 100 mg

    Available on backorder

  • Fangchinoline is an alkaloid that has been found in S. tetrandrae and has diverse biological activities, including anti-inflammatory, neuroprotective, and anticancer properties.{52160,52161,52162} It inhibits the activity of sheep COX and decreases IL-6-induced proliferation of MH60 mouse hybridoma cells with IC50 values of 129 and 3.7 µM, respectively.{52160} Fangchinoline (1 and 10 µM) reduces cyanide-induced increases in secreted glutamate levels and cell death in primary neonatal rat cerebellar granule neurons.{52161} It decreases proliferation of PC3 human prostate cancer cells by 63 and 86% when used at concentrations of 20 and 30 µM, respectively.{52162} Fangchinoline reduces tumor growth in a PC3 mouse xenograft model when administered at a dose of 5 mg/kg per day for 12 days.  

     

    Brand:
    Cayman
    SKU:29243 - 5 mg

    Available on backorder

  • Fangchinoline is an alkaloid that has been found in S. tetrandrae and has diverse biological activities, including anti-inflammatory, neuroprotective, and anticancer properties.{52160,52161,52162} It inhibits the activity of sheep COX and decreases IL-6-induced proliferation of MH60 mouse hybridoma cells with IC50 values of 129 and 3.7 µM, respectively.{52160} Fangchinoline (1 and 10 µM) reduces cyanide-induced increases in secreted glutamate levels and cell death in primary neonatal rat cerebellar granule neurons.{52161} It decreases proliferation of PC3 human prostate cancer cells by 63 and 86% when used at concentrations of 20 and 30 µM, respectively.{52162} Fangchinoline reduces tumor growth in a PC3 mouse xenograft model when administered at a dose of 5 mg/kg per day for 12 days.  

     

    Brand:
    Cayman
    SKU:29243 - 50 mg

    Available on backorder

  • Fantofarone is a calcium channel inhibitor.{47567} It selectively inhibits the L-type voltage-gated calcium channel in isolated rat aorta (IC50 = 0.61 nM) over α1- and β-adrenergic, muscarinic, and histamine H2 receptors in rat heart homogenates (IC50s = >10, 4, >10, and >10 µM, respectively), and the serotonin receptor subtypes 5-HT1 and 5-HT2, as well as histamine H1 and adenosine A1 receptors, in rat brain homogenates (IC50s = >10, >10, 4, and >10 µM, respectively). Fantofarone inhibits peak calcium current in depolarized and hyperpolarized L-type voltage-gated calcium channels (IC50s = 1.4 and 150 nM, respectively).{47568} It inhibits potassium chloride- and norepinephrine-induced contractions in isolated rat aorta (IC50s = 5.64 and 96 nM, respectively).{47567} It enhances recovery of cardiac output during reperfusion of isolated rat hearts when used at a concentration of 10 nM.{47569} Fantofarone prevents angioplasty-induced vasospasms in the femoral artery in a rabbit model of focal atherosclerosis when administered at a dose of 50 µg/kg.{47570}  

     

    Brand:
    Cayman
    SKU:26381 - 1 mg

    Available on backorder

  • Fantofarone is a calcium channel inhibitor.{47567} It selectively inhibits the L-type voltage-gated calcium channel in isolated rat aorta (IC50 = 0.61 nM) over α1- and β-adrenergic, muscarinic, and histamine H2 receptors in rat heart homogenates (IC50s = >10, 4, >10, and >10 µM, respectively), and the serotonin receptor subtypes 5-HT1 and 5-HT2, as well as histamine H1 and adenosine A1 receptors, in rat brain homogenates (IC50s = >10, >10, 4, and >10 µM, respectively). Fantofarone inhibits peak calcium current in depolarized and hyperpolarized L-type voltage-gated calcium channels (IC50s = 1.4 and 150 nM, respectively).{47568} It inhibits potassium chloride- and norepinephrine-induced contractions in isolated rat aorta (IC50s = 5.64 and 96 nM, respectively).{47567} It enhances recovery of cardiac output during reperfusion of isolated rat hearts when used at a concentration of 10 nM.{47569} Fantofarone prevents angioplasty-induced vasospasms in the femoral artery in a rabbit model of focal atherosclerosis when administered at a dose of 50 µg/kg.{47570}  

     

    Brand:
    Cayman
    SKU:26381 - 10 mg

    Available on backorder

  • Fantofarone is a calcium channel inhibitor.{47567} It selectively inhibits the L-type voltage-gated calcium channel in isolated rat aorta (IC50 = 0.61 nM) over α1- and β-adrenergic, muscarinic, and histamine H2 receptors in rat heart homogenates (IC50s = >10, 4, >10, and >10 µM, respectively), and the serotonin receptor subtypes 5-HT1 and 5-HT2, as well as histamine H1 and adenosine A1 receptors, in rat brain homogenates (IC50s = >10, >10, 4, and >10 µM, respectively). Fantofarone inhibits peak calcium current in depolarized and hyperpolarized L-type voltage-gated calcium channels (IC50s = 1.4 and 150 nM, respectively).{47568} It inhibits potassium chloride- and norepinephrine-induced contractions in isolated rat aorta (IC50s = 5.64 and 96 nM, respectively).{47567} It enhances recovery of cardiac output during reperfusion of isolated rat hearts when used at a concentration of 10 nM.{47569} Fantofarone prevents angioplasty-induced vasospasms in the femoral artery in a rabbit model of focal atherosclerosis when administered at a dose of 50 µg/kg.{47570}  

     

    Brand:
    Cayman
    SKU:26381 - 25 mg

    Available on backorder

  • Fantofarone is a calcium channel inhibitor.{47567} It selectively inhibits the L-type voltage-gated calcium channel in isolated rat aorta (IC50 = 0.61 nM) over α1- and β-adrenergic, muscarinic, and histamine H2 receptors in rat heart homogenates (IC50s = >10, 4, >10, and >10 µM, respectively), and the serotonin receptor subtypes 5-HT1 and 5-HT2, as well as histamine H1 and adenosine A1 receptors, in rat brain homogenates (IC50s = >10, >10, 4, and >10 µM, respectively). Fantofarone inhibits peak calcium current in depolarized and hyperpolarized L-type voltage-gated calcium channels (IC50s = 1.4 and 150 nM, respectively).{47568} It inhibits potassium chloride- and norepinephrine-induced contractions in isolated rat aorta (IC50s = 5.64 and 96 nM, respectively).{47567} It enhances recovery of cardiac output during reperfusion of isolated rat hearts when used at a concentration of 10 nM.{47569} Fantofarone prevents angioplasty-induced vasospasms in the femoral artery in a rabbit model of focal atherosclerosis when administered at a dose of 50 µg/kg.{47570}  

     

    Brand:
    Cayman
    SKU:26381 - 5 mg

    Available on backorder

  • Farampator is a positive allosteric modulator of AMPA receptors that has an EC50 value greater than 32 µM for evoking glutamate currents in isolated pyramidal neurons.{39175} In rats, it enhances novel object recognition memory (0.1 mg/kg, p.o.) and attentional set-shifting (0.3 mg/kg, p.o.) and reverses a scopolamine-induced deficit in cued fear conditioning (0.1 mg/kg, p.o.).{39176}  

     

    Brand:
    Cayman
    SKU:21510 -

    Out of stock

  • Farampator is a positive allosteric modulator of AMPA receptors that has an EC50 value greater than 32 µM for evoking glutamate currents in isolated pyramidal neurons.{39175} In rats, it enhances novel object recognition memory (0.1 mg/kg, p.o.) and attentional set-shifting (0.3 mg/kg, p.o.) and reverses a scopolamine-induced deficit in cued fear conditioning (0.1 mg/kg, p.o.).{39176}  

     

    Brand:
    Cayman
    SKU:21510 -

    Out of stock

  • Farampator is a positive allosteric modulator of AMPA receptors that has an EC50 value greater than 32 µM for evoking glutamate currents in isolated pyramidal neurons.{39175} In rats, it enhances novel object recognition memory (0.1 mg/kg, p.o.) and attentional set-shifting (0.3 mg/kg, p.o.) and reverses a scopolamine-induced deficit in cued fear conditioning (0.1 mg/kg, p.o.).{39176}  

     

    Brand:
    Cayman
    SKU:21510 -

    Out of stock

  • Farnesyl alcohol is an isoprenoid originally isolated from plants but also produced in mammals, including humans, as an intermediate in the mevalonate biosynthesis pathway.{39250} It acts as an agonist at the peroxisome proliferator-activated receptors PPARα and PPARγ (ED50s = 5.5 and 28 µM, respectively).{39249} Farnesyl alcohol has broad anticancer properties in vitro and in xenograft mouse models, inhibiting proliferation, slowing tumor growth, and inducing apoptosis.{39246,39245,39247} In addition, it acts as a quorum sensing molecule in fungi, including C. albicans, where it reduces virulence by blocking the transition from yeast to mycelium.{39244,39248}  

     

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  • Farnesyl alcohol is an isoprenoid originally isolated from plants but also produced in mammals, including humans, as an intermediate in the mevalonate biosynthesis pathway.{39250} It acts as an agonist at the peroxisome proliferator-activated receptors PPARα and PPARγ (ED50s = 5.5 and 28 µM, respectively).{39249} Farnesyl alcohol has broad anticancer properties in vitro and in xenograft mouse models, inhibiting proliferation, slowing tumor growth, and inducing apoptosis.{39246,39245,39247} In addition, it acts as a quorum sensing molecule in fungi, including C. albicans, where it reduces virulence by blocking the transition from yeast to mycelium.{39244,39248}  

     

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  • Protein farnesylation is a posttranslational modification where a farnesyl isoprenoid moiety is attached to cysteine residues located near the C-terminus of proteins. Farnesyl alcohol azide acts as a replacement for endogenously-produced farnesyl alcohol and becomes attached to proteins through normal biological processes in cells or animals.{17990} The terminal azide group can then be used in simple chemical linking reactions, known as click chemistry, to readily tag farnesylated proteins for subsequent analysis.{17990,17991,17992}  

     

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  • Protein farnesylation is a posttranslational modification where a farnesyl isoprenoid moiety is attached to cysteine residues located near the C-terminus of proteins. Farnesyl alcohol azide acts as a replacement for endogenously-produced farnesyl alcohol and becomes attached to proteins through normal biological processes in cells or animals.{17990} The terminal azide group can then be used in simple chemical linking reactions, known as click chemistry, to readily tag farnesylated proteins for subsequent analysis.{17990,17991,17992}  

     

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  • Protein farnesylation is a posttranslational modification where a farnesyl isoprenoid moiety is attached to cysteine residues located near the C-terminus of proteins. Farnesyl alcohol azide acts as a replacement for endogenously-produced farnesyl alcohol and becomes attached to proteins through normal biological processes in cells or animals.{17990} The terminal azide group can then be used in simple chemical linking reactions, known as click chemistry, to readily tag farnesylated proteins for subsequent analysis.{17990,17991,17992}  

     

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  • Farnesyl pyrophosphate is an intermediate in the HMG-CoA reductase pathway and used in the biosynthesis of terpenes, terpenoids, and sterols.{8343} It also serves as a donor in post-translational isoprenylation of proteins.{24323} FPP has been identified as an antagonist of P2Y12 receptors (IC50 = 45 μM), attenuating platelet aggregation.{24324} It has also been shown to regulate adipocyte function as an endogenous PPARγ agonist.{24326} Additionally, because of a flexible hydrocarbon chain that enables different conformations, FPP is a promiscuous ligand for a subset of nuclear receptors.{24325}  

     

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    Cayman
    SKU:63250 - 1 mg

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  • Farnesyl pyrophosphate is an intermediate in the HMG-CoA reductase pathway and used in the biosynthesis of terpenes, terpenoids, and sterols.{8343} It also serves as a donor in post-translational isoprenylation of proteins.{24323} FPP has been identified as an antagonist of P2Y12 receptors (IC50 = 45 μM), attenuating platelet aggregation.{24324} It has also been shown to regulate adipocyte function as an endogenous PPARγ agonist.{24326} Additionally, because of a flexible hydrocarbon chain that enables different conformations, FPP is a promiscuous ligand for a subset of nuclear receptors.{24325}  

     

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    Cayman
    SKU:63250 - 250 µg

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  • Farnesyl pyrophosphate is an intermediate in the HMG-CoA reductase pathway and used in the biosynthesis of terpenes, terpenoids, and sterols.{8343} It also serves as a donor in post-translational isoprenylation of proteins.{24323} FPP has been identified as an antagonist of P2Y12 receptors (IC50 = 45 μM), attenuating platelet aggregation.{24324} It has also been shown to regulate adipocyte function as an endogenous PPARγ agonist.{24326} Additionally, because of a flexible hydrocarbon chain that enables different conformations, FPP is a promiscuous ligand for a subset of nuclear receptors.{24325}  

     

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    Cayman
    SKU:63250 - 5 mg

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  • Farnesyl pyrophosphate is an intermediate in the HMG-CoA reductase pathway and used in the biosynthesis of terpenes, terpenoids, and sterols.{8343} It also serves as a donor in post-translational isoprenylation of proteins.{24323} FPP has been identified as an antagonist of P2Y12 receptors (IC50 = 45 μM), attenuating platelet aggregation.{24324} It has also been shown to regulate adipocyte function as an endogenous PPARγ agonist.{24326} Additionally, because of a flexible hydrocarbon chain that enables different conformations, FPP is a promiscuous ligand for a subset of nuclear receptors.{24325}  

     

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    Cayman
    SKU:63250 - 500 µg

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  • Association of Ras protein with the inner surface of the plasma membrane is required for Ras signaling activity. Farnesyl thiosalicylic acid (FTS) is an inhibitor of Ras-mediated signaling that functions by dislodging Ras from the cell membrane thereby rendering it susceptible to proteolytic degradation.{15696} FTS inhibits the growth of human Ha-ras-transformed Rat1 fibroblasts with an IC50 value of 7.5 µM.{15698} It does not inhibit Ras farnesylation in vitro and although FTS does inhibit prenylated protein methyltransferase (PPMTase) in cell-free systems with a Ki value of 2.6 µM, it is relatively ineffective at inhibiting methylation in whole cells.{15695} Treatment of chow-fed ApoE-deficient mice with 5 mg/kg FTS three times per week for six weeks reduces early atherosclerotic lesion development by 52% compared to controls.{15694}  

     

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    Cayman
    SKU:10010501 - 10 mg

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  • Association of Ras protein with the inner surface of the plasma membrane is required for Ras signaling activity. Farnesyl thiosalicylic acid (FTS) is an inhibitor of Ras-mediated signaling that functions by dislodging Ras from the cell membrane thereby rendering it susceptible to proteolytic degradation.{15696} FTS inhibits the growth of human Ha-ras-transformed Rat1 fibroblasts with an IC50 value of 7.5 µM.{15698} It does not inhibit Ras farnesylation in vitro and although FTS does inhibit prenylated protein methyltransferase (PPMTase) in cell-free systems with a Ki value of 2.6 µM, it is relatively ineffective at inhibiting methylation in whole cells.{15695} Treatment of chow-fed ApoE-deficient mice with 5 mg/kg FTS three times per week for six weeks reduces early atherosclerotic lesion development by 52% compared to controls.{15694}  

     

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    Cayman
    SKU:10010501 - 25 mg

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  • Association of Ras protein with the inner surface of the plasma membrane is required for Ras signaling activity. Farnesyl thiosalicylic acid (FTS) is an inhibitor of Ras-mediated signaling that functions by dislodging Ras from the cell membrane thereby rendering it susceptible to proteolytic degradation.{15696} FTS inhibits the growth of human Ha-ras-transformed Rat1 fibroblasts with an IC50 value of 7.5 µM.{15698} It does not inhibit Ras farnesylation in vitro and although FTS does inhibit prenylated protein methyltransferase (PPMTase) in cell-free systems with a Ki value of 2.6 µM, it is relatively ineffective at inhibiting methylation in whole cells.{15695} Treatment of chow-fed ApoE-deficient mice with 5 mg/kg FTS three times per week for six weeks reduces early atherosclerotic lesion development by 52% compared to controls.{15694}  

     

    Brand:
    Cayman
    SKU:10010501 - 5 mg

    Available on backorder

  • Association of Ras protein with the inner surface of the plasma membrane is required for Ras signaling activity. Farnesyl thiosalicylic acid (FTS) is an inhibitor of Ras-mediated signaling that functions by dislodging Ras from the cell membrane thereby rendering it susceptible to proteolytic degradation.{15696} FTS inhibits the growth of human Ha-ras-transformed Rat1 fibroblasts with an IC50 value of 7.5 µM.{15698} It does not inhibit Ras farnesylation in vitro and although FTS does inhibit prenylated protein methyltransferase (PPMTase) in cell-free systems with a Ki value of 2.6 µM, it is relatively ineffective at inhibiting methylation in whole cells.{15695} Treatment of chow-fed ApoE-deficient mice with 5 mg/kg FTS three times per week for six weeks reduces early atherosclerotic lesion development by 52% compared to controls.{15694}  

     

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    Cayman
    SKU:10010501 - 50 mg

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  • Association of Ras protein with the inner surface of the plasma membrane is required for Ras signaling activity. Farnesyl thiosalicylic acid (FTS) amide is an FTS derivative with an amide added to the carboxyl group. FTS amide inhibits the growth of PANC-1 and U87 tumor cells with IC50 values of 20 and 10 µM, respectively, a relatively higher potency compared to that of FTS (IC50s = 35 and 50 µM, respectively).{16693} Treatment of nude mice bearing either U87 glioblastoma or PANC-1 tumors with 100 mg/kg FTS amide twice daily for four days inhibits tumor growth by at least 50% of controls.  

     

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  • Association of Ras protein with the inner surface of the plasma membrane is required for Ras signaling activity. Farnesyl thiosalicylic acid (FTS) amide is an FTS derivative with an amide added to the carboxyl group. FTS amide inhibits the growth of PANC-1 and U87 tumor cells with IC50 values of 20 and 10 µM, respectively, a relatively higher potency compared to that of FTS (IC50s = 35 and 50 µM, respectively).{16693} Treatment of nude mice bearing either U87 glioblastoma or PANC-1 tumors with 100 mg/kg FTS amide twice daily for four days inhibits tumor growth by at least 50% of controls.  

     

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    Cayman
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  • Association of Ras protein with the inner surface of the plasma membrane is required for Ras signaling activity. Farnesyl thiosalicylic acid (FTS) amide is an FTS derivative with an amide added to the carboxyl group. FTS amide inhibits the growth of PANC-1 and U87 tumor cells with IC50 values of 20 and 10 µM, respectively, a relatively higher potency compared to that of FTS (IC50s = 35 and 50 µM, respectively).{16693} Treatment of nude mice bearing either U87 glioblastoma or PANC-1 tumors with 100 mg/kg FTS amide twice daily for four days inhibits tumor growth by at least 50% of controls.  

     

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    Cayman
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  • Association of Ras protein with the inner surface of the plasma membrane is required for Ras signaling activity. Farnesyl thiosalicylic acid (FTS) amide is an FTS derivative with an amide added to the carboxyl group. FTS amide inhibits the growth of PANC-1 and U87 tumor cells with IC50 values of 20 and 10 µM, respectively, a relatively higher potency compared to that of FTS (IC50s = 35 and 50 µM, respectively).{16693} Treatment of nude mice bearing either U87 glioblastoma or PANC-1 tumors with 100 mg/kg FTS amide twice daily for four days inhibits tumor growth by at least 50% of controls.  

     

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  • Fascaplysin is an inhibitor of cyclin D kinase 4/ cyclin D1 (IC50 = 0.35 μM) that was originally isolated from the marine sponge Thorectandra.{33462} It is significantly less selective for Cdk6/cyclin D1 (IC50 = 3.4 μM) and does not inhibit other Cdks and tyrosine kinases.{33462} Fascaplysin is reported to have antiproliferative activity against retinoblastoma-positive tumor cells, blocking retinoblastoma phosphorylation and inducing G1 arrest.{33462} Inhibition of Cdk4 via fascaplysin has been shown to induce peroxisome-proliferator-activated receptor γ-1α deacetylation (IC50 = 0.7 µM) and has been used to demonstrate a role for insulin-activated cyclinD1-Cdk4 signaling in the control of glucose metabolism.{26552}  

     

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    Cayman
    SKU:21715 -

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  • Fascaplysin is an inhibitor of cyclin D kinase 4/ cyclin D1 (IC50 = 0.35 μM) that was originally isolated from the marine sponge Thorectandra.{33462} It is significantly less selective for Cdk6/cyclin D1 (IC50 = 3.4 μM) and does not inhibit other Cdks and tyrosine kinases.{33462} Fascaplysin is reported to have antiproliferative activity against retinoblastoma-positive tumor cells, blocking retinoblastoma phosphorylation and inducing G1 arrest.{33462} Inhibition of Cdk4 via fascaplysin has been shown to induce peroxisome-proliferator-activated receptor γ-1α deacetylation (IC50 = 0.7 µM) and has been used to demonstrate a role for insulin-activated cyclinD1-Cdk4 signaling in the control of glucose metabolism.{26552}  

     

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    Cayman
    SKU:21715 -

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  • Fasentin is an inhibitor of glucose transport.{43670} It partially inhibits glucose uptake in U937 and DU145 cells when used at concentrations ranging from 15 to 80 µM. Fasentin sensitizes PPC-1 prostate cancer and U937 leukemia cells, but not DU145 prostate cancer cells, to cell death induced by the Fas receptor activator CH-11 activating anti-Fas antibody (FAS). It also increases the expression of AspSyn and PCK2, genes associated with glucose deprivation, in PPC-1 cells and halts the cell cycle at the G0/G1 phase in U937 cells when used at concentrations of 50 and 40 µM, respectively.  

     

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    Cayman
    SKU:27050 - 1 mg

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  • Fasentin is an inhibitor of glucose transport.{43670} It partially inhibits glucose uptake in U937 and DU145 cells when used at concentrations ranging from 15 to 80 µM. Fasentin sensitizes PPC-1 prostate cancer and U937 leukemia cells, but not DU145 prostate cancer cells, to cell death induced by the Fas receptor activator CH-11 activating anti-Fas antibody (FAS). It also increases the expression of AspSyn and PCK2, genes associated with glucose deprivation, in PPC-1 cells and halts the cell cycle at the G0/G1 phase in U937 cells when used at concentrations of 50 and 40 µM, respectively.  

     

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    Cayman
    SKU:27050 - 10 mg

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  • Fasentin is an inhibitor of glucose transport.{43670} It partially inhibits glucose uptake in U937 and DU145 cells when used at concentrations ranging from 15 to 80 µM. Fasentin sensitizes PPC-1 prostate cancer and U937 leukemia cells, but not DU145 prostate cancer cells, to cell death induced by the Fas receptor activator CH-11 activating anti-Fas antibody (FAS). It also increases the expression of AspSyn and PCK2, genes associated with glucose deprivation, in PPC-1 cells and halts the cell cycle at the G0/G1 phase in U937 cells when used at concentrations of 50 and 40 µM, respectively.  

     

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    Cayman
    SKU:27050 - 25 mg

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  • Fasentin is an inhibitor of glucose transport.{43670} It partially inhibits glucose uptake in U937 and DU145 cells when used at concentrations ranging from 15 to 80 µM. Fasentin sensitizes PPC-1 prostate cancer and U937 leukemia cells, but not DU145 prostate cancer cells, to cell death induced by the Fas receptor activator CH-11 activating anti-Fas antibody (FAS). It also increases the expression of AspSyn and PCK2, genes associated with glucose deprivation, in PPC-1 cells and halts the cell cycle at the G0/G1 phase in U937 cells when used at concentrations of 50 and 40 µM, respectively.  

     

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    Cayman
    SKU:27050 - 5 mg

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  • Fast Green FCF is a dye used to stain proteins for IEF (isoelectric focusing) and SDS-PAGE. When bound to proteins, Fast Green FCF fluoresces near infrared (absorption maximum: 624 nm).{22804} Fast Green FCF staining is linear over a wider range of protein concentrations compared to Brilliant Blue R.  

     

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  • Fast Green FCF is a dye used to stain proteins for IEF (isoelectric focusing) and SDS-PAGE. When bound to proteins, Fast Green FCF fluoresces near infrared (absorption maximum: 624 nm).{22804} Fast Green FCF staining is linear over a wider range of protein concentrations compared to Brilliant Blue R.  

     

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    Cayman
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  • Fast Green FCF is a dye used to stain proteins for IEF (isoelectric focusing) and SDS-PAGE. When bound to proteins, Fast Green FCF fluoresces near infrared (absorption maximum: 624 nm).{22804} Fast Green FCF staining is linear over a wider range of protein concentrations compared to Brilliant Blue R.  

     

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    Cayman
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  • Fast Green FCF is a dye used to stain proteins for IEF (isoelectric focusing) and SDS-PAGE. When bound to proteins, Fast Green FCF fluoresces near infrared (absorption maximum: 624 nm).{22804} Fast Green FCF staining is linear over a wider range of protein concentrations compared to Brilliant Blue R.  

     

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    Cayman
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  • Sterol regulatory element binding proteins (SREBPs) are transcription factors that have pivotal roles in lipogenesis and fat metabolism.{15316} The activation of SREBPs requires escort to the Golgi by SREBP cleavage-activating protein (SCAP) followed by proteolytic release of SREBP from the Golgi.{15551} Fatostatin is an inhibitor of SREBP activation, preventing SCAP-mediated escort of either SREBP-1 or SREBP-2 to the Golgi (IC50 = 5.6 µM).{17397,23867} This blocks constitutive SREBP-mediated gene expression in the human prostate cancer cell line DU145.{17397} Fatostatin prevents insulin-induced adipogenesis of 3T3-L1 cells as well as growth induced by insulin-like growth factor 1 in DU145 cells (IC50 = 0.1 µM).{23869} Through its actions on SCAP/SREBP-1, it inhibits high glucose-induced upregulation of TGF-β in primary rat mesangial cells.{23868} This compound also alters lipid metabolism in vivo, reducing hepatic fat accumulation in ob/ob mice.{17397}  

     

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    Cayman
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  • Sterol regulatory element binding proteins (SREBPs) are transcription factors that have pivotal roles in lipogenesis and fat metabolism.{15316} The activation of SREBPs requires escort to the Golgi by SREBP cleavage-activating protein (SCAP) followed by proteolytic release of SREBP from the Golgi.{15551} Fatostatin is an inhibitor of SREBP activation, preventing SCAP-mediated escort of either SREBP-1 or SREBP-2 to the Golgi (IC50 = 5.6 µM).{17397,23867} This blocks constitutive SREBP-mediated gene expression in the human prostate cancer cell line DU145.{17397} Fatostatin prevents insulin-induced adipogenesis of 3T3-L1 cells as well as growth induced by insulin-like growth factor 1 in DU145 cells (IC50 = 0.1 µM).{23869} Through its actions on SCAP/SREBP-1, it inhibits high glucose-induced upregulation of TGF-β in primary rat mesangial cells.{23868} This compound also alters lipid metabolism in vivo, reducing hepatic fat accumulation in ob/ob mice.{17397}  

     

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    Cayman
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  • Sterol regulatory element binding proteins (SREBPs) are transcription factors that have pivotal roles in lipogenesis and fat metabolism.{15316} The activation of SREBPs requires escort to the Golgi by SREBP cleavage-activating protein (SCAP) followed by proteolytic release of SREBP from the Golgi.{15551} Fatostatin is an inhibitor of SREBP activation, preventing SCAP-mediated escort of either SREBP-1 or SREBP-2 to the Golgi (IC50 = 5.6 µM).{17397,23867} This blocks constitutive SREBP-mediated gene expression in the human prostate cancer cell line DU145.{17397} Fatostatin prevents insulin-induced adipogenesis of 3T3-L1 cells as well as growth induced by insulin-like growth factor 1 in DU145 cells (IC50 = 0.1 µM).{23869} Through its actions on SCAP/SREBP-1, it inhibits high glucose-induced upregulation of TGF-β in primary rat mesangial cells.{23868} This compound also alters lipid metabolism in vivo, reducing hepatic fat accumulation in ob/ob mice.{17397}  

     

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    Cayman
    SKU:-
  • Sterol regulatory element binding proteins (SREBPs) are transcription factors that have pivotal roles in lipogenesis and fat metabolism.{15316} The activation of SREBPs requires escort to the Golgi by SREBP cleavage-activating protein (SCAP) followed by proteolytic release of SREBP from the Golgi.{15551} Fatostatin is an inhibitor of SREBP activation, preventing SCAP-mediated escort of either SREBP-1 or SREBP-2 to the Golgi (IC50 = 5.6 µM).{17397,23867} This blocks constitutive SREBP-mediated gene expression in the human prostate cancer cell line DU145.{17397} Fatostatin prevents insulin-induced adipogenesis of 3T3-L1 cells as well as growth induced by insulin-like growth factor 1 in DU145 cells (IC50 = 0.1 µM).{23869} Through its actions on SCAP/SREBP-1, it inhibits high glucose-induced upregulation of TGF-β in primary rat mesangial cells.{23868} This compound also alters lipid metabolism in vivo, reducing hepatic fat accumulation in ob/ob mice.{17397}  

     

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    Cayman
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  • FAUC-365 is a dopamine D3 receptor antagonist (Ki = 0.5 nM).{42635} It is selective for dopamine D3 receptors over dopamine D1, D2L, D2S, and D4 receptors (Kis = 8.8, 3.6, 2.6, and 0.34 µM, respectively) as well as the serotonin (5-HT) receptor subtypes 5-HT1A and 5-HT2 (Kis = 0.36 and 2 µM, respectively). FAUC-365 (1-10 mg/kg) prevents memory impairment in the novel object recognition test in dopamine transporter knockdown (DAT-KD) mice when administered prior to object learning.{42636}  

     

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    Cayman
    SKU:20457 -

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