Chemicals

Showing 9901–10050 of 41137 results

  • ARN14686 is an activity-based affinity probe for the detection of N-acylethanolamine acid amidase (NAAA) using click chemistry.{36895} It binds covalently to the N-terminal cysteine of catalytically active NAAA to form a thioester adduct. ARN14686 inhibits the hydrolysis of the NAAA substrate PAMCA in HEK293 cells (IC50s = 6 and 13 nM for human and rat recombinant enzymes, respectively) and is selective for NAAA over acid ceramidase (IC50 = 1,200 nM for the rat enzyme). It labels NAAA in HEK293 cells overexpressing human or rat recombinant NAAA and, when used at concentrations of 1 and 10 µM, in rat lung lysosomal fractions in vitro. It also detects NAAA in lung lysosomal fractions following intravenous administration at a dose of 10 mg/kg in rats. ARN14686 (3 mg/kg) has been used to determine that catalytically active NAAA is present in inflamed rat paw in a complete Freund’s adjuvant model of inflammation.{36896}  

     

    Brand:
    Cayman
    SKU:24261 - 1 mg

    Available on backorder

  • ARN14686 is an activity-based affinity probe for the detection of N-acylethanolamine acid amidase (NAAA) using click chemistry.{36895} It binds covalently to the N-terminal cysteine of catalytically active NAAA to form a thioester adduct. ARN14686 inhibits the hydrolysis of the NAAA substrate PAMCA in HEK293 cells (IC50s = 6 and 13 nM for human and rat recombinant enzymes, respectively) and is selective for NAAA over acid ceramidase (IC50 = 1,200 nM for the rat enzyme). It labels NAAA in HEK293 cells overexpressing human or rat recombinant NAAA and, when used at concentrations of 1 and 10 µM, in rat lung lysosomal fractions in vitro. It also detects NAAA in lung lysosomal fractions following intravenous administration at a dose of 10 mg/kg in rats. ARN14686 (3 mg/kg) has been used to determine that catalytically active NAAA is present in inflamed rat paw in a complete Freund’s adjuvant model of inflammation.{36896}  

     

    Brand:
    Cayman
    SKU:24261 - 10 mg

    Available on backorder

  • ARN14686 is an activity-based affinity probe for the detection of N-acylethanolamine acid amidase (NAAA) using click chemistry.{36895} It binds covalently to the N-terminal cysteine of catalytically active NAAA to form a thioester adduct. ARN14686 inhibits the hydrolysis of the NAAA substrate PAMCA in HEK293 cells (IC50s = 6 and 13 nM for human and rat recombinant enzymes, respectively) and is selective for NAAA over acid ceramidase (IC50 = 1,200 nM for the rat enzyme). It labels NAAA in HEK293 cells overexpressing human or rat recombinant NAAA and, when used at concentrations of 1 and 10 µM, in rat lung lysosomal fractions in vitro. It also detects NAAA in lung lysosomal fractions following intravenous administration at a dose of 10 mg/kg in rats. ARN14686 (3 mg/kg) has been used to determine that catalytically active NAAA is present in inflamed rat paw in a complete Freund’s adjuvant model of inflammation.{36896}  

     

    Brand:
    Cayman
    SKU:24261 - 25 mg

    Available on backorder

  • ARN14686 is an activity-based affinity probe for the detection of N-acylethanolamine acid amidase (NAAA) using click chemistry.{36895} It binds covalently to the N-terminal cysteine of catalytically active NAAA to form a thioester adduct. ARN14686 inhibits the hydrolysis of the NAAA substrate PAMCA in HEK293 cells (IC50s = 6 and 13 nM for human and rat recombinant enzymes, respectively) and is selective for NAAA over acid ceramidase (IC50 = 1,200 nM for the rat enzyme). It labels NAAA in HEK293 cells overexpressing human or rat recombinant NAAA and, when used at concentrations of 1 and 10 µM, in rat lung lysosomal fractions in vitro. It also detects NAAA in lung lysosomal fractions following intravenous administration at a dose of 10 mg/kg in rats. ARN14686 (3 mg/kg) has been used to determine that catalytically active NAAA is present in inflamed rat paw in a complete Freund’s adjuvant model of inflammation.{36896}  

     

    Brand:
    Cayman
    SKU:24261 - 5 mg

    Available on backorder

  • ARN14974 is a benzoxazolone carboxamide inhibitor of acid ceramidase (IC50 = 79 nM).{27811} It inhibits acid ceramidase activity, reduces levels of sphingosine and dihydroceramide, and increases levels of ceramide in SW403 adenocarcinoma cells and RAW 264.7 murine macrophages when used at concentrations ranging from 0.1 to 20 mM. In vivo, ARN14974 (10 mg/kg, i.v.) reduces acid ceramidase activity in multiple organs, including brain, liver, heart, lungs, and kidney, and increases pulmonary ceramide levels in mice.  

     

    Brand:
    Cayman
    SKU:-

    Out of stock

  • ARN14974 is a benzoxazolone carboxamide inhibitor of acid ceramidase (IC50 = 79 nM).{27811} It inhibits acid ceramidase activity, reduces levels of sphingosine and dihydroceramide, and increases levels of ceramide in SW403 adenocarcinoma cells and RAW 264.7 murine macrophages when used at concentrations ranging from 0.1 to 20 mM. In vivo, ARN14974 (10 mg/kg, i.v.) reduces acid ceramidase activity in multiple organs, including brain, liver, heart, lungs, and kidney, and increases pulmonary ceramide levels in mice.  

     

    Brand:
    Cayman
    SKU:-

    Out of stock

  • ARN14974 is a benzoxazolone carboxamide inhibitor of acid ceramidase (IC50 = 79 nM).{27811} It inhibits acid ceramidase activity, reduces levels of sphingosine and dihydroceramide, and increases levels of ceramide in SW403 adenocarcinoma cells and RAW 264.7 murine macrophages when used at concentrations ranging from 0.1 to 20 mM. In vivo, ARN14974 (10 mg/kg, i.v.) reduces acid ceramidase activity in multiple organs, including brain, liver, heart, lungs, and kidney, and increases pulmonary ceramide levels in mice.  

     

    Brand:
    Cayman
    SKU:-

    Out of stock

  • ARN14974 is a benzoxazolone carboxamide inhibitor of acid ceramidase (IC50 = 79 nM).{27811} It inhibits acid ceramidase activity, reduces levels of sphingosine and dihydroceramide, and increases levels of ceramide in SW403 adenocarcinoma cells and RAW 264.7 murine macrophages when used at concentrations ranging from 0.1 to 20 mM. In vivo, ARN14974 (10 mg/kg, i.v.) reduces acid ceramidase activity in multiple organs, including brain, liver, heart, lungs, and kidney, and increases pulmonary ceramide levels in mice.  

     

    Brand:
    Cayman
    SKU:-

    Out of stock

  • ARN14988 is a potent inhibitor of acid ceramidase (IC50 = 12.8 nM for the human enzyme).{40582} It inhibits acid ceramidase activity and increases levels of C16 dihydro ceramide (Item No. 24369) and C16 ceramide (Item No. 10681) in A375, G361, M14, MeWo, MNT-1, and SK-MEL-28 melanoma cells. ARN14988 also reduces growth of A375 and G361 melanoma cells (EC50s = 41.8 and 67.7 µM, respectively).  

     

    Brand:
    Cayman
    SKU:24284 - 1 mg

    Available on backorder

  • ARN14988 is a potent inhibitor of acid ceramidase (IC50 = 12.8 nM for the human enzyme).{40582} It inhibits acid ceramidase activity and increases levels of C16 dihydro ceramide (Item No. 24369) and C16 ceramide (Item No. 10681) in A375, G361, M14, MeWo, MNT-1, and SK-MEL-28 melanoma cells. ARN14988 also reduces growth of A375 and G361 melanoma cells (EC50s = 41.8 and 67.7 µM, respectively).  

     

    Brand:
    Cayman
    SKU:24284 - 10 mg

    Available on backorder

  • ARN14988 is a potent inhibitor of acid ceramidase (IC50 = 12.8 nM for the human enzyme).{40582} It inhibits acid ceramidase activity and increases levels of C16 dihydro ceramide (Item No. 24369) and C16 ceramide (Item No. 10681) in A375, G361, M14, MeWo, MNT-1, and SK-MEL-28 melanoma cells. ARN14988 also reduces growth of A375 and G361 melanoma cells (EC50s = 41.8 and 67.7 µM, respectively).  

     

    Brand:
    Cayman
    SKU:24284 - 25 mg

    Available on backorder

  • ARN14988 is a potent inhibitor of acid ceramidase (IC50 = 12.8 nM for the human enzyme).{40582} It inhibits acid ceramidase activity and increases levels of C16 dihydro ceramide (Item No. 24369) and C16 ceramide (Item No. 10681) in A375, G361, M14, MeWo, MNT-1, and SK-MEL-28 melanoma cells. ARN14988 also reduces growth of A375 and G361 melanoma cells (EC50s = 41.8 and 67.7 µM, respectively).  

     

    Brand:
    Cayman
    SKU:24284 - 5 mg

    Available on backorder

  • ARN19874 is an inhibitor of N-acyl phosphatidylethanolamine phospholipase D (NAPE-PLD; IC50 = 33.7 µM).{40567} It is selective for NAPD-PLD over carbonic anhydrase II, neutral endopeptidase, and angiotensin-converting enzyme (ACE) up to 50 µM. ARN19874 (50 µM) increases the levels of certain NAPE substrates and decreases the endogenous levels of stearoyl ethanolamide (Item No. 90245), but not oleoyl ethanolamide (Item No. 90265) or palmitoyl ethanolamide (Item No. 90350), in HEK293 cells.  

     

    Brand:
    Cayman
    SKU:24283 - 1 mg

    Available on backorder

  • ARN19874 is an inhibitor of N-acyl phosphatidylethanolamine phospholipase D (NAPE-PLD; IC50 = 33.7 µM).{40567} It is selective for NAPD-PLD over carbonic anhydrase II, neutral endopeptidase, and angiotensin-converting enzyme (ACE) up to 50 µM. ARN19874 (50 µM) increases the levels of certain NAPE substrates and decreases the endogenous levels of stearoyl ethanolamide (Item No. 90245), but not oleoyl ethanolamide (Item No. 90265) or palmitoyl ethanolamide (Item No. 90350), in HEK293 cells.  

     

    Brand:
    Cayman
    SKU:24283 - 10 mg

    Available on backorder

  • ARN19874 is an inhibitor of N-acyl phosphatidylethanolamine phospholipase D (NAPE-PLD; IC50 = 33.7 µM).{40567} It is selective for NAPD-PLD over carbonic anhydrase II, neutral endopeptidase, and angiotensin-converting enzyme (ACE) up to 50 µM. ARN19874 (50 µM) increases the levels of certain NAPE substrates and decreases the endogenous levels of stearoyl ethanolamide (Item No. 90245), but not oleoyl ethanolamide (Item No. 90265) or palmitoyl ethanolamide (Item No. 90350), in HEK293 cells.  

     

    Brand:
    Cayman
    SKU:24283 - 5 mg

    Available on backorder

  • ARN19874 is an inhibitor of N-acyl phosphatidylethanolamine phospholipase D (NAPE-PLD; IC50 = 33.7 µM).{40567} It is selective for NAPD-PLD over carbonic anhydrase II, neutral endopeptidase, and angiotensin-converting enzyme (ACE) up to 50 µM. ARN19874 (50 µM) increases the levels of certain NAPE substrates and decreases the endogenous levels of stearoyl ethanolamide (Item No. 90245), but not oleoyl ethanolamide (Item No. 90265) or palmitoyl ethanolamide (Item No. 90350), in HEK293 cells.  

     

    Brand:
    Cayman
    SKU:24283 - 500 µg

    Available on backorder

  • ARN3236 is an inhibitor of salt-inducible kinase 2 (SIK2; IC50 = 50s = 21.63 and 6.63 nM, respectively). It inhibits TNF-α secretion in RAW 264.7 cells (IC50 = ~2.5 µM) and reduces phosphorylation of the SIK2 targets CRTC3 and HDAC4 in macrophages when used at a concentration of 3 µM. ARN3236 inhibits growth of 10 ovarian cancer cell lines (IC50s = 0.8-2.6 µM) and increases the sensitivity of eight of them to paclitaxel (Item No. 10461).{54419} It halts the cell cycle at the G2/M phase and induces apoptosis and tetraploidy in SKOV3 cells when used at a concentration of 1 µM. ARN3236 (60 mg/kg per day) has an additive effect on reducing tumor growth when used in combination with paclitaxel in an ovarian cancer mouse xenograft model.  

     

    Brand:
    Cayman
    SKU:31457 - 1 mg

    Available on backorder

  • ARN3236 is an inhibitor of salt-inducible kinase 2 (SIK2; IC50 = 50s = 21.63 and 6.63 nM, respectively). It inhibits TNF-α secretion in RAW 264.7 cells (IC50 = ~2.5 µM) and reduces phosphorylation of the SIK2 targets CRTC3 and HDAC4 in macrophages when used at a concentration of 3 µM. ARN3236 inhibits growth of 10 ovarian cancer cell lines (IC50s = 0.8-2.6 µM) and increases the sensitivity of eight of them to paclitaxel (Item No. 10461).{54419} It halts the cell cycle at the G2/M phase and induces apoptosis and tetraploidy in SKOV3 cells when used at a concentration of 1 µM. ARN3236 (60 mg/kg per day) has an additive effect on reducing tumor growth when used in combination with paclitaxel in an ovarian cancer mouse xenograft model.  

     

    Brand:
    Cayman
    SKU:31457 - 10 mg

    Available on backorder

  • ARN3236 is an inhibitor of salt-inducible kinase 2 (SIK2; IC50 = 50s = 21.63 and 6.63 nM, respectively). It inhibits TNF-α secretion in RAW 264.7 cells (IC50 = ~2.5 µM) and reduces phosphorylation of the SIK2 targets CRTC3 and HDAC4 in macrophages when used at a concentration of 3 µM. ARN3236 inhibits growth of 10 ovarian cancer cell lines (IC50s = 0.8-2.6 µM) and increases the sensitivity of eight of them to paclitaxel (Item No. 10461).{54419} It halts the cell cycle at the G2/M phase and induces apoptosis and tetraploidy in SKOV3 cells when used at a concentration of 1 µM. ARN3236 (60 mg/kg per day) has an additive effect on reducing tumor growth when used in combination with paclitaxel in an ovarian cancer mouse xenograft model.  

     

    Brand:
    Cayman
    SKU:31457 - 25 mg

    Available on backorder

  • ARN3236 is an inhibitor of salt-inducible kinase 2 (SIK2; IC50 = 50s = 21.63 and 6.63 nM, respectively). It inhibits TNF-α secretion in RAW 264.7 cells (IC50 = ~2.5 µM) and reduces phosphorylation of the SIK2 targets CRTC3 and HDAC4 in macrophages when used at a concentration of 3 µM. ARN3236 inhibits growth of 10 ovarian cancer cell lines (IC50s = 0.8-2.6 µM) and increases the sensitivity of eight of them to paclitaxel (Item No. 10461).{54419} It halts the cell cycle at the G2/M phase and induces apoptosis and tetraploidy in SKOV3 cells when used at a concentration of 1 µM. ARN3236 (60 mg/kg per day) has an additive effect on reducing tumor growth when used in combination with paclitaxel in an ovarian cancer mouse xenograft model.  

     

    Brand:
    Cayman
    SKU:31457 - 5 mg

    Available on backorder

  • ARN726 is an inhibitor of N-acylethanolamine acid amidase (NAAA; IC50s = 27 and 63 nM for the human and rat enzyme, respectively).{50197} It is selective for NAAA over fatty acid amide hydrolase (FAAH) and acid ceramidase (IC50s = >100 and 12.5 μM, respectively), as well as a panel of 28 lipid metabolism- and inflammation-related enzymes at 10 μM. ARN726 (1-30 mg/kg) decreases lung myeloperoxidase activity and pleural exudate TNF-α levels in a mouse model of carrageenan-induced lung inflammation. It inhibits NAAA and reverses complete Freund’s adjuvant-induced decreases in palmitoyl ethanolamide (PEA; Item No. 90350) and oleoyl ethanolamide (OEA; Item No. 90265) levels in inflamed paw tissue in a rat model of arthritis.{36896}  

     

    Brand:
    Cayman
    SKU:24259 - 1 mg

    Available on backorder

  • ARN726 is an inhibitor of N-acylethanolamine acid amidase (NAAA; IC50s = 27 and 63 nM for the human and rat enzyme, respectively).{50197} It is selective for NAAA over fatty acid amide hydrolase (FAAH) and acid ceramidase (IC50s = >100 and 12.5 μM, respectively), as well as a panel of 28 lipid metabolism- and inflammation-related enzymes at 10 μM. ARN726 (1-30 mg/kg) decreases lung myeloperoxidase activity and pleural exudate TNF-α levels in a mouse model of carrageenan-induced lung inflammation. It inhibits NAAA and reverses complete Freund’s adjuvant-induced decreases in palmitoyl ethanolamide (PEA; Item No. 90350) and oleoyl ethanolamide (OEA; Item No. 90265) levels in inflamed paw tissue in a rat model of arthritis.{36896}  

     

    Brand:
    Cayman
    SKU:24259 - 10 mg

    Available on backorder

  • ARN726 is an inhibitor of N-acylethanolamine acid amidase (NAAA; IC50s = 27 and 63 nM for the human and rat enzyme, respectively).{50197} It is selective for NAAA over fatty acid amide hydrolase (FAAH) and acid ceramidase (IC50s = >100 and 12.5 μM, respectively), as well as a panel of 28 lipid metabolism- and inflammation-related enzymes at 10 μM. ARN726 (1-30 mg/kg) decreases lung myeloperoxidase activity and pleural exudate TNF-α levels in a mouse model of carrageenan-induced lung inflammation. It inhibits NAAA and reverses complete Freund’s adjuvant-induced decreases in palmitoyl ethanolamide (PEA; Item No. 90350) and oleoyl ethanolamide (OEA; Item No. 90265) levels in inflamed paw tissue in a rat model of arthritis.{36896}  

     

    Brand:
    Cayman
    SKU:24259 - 25 mg

    Available on backorder

  • ARN726 is an inhibitor of N-acylethanolamine acid amidase (NAAA; IC50s = 27 and 63 nM for the human and rat enzyme, respectively).{50197} It is selective for NAAA over fatty acid amide hydrolase (FAAH) and acid ceramidase (IC50s = >100 and 12.5 μM, respectively), as well as a panel of 28 lipid metabolism- and inflammation-related enzymes at 10 μM. ARN726 (1-30 mg/kg) decreases lung myeloperoxidase activity and pleural exudate TNF-α levels in a mouse model of carrageenan-induced lung inflammation. It inhibits NAAA and reverses complete Freund’s adjuvant-induced decreases in palmitoyl ethanolamide (PEA; Item No. 90350) and oleoyl ethanolamide (OEA; Item No. 90265) levels in inflamed paw tissue in a rat model of arthritis.{36896}  

     

    Brand:
    Cayman
    SKU:24259 - 5 mg

    Available on backorder

  • ARN810 is a selective estrogen receptor degrader (SERD) that binds to ERα and ERβ (IC50s = 6.1 and 8.8 nM, respectively) and induces degradation of ERα in MCF-7 cells (EC50 = 0.7 nM).{53182} It inhibits ERα transcriptional activity induced by 17β-estradiol (Item No. 10006315) in a reporter assay and reduces MCF-7 breast cancer cell viability (IC50 = 2 nM). ARN810 (1 mg/kg, p.o.) inhibits 17β-estradiol-induced uterine weight gain in rats. It reduces tumor volume in tamoxifen-sensitive and -resistant MCF-7 mouse xenograft models in a dose-dependent manner.  

     

    Brand:
    Cayman
    SKU:29595 - 1 mg

    Available on backorder

  • ARN810 is a selective estrogen receptor degrader (SERD) that binds to ERα and ERβ (IC50s = 6.1 and 8.8 nM, respectively) and induces degradation of ERα in MCF-7 cells (EC50 = 0.7 nM).{53182} It inhibits ERα transcriptional activity induced by 17β-estradiol (Item No. 10006315) in a reporter assay and reduces MCF-7 breast cancer cell viability (IC50 = 2 nM). ARN810 (1 mg/kg, p.o.) inhibits 17β-estradiol-induced uterine weight gain in rats. It reduces tumor volume in tamoxifen-sensitive and -resistant MCF-7 mouse xenograft models in a dose-dependent manner.  

     

    Brand:
    Cayman
    SKU:29595 - 10 mg

    Available on backorder

  • ARN810 is a selective estrogen receptor degrader (SERD) that binds to ERα and ERβ (IC50s = 6.1 and 8.8 nM, respectively) and induces degradation of ERα in MCF-7 cells (EC50 = 0.7 nM).{53182} It inhibits ERα transcriptional activity induced by 17β-estradiol (Item No. 10006315) in a reporter assay and reduces MCF-7 breast cancer cell viability (IC50 = 2 nM). ARN810 (1 mg/kg, p.o.) inhibits 17β-estradiol-induced uterine weight gain in rats. It reduces tumor volume in tamoxifen-sensitive and -resistant MCF-7 mouse xenograft models in a dose-dependent manner.  

     

    Brand:
    Cayman
    SKU:29595 - 25 mg

    Available on backorder

  • ARN810 is a selective estrogen receptor degrader (SERD) that binds to ERα and ERβ (IC50s = 6.1 and 8.8 nM, respectively) and induces degradation of ERα in MCF-7 cells (EC50 = 0.7 nM).{53182} It inhibits ERα transcriptional activity induced by 17β-estradiol (Item No. 10006315) in a reporter assay and reduces MCF-7 breast cancer cell viability (IC50 = 2 nM). ARN810 (1 mg/kg, p.o.) inhibits 17β-estradiol-induced uterine weight gain in rats. It reduces tumor volume in tamoxifen-sensitive and -resistant MCF-7 mouse xenograft models in a dose-dependent manner.  

     

    Brand:
    Cayman
    SKU:29595 - 5 mg

    Available on backorder

  • Matrix metalloproteinases (MMPs) belong to a family of proteases that play a crucial role in tissue remodeling and repair by degrading extracellular matrix proteins to enable cell migration.{16569} During cancer progression both MMP-2 and MMP-9 play a role in metastatic tumor dispersion and angiogenesis. ARP 100 is a biphenylsulfonamide that acts as a selective inhibitor of MMP-2 demonstrating an IC50 value of 12 nM.{17394,17393} Due to its specific zinc binding domain configuration, the inhibitory activity of ARP 100 is significantly less potent towards MMP-1, MMP-3, MMP-7, and MMP-9 (IC50 values are 50, 4.5, 50, and 2 µM, respectively).{17394,17393} At 50 nM, ARP 100 suppresses the invasive behavior of HT1080 tumor cells grown on matrigel.{17394}  

     

    Brand:
    Cayman
    SKU:-
  • Matrix metalloproteinases (MMPs) belong to a family of proteases that play a crucial role in tissue remodeling and repair by degrading extracellular matrix proteins to enable cell migration.{16569} During cancer progression both MMP-2 and MMP-9 play a role in metastatic tumor dispersion and angiogenesis. ARP 100 is a biphenylsulfonamide that acts as a selective inhibitor of MMP-2 demonstrating an IC50 value of 12 nM.{17394,17393} Due to its specific zinc binding domain configuration, the inhibitory activity of ARP 100 is significantly less potent towards MMP-1, MMP-3, MMP-7, and MMP-9 (IC50 values are 50, 4.5, 50, and 2 µM, respectively).{17394,17393} At 50 nM, ARP 100 suppresses the invasive behavior of HT1080 tumor cells grown on matrigel.{17394}  

     

    Brand:
    Cayman
    SKU:-
  • Matrix metalloproteinases (MMPs) belong to a family of proteases that play a crucial role in tissue remodeling and repair by degrading extracellular matrix proteins to enable cell migration.{16569} During cancer progression both MMP-2 and MMP-9 play a role in metastatic tumor dispersion and angiogenesis. ARP 100 is a biphenylsulfonamide that acts as a selective inhibitor of MMP-2 demonstrating an IC50 value of 12 nM.{17394,17393} Due to its specific zinc binding domain configuration, the inhibitory activity of ARP 100 is significantly less potent towards MMP-1, MMP-3, MMP-7, and MMP-9 (IC50 values are 50, 4.5, 50, and 2 µM, respectively).{17394,17393} At 50 nM, ARP 100 suppresses the invasive behavior of HT1080 tumor cells grown on matrigel.{17394}  

     

    Brand:
    Cayman
    SKU:-
  • Aminopeptidase B is a Zn2+-dependent exopeptidase that selectively removes arginine and/or lysine from the amino terminus of peptide substrates.{29942} This enzyme is a metalloprotease commonly found on the surface of mammalian cells, including macrophages and lymphocytes. Arphamenine B is an aminopeptidase B inhibitor first isolated from bacteria.{29946,29945} Like the aminopeptidase inhibitors bestatin (Item No. 70520) and amastatin (Item No. 16719), arphamenine B enhances immune responses.{29946} Arphamenine B is commonly used to characterize novel proteases.{29943,29944}  

     

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    Cayman
    SKU:-

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  • Aminopeptidase B is a Zn2+-dependent exopeptidase that selectively removes arginine and/or lysine from the amino terminus of peptide substrates.{29942} This enzyme is a metalloprotease commonly found on the surface of mammalian cells, including macrophages and lymphocytes. Arphamenine B is an aminopeptidase B inhibitor first isolated from bacteria.{29946,29945} Like the aminopeptidase inhibitors bestatin (Item No. 70520) and amastatin (Item No. 16719), arphamenine B enhances immune responses.{29946} Arphamenine B is commonly used to characterize novel proteases.{29943,29944}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • Aminopeptidase B is a Zn2+-dependent exopeptidase that selectively removes arginine and/or lysine from the amino terminus of peptide substrates.{29942} This enzyme is a metalloprotease commonly found on the surface of mammalian cells, including macrophages and lymphocytes. Arphamenine B is an aminopeptidase B inhibitor first isolated from bacteria.{29946,29945} Like the aminopeptidase inhibitors bestatin (Item No. 70520) and amastatin (Item No. 16719), arphamenine B enhances immune responses.{29946} Arphamenine B is commonly used to characterize novel proteases.{29943,29944}  

     

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    Cayman
    SKU:-

    Available on backorder

  • ARQ-092 is an allosteric, orally bioavailable, pan-Akt inhibitor (IC50s = 5.0, 4.5, and 16 nM for Akt1, Akt2, and Akt3, respectively).{33792} It is selective for Akt isoforms over a panel of 303 other kinases.{33792} ARQ-092 binds inactive Akt and prevents membrane localization and full Akt activation.{33792,33790} It also directly inhibits the membrane-associated active form of Akt, preventing phosphorylation of downstream targets.{33792,33790} ARQ-092 inhibits the proliferation of a wide range of cancer cells in vitro, inhibits the mutated Akt form found in Proteus syndrome, and attenuates heterotypic cell-cell interactions in a mouse model of sickle cell disease.{33792,33790,32947,33791}  

     

    Brand:
    Cayman
    SKU:21388 -

    Out of stock

  • ARQ-092 is an allosteric, orally bioavailable, pan-Akt inhibitor (IC50s = 5.0, 4.5, and 16 nM for Akt1, Akt2, and Akt3, respectively).{33792} It is selective for Akt isoforms over a panel of 303 other kinases.{33792} ARQ-092 binds inactive Akt and prevents membrane localization and full Akt activation.{33792,33790} It also directly inhibits the membrane-associated active form of Akt, preventing phosphorylation of downstream targets.{33792,33790} ARQ-092 inhibits the proliferation of a wide range of cancer cells in vitro, inhibits the mutated Akt form found in Proteus syndrome, and attenuates heterotypic cell-cell interactions in a mouse model of sickle cell disease.{33792,33790,32947,33791}  

     

    Brand:
    Cayman
    SKU:21388 -

    Out of stock

  • ARQ-092 is an allosteric, orally bioavailable, pan-Akt inhibitor (IC50s = 5.0, 4.5, and 16 nM for Akt1, Akt2, and Akt3, respectively).{33792} It is selective for Akt isoforms over a panel of 303 other kinases.{33792} ARQ-092 binds inactive Akt and prevents membrane localization and full Akt activation.{33792,33790} It also directly inhibits the membrane-associated active form of Akt, preventing phosphorylation of downstream targets.{33792,33790} ARQ-092 inhibits the proliferation of a wide range of cancer cells in vitro, inhibits the mutated Akt form found in Proteus syndrome, and attenuates heterotypic cell-cell interactions in a mouse model of sickle cell disease.{33792,33790,32947,33791}  

     

    Brand:
    Cayman
    SKU:21388 -

    Out of stock

  • ARQ-092 is an allosteric, orally bioavailable, pan-Akt inhibitor (IC50s = 5.0, 4.5, and 16 nM for Akt1, Akt2, and Akt3, respectively).{33792} It is selective for Akt isoforms over a panel of 303 other kinases.{33792} ARQ-092 binds inactive Akt and prevents membrane localization and full Akt activation.{33792,33790} It also directly inhibits the membrane-associated active form of Akt, preventing phosphorylation of downstream targets.{33792,33790} ARQ-092 inhibits the proliferation of a wide range of cancer cells in vitro, inhibits the mutated Akt form found in Proteus syndrome, and attenuates heterotypic cell-cell interactions in a mouse model of sickle cell disease.{33792,33790,32947,33791}  

     

    Brand:
    Cayman
    SKU:21388 -

    Out of stock

  • Arry-380 analog was designed as an inhibitor of EGFR (ErbB1).{40812}  

     

    Brand:
    Cayman
    SKU:24186 - 1 mg

    Available on backorder

  • Arry-380 analog was designed as an inhibitor of EGFR (ErbB1).{40812}  

     

    Brand:
    Cayman
    SKU:24186 - 10 mg

    Available on backorder

  • Arry-380 analog was designed as an inhibitor of EGFR (ErbB1).{40812}  

     

    Brand:
    Cayman
    SKU:24186 - 25 mg

    Available on backorder

  • Arry-380 analog was designed as an inhibitor of EGFR (ErbB1).{40812}  

     

    Brand:
    Cayman
    SKU:24186 - 5 mg

    Available on backorder

  • ARRY-520 is a potent inhibitor of the kinesin spindle protein Eg5 (IC50 = 6 nM).{42111} It is selective for Eg5 over a panel of 8 kinesins (IC50s = >100 μM) and a panel of 224 kinases at a concentration of 10 μM. ARRY-520 induces time-and dose-dependent cell death in HL-60, Jurkat, OCI-AML3, U937, and MOLM-13 leukemic cells.{42112} Downregulation of Eg5 expression sensitizes HL-60 cells to ARRY-520 (IC50s = 11.3 and 2 nM for wild-type and Eg5 knockdown HL-60 cells, respectively). ARRY-520 induces cell cycle arrest at the G2/M phase in a p53- and XIAP-independent manner in OCI-AML3 cells. It also inhibits blast colony formation of bone marrow samples derived from human acute myeloid leukemia (AML) patients. In vivo, ARRY-520 (20 mg/kg per day) completely eliminates tumors in the RPMI-8226 multiple myeloma and HL-60 and MV4-11 AML mouse xenograft models.{42111}  

     

    Brand:
    Cayman
    SKU:21883 -

    Out of stock

  • ARRY-520 is a potent inhibitor of the kinesin spindle protein Eg5 (IC50 = 6 nM).{42111} It is selective for Eg5 over a panel of 8 kinesins (IC50s = >100 μM) and a panel of 224 kinases at a concentration of 10 μM. ARRY-520 induces time-and dose-dependent cell death in HL-60, Jurkat, OCI-AML3, U937, and MOLM-13 leukemic cells.{42112} Downregulation of Eg5 expression sensitizes HL-60 cells to ARRY-520 (IC50s = 11.3 and 2 nM for wild-type and Eg5 knockdown HL-60 cells, respectively). ARRY-520 induces cell cycle arrest at the G2/M phase in a p53- and XIAP-independent manner in OCI-AML3 cells. It also inhibits blast colony formation of bone marrow samples derived from human acute myeloid leukemia (AML) patients. In vivo, ARRY-520 (20 mg/kg per day) completely eliminates tumors in the RPMI-8226 multiple myeloma and HL-60 and MV4-11 AML mouse xenograft models.{42111}  

     

    Brand:
    Cayman
    SKU:21883 -

    Out of stock

  • ARRY-520 is a potent inhibitor of the kinesin spindle protein Eg5 (IC50 = 6 nM).{42111} It is selective for Eg5 over a panel of 8 kinesins (IC50s = >100 μM) and a panel of 224 kinases at a concentration of 10 μM. ARRY-520 induces time-and dose-dependent cell death in HL-60, Jurkat, OCI-AML3, U937, and MOLM-13 leukemic cells.{42112} Downregulation of Eg5 expression sensitizes HL-60 cells to ARRY-520 (IC50s = 11.3 and 2 nM for wild-type and Eg5 knockdown HL-60 cells, respectively). ARRY-520 induces cell cycle arrest at the G2/M phase in a p53- and XIAP-independent manner in OCI-AML3 cells. It also inhibits blast colony formation of bone marrow samples derived from human acute myeloid leukemia (AML) patients. In vivo, ARRY-520 (20 mg/kg per day) completely eliminates tumors in the RPMI-8226 multiple myeloma and HL-60 and MV4-11 AML mouse xenograft models.{42111}  

     

    Brand:
    Cayman
    SKU:21883 -

    Out of stock

  • ARRY-520 is a potent inhibitor of the kinesin spindle protein Eg5 (IC50 = 6 nM).{42111} It is selective for Eg5 over a panel of 8 kinesins (IC50s = >100 μM) and a panel of 224 kinases at a concentration of 10 μM. ARRY-520 induces time-and dose-dependent cell death in HL-60, Jurkat, OCI-AML3, U937, and MOLM-13 leukemic cells.{42112} Downregulation of Eg5 expression sensitizes HL-60 cells to ARRY-520 (IC50s = 11.3 and 2 nM for wild-type and Eg5 knockdown HL-60 cells, respectively). ARRY-520 induces cell cycle arrest at the G2/M phase in a p53- and XIAP-independent manner in OCI-AML3 cells. It also inhibits blast colony formation of bone marrow samples derived from human acute myeloid leukemia (AML) patients. In vivo, ARRY-520 (20 mg/kg per day) completely eliminates tumors in the RPMI-8226 multiple myeloma and HL-60 and MV4-11 AML mouse xenograft models.{42111}  

     

    Brand:
    Cayman
    SKU:21883 -

    Out of stock

  • ARS1620 is a covalent inhibitor of K-RASG12C (IC50 = G12C (IC50s = 150 nM) over H441, A549, and HCT116 cells expressing wild-type K-RAS (IC50s = >10 μM). ARS1620 (200 mg/kg) induces tumor regression in a MIA-PaCa2, but not an H441, mouse xenograft model. It also decreases tumor volume in patient-derived xenograft (PDX) mouse models expressing K-RASG12C, but not K-RASG12D or wild-type K-RAS.  

     

    Brand:
    Cayman
    SKU:27915 - 1 mg

    Available on backorder

  • ARS1620 is a covalent inhibitor of K-RASG12C (IC50 = G12C (IC50s = 150 nM) over H441, A549, and HCT116 cells expressing wild-type K-RAS (IC50s = >10 μM). ARS1620 (200 mg/kg) induces tumor regression in a MIA-PaCa2, but not an H441, mouse xenograft model. It also decreases tumor volume in patient-derived xenograft (PDX) mouse models expressing K-RASG12C, but not K-RASG12D or wild-type K-RAS.  

     

    Brand:
    Cayman
    SKU:27915 - 5 mg

    Available on backorder

  • ARS853 is an inhibitor of K-RASG12C, a mutant form of K-RAS that accumulates in the active GTP-bound state in certain cancer cells.{30527} ARS853 binds to the inactive GDP-bound state of K-RASG12C. It decreases the level of active GTP-bound K-RAS by 95% when used at a concentration of 10 µM in K-RASG12C mutant lung cancer cells. It also decreases phosphorylation of c-RAF, ERK, and Akt. ARS853 inhibits proliferation of six lung cancer cell lines containing the K-RASG12C mutation, including H358 cells (IC50 = 2.5 µM), but does not inhibit proliferation of PC-9 cells, which contain wild-type K-RAS.  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • ARS853 is an inhibitor of K-RASG12C, a mutant form of K-RAS that accumulates in the active GTP-bound state in certain cancer cells.{30527} ARS853 binds to the inactive GDP-bound state of K-RASG12C. It decreases the level of active GTP-bound K-RAS by 95% when used at a concentration of 10 µM in K-RASG12C mutant lung cancer cells. It also decreases phosphorylation of c-RAF, ERK, and Akt. ARS853 inhibits proliferation of six lung cancer cell lines containing the K-RASG12C mutation, including H358 cells (IC50 = 2.5 µM), but does not inhibit proliferation of PC-9 cells, which contain wild-type K-RAS.  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • ARS853 is an inhibitor of K-RASG12C, a mutant form of K-RAS that accumulates in the active GTP-bound state in certain cancer cells.{30527} ARS853 binds to the inactive GDP-bound state of K-RASG12C. It decreases the level of active GTP-bound K-RAS by 95% when used at a concentration of 10 µM in K-RASG12C mutant lung cancer cells. It also decreases phosphorylation of c-RAF, ERK, and Akt. ARS853 inhibits proliferation of six lung cancer cell lines containing the K-RASG12C mutation, including H358 cells (IC50 = 2.5 µM), but does not inhibit proliferation of PC-9 cells, which contain wild-type K-RAS.  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • ARS853 is an inhibitor of K-RASG12C, a mutant form of K-RAS that accumulates in the active GTP-bound state in certain cancer cells.{30527} ARS853 binds to the inactive GDP-bound state of K-RASG12C. It decreases the level of active GTP-bound K-RAS by 95% when used at a concentration of 10 µM in K-RASG12C mutant lung cancer cells. It also decreases phosphorylation of c-RAF, ERK, and Akt. ARS853 inhibits proliferation of six lung cancer cell lines containing the K-RASG12C mutation, including H358 cells (IC50 = 2.5 µM), but does not inhibit proliferation of PC-9 cells, which contain wild-type K-RAS.  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • Arteether is a derivative of the antimalarial drug artemisinin (Item No. 11816). Arteether inhibits P. falciparum with an IC50 value of 1.27 nM in vitro.{39374} It is effective against various strains of P. berghei in mice with ED90 values of 0.5-8.2 nM.  

     

    Brand:
    Cayman
    SKU:11814 - 10 mg

    Available on backorder

  • Arteether is a derivative of the antimalarial drug artemisinin (Item No. 11816). Arteether inhibits P. falciparum with an IC50 value of 1.27 nM in vitro.{39374} It is effective against various strains of P. berghei in mice with ED90 values of 0.5-8.2 nM.  

     

    Brand:
    Cayman
    SKU:11814 - 25 mg

    Available on backorder

  • Arteether is a derivative of the antimalarial drug artemisinin (Item No. 11816). Arteether inhibits P. falciparum with an IC50 value of 1.27 nM in vitro.{39374} It is effective against various strains of P. berghei in mice with ED90 values of 0.5-8.2 nM.  

     

    Brand:
    Cayman
    SKU:11814 - 5 mg

    Available on backorder

  • Arteether is a derivative of the antimalarial drug artemisinin (Item No. 11816). Arteether inhibits P. falciparum with an IC50 value of 1.27 nM in vitro.{39374} It is effective against various strains of P. berghei in mice with ED90 values of 0.5-8.2 nM.  

     

    Brand:
    Cayman
    SKU:11814 - 50 mg

    Available on backorder

  • Artefenomel is an ozonide antimalarial agent.{52714} It is active against 3D7, Cam3.II, and Cam3.II_rev P. falciparum strains (LC50s = 8.7, 4.4, and 6.1 nM, respectively). Artefenomel reduces the number of trophozoites in P. falciparum-infected isolated human red blood cells (IC50 = 31 nM).{52715} In vivo, artefenomel (30 mg/kg) is 100% curative in a mouse model of P. berghei infection.{52716}  

     

    Brand:
    Cayman
    SKU:30677 - 1 mg

    Available on backorder

  • Artefenomel is an ozonide antimalarial agent.{52714} It is active against 3D7, Cam3.II, and Cam3.II_rev P. falciparum strains (LC50s = 8.7, 4.4, and 6.1 nM, respectively). Artefenomel reduces the number of trophozoites in P. falciparum-infected isolated human red blood cells (IC50 = 31 nM).{52715} In vivo, artefenomel (30 mg/kg) is 100% curative in a mouse model of P. berghei infection.{52716}  

     

    Brand:
    Cayman
    SKU:30677 - 5 mg

    Available on backorder

  • Artemether is an antiparasitic compound and a derivative of artemisinin (Item No. 11816).{48487} It induces mortality in adult wild-type and pfatp6-mutant P. falciparum but the efficacy is decreased in the mutants (IC50s = 8.2 and 13.5 nM, respectively).{48485} Artemether reduces parasitemia in P. falciparum-infected monkeys and P. berghei-infected mice with 50% curative dose (CD50) values of 7.1 and 55 mg/kg, respectively.{48486} It also reduces the worm burden of S. mansoni trematodes in mice when used at doses ranging from 200 to 500 mg/kg.{48487} Formulations containing artemether have been used in the treatment of malaria.  

     

    Brand:
    Cayman
    SKU:11815 - 1 g

    Available on backorder

  • Artemether is an antiparasitic compound and a derivative of artemisinin (Item No. 11816).{48487} It induces mortality in adult wild-type and pfatp6-mutant P. falciparum but the efficacy is decreased in the mutants (IC50s = 8.2 and 13.5 nM, respectively).{48485} Artemether reduces parasitemia in P. falciparum-infected monkeys and P. berghei-infected mice with 50% curative dose (CD50) values of 7.1 and 55 mg/kg, respectively.{48486} It also reduces the worm burden of S. mansoni trematodes in mice when used at doses ranging from 200 to 500 mg/kg.{48487} Formulations containing artemether have been used in the treatment of malaria.  

     

    Brand:
    Cayman
    SKU:11815 - 500 mg

    Available on backorder

  • Artemether-d3 is intended for use as an internal standard for the quantification of artemether (Item No. 11815) by GC- or LC-MS. Artemether is an antiparasitic agent and a derivative of artemisinin (Item No. 11816).{48487} It induces mortality in adult wild-type and pfatp6-mutant P. falciparum but the efficacy is decreased in the mutants (IC50s = 8.2 and 13.5 nM, respectively).{48485} Artemether reduces parasitemia in P. falciparum-infected monkeys and P. berghei-infected mice with 50% curative dose (CD50) values of 7.1 and 55 mg/kg, respectively.{48486} It also reduces the worm burden of S. mansoni trematodes in mice when used at doses ranging from 200 to 500 mg/kg.{48487} Formulations containing artemether have been used in the treatment of malaria.  

     

    Brand:
    Cayman
    SKU:28517 - 1 mg

    Available on backorder

  • Artemether-d3 is intended for use as an internal standard for the quantification of artemether (Item No. 11815) by GC- or LC-MS. Artemether is an antiparasitic agent and a derivative of artemisinin (Item No. 11816).{48487} It induces mortality in adult wild-type and pfatp6-mutant P. falciparum but the efficacy is decreased in the mutants (IC50s = 8.2 and 13.5 nM, respectively).{48485} Artemether reduces parasitemia in P. falciparum-infected monkeys and P. berghei-infected mice with 50% curative dose (CD50) values of 7.1 and 55 mg/kg, respectively.{48486} It also reduces the worm burden of S. mansoni trematodes in mice when used at doses ranging from 200 to 500 mg/kg.{48487} Formulations containing artemether have been used in the treatment of malaria.  

     

    Brand:
    Cayman
    SKU:28517 - 10 mg

    Available on backorder

  • Artemether-d3 is intended for use as an internal standard for the quantification of artemether (Item No. 11815) by GC- or LC-MS. Artemether is an antiparasitic agent and a derivative of artemisinin (Item No. 11816).{48487} It induces mortality in adult wild-type and pfatp6-mutant P. falciparum but the efficacy is decreased in the mutants (IC50s = 8.2 and 13.5 nM, respectively).{48485} Artemether reduces parasitemia in P. falciparum-infected monkeys and P. berghei-infected mice with 50% curative dose (CD50) values of 7.1 and 55 mg/kg, respectively.{48486} It also reduces the worm burden of S. mansoni trematodes in mice when used at doses ranging from 200 to 500 mg/kg.{48487} Formulations containing artemether have been used in the treatment of malaria.  

     

    Brand:
    Cayman
    SKU:28517 - 5 mg

    Available on backorder

  • Artemisinic acid is a sesquiterpene that has been isolated from A. annua.{41903} It has been used in the synthesis of the antimalarial agent artemisinin (Item No. 11816).{41904} Artemisinic acid (50-400 µM) decreases triglyceride levels and glycerol-3-phosphate dehydrogenase (GPDH) activity in human adipose tissue-derived mesenchymal stem cells (hAMSCs) in a dose-dependent manner and inhibits adipocyte differentiation when used at a concentration of 200 µM.{41905} It reduces mRNA expression and protein levels of C/EBPα, C/EBPδ, and PPARγ as well as the ratio of phosphorylated JNK to JNK in hAMSCs. Artemisinic acid also decreases C/EBPα and HMG-CoA reductase mRNA expression and inhibits cholesterol synthesis and melanogenesis in human epidermal melanocytes.{41906}  

     

    Brand:
    Cayman
    SKU:25059 - 10 mg

    Available on backorder

  • Artemisinic acid is a sesquiterpene that has been isolated from A. annua.{41903} It has been used in the synthesis of the antimalarial agent artemisinin (Item No. 11816).{41904} Artemisinic acid (50-400 µM) decreases triglyceride levels and glycerol-3-phosphate dehydrogenase (GPDH) activity in human adipose tissue-derived mesenchymal stem cells (hAMSCs) in a dose-dependent manner and inhibits adipocyte differentiation when used at a concentration of 200 µM.{41905} It reduces mRNA expression and protein levels of C/EBPα, C/EBPδ, and PPARγ as well as the ratio of phosphorylated JNK to JNK in hAMSCs. Artemisinic acid also decreases C/EBPα and HMG-CoA reductase mRNA expression and inhibits cholesterol synthesis and melanogenesis in human epidermal melanocytes.{41906}  

     

    Brand:
    Cayman
    SKU:25059 - 100 mg

    Available on backorder

  • Artemisinic acid is a sesquiterpene that has been isolated from A. annua.{41903} It has been used in the synthesis of the antimalarial agent artemisinin (Item No. 11816).{41904} Artemisinic acid (50-400 µM) decreases triglyceride levels and glycerol-3-phosphate dehydrogenase (GPDH) activity in human adipose tissue-derived mesenchymal stem cells (hAMSCs) in a dose-dependent manner and inhibits adipocyte differentiation when used at a concentration of 200 µM.{41905} It reduces mRNA expression and protein levels of C/EBPα, C/EBPδ, and PPARγ as well as the ratio of phosphorylated JNK to JNK in hAMSCs. Artemisinic acid also decreases C/EBPα and HMG-CoA reductase mRNA expression and inhibits cholesterol synthesis and melanogenesis in human epidermal melanocytes.{41906}  

     

    Brand:
    Cayman
    SKU:25059 - 25 mg

    Available on backorder

  • Artemisinic acid is a sesquiterpene that has been isolated from A. annua.{41903} It has been used in the synthesis of the antimalarial agent artemisinin (Item No. 11816).{41904} Artemisinic acid (50-400 µM) decreases triglyceride levels and glycerol-3-phosphate dehydrogenase (GPDH) activity in human adipose tissue-derived mesenchymal stem cells (hAMSCs) in a dose-dependent manner and inhibits adipocyte differentiation when used at a concentration of 200 µM.{41905} It reduces mRNA expression and protein levels of C/EBPα, C/EBPδ, and PPARγ as well as the ratio of phosphorylated JNK to JNK in hAMSCs. Artemisinic acid also decreases C/EBPα and HMG-CoA reductase mRNA expression and inhibits cholesterol synthesis and melanogenesis in human epidermal melanocytes.{41906}  

     

    Brand:
    Cayman
    SKU:25059 - 50 mg

    Available on backorder

  • Artemisinin is an antimalarial agent with anticancer activity.{21232,37702} It is an iron(II) oxide-reactive endoperoxide that generates reactive oxygen species (ROS) upon cleavage of its endoperoxide bridge.{35319} It reduces the growth of various P. falciparum strains in vitro (IC50s = 3.98-20.36 nM) and reduces parasitemia in mice infected with P. falciparum with a curative dose (CD50) value of 140 mg/kg.{21232,37703} It also reduces P. berghei infection in mice (ED50 = 5.6 mg/kg per day).{37704} Artemisinin (100-400 μM) induces cell cycle arrest in the G0/G1 phase and apoptosis and inhibits growth of SK-N-AS, BE(2)-C, SK-N-DZ, and SHEP1 neuroblastoma cells in a time- and concentration-dependent manner.{37702} It also suppresses BE(2)-C cell colony formation in a soft agar assay and reduces tumor growth in a BE(2)-C mouse xenograft model. Formulations containing artemisinin have been used in combination therapies for the treatment of malaria.  

     

    Brand:
    Cayman
    SKU:11816 - 1 g

    Available on backorder

  • Artemisinin is an antimalarial agent with anticancer activity.{21232,37702} It is an iron(II) oxide-reactive endoperoxide that generates reactive oxygen species (ROS) upon cleavage of its endoperoxide bridge.{35319} It reduces the growth of various P. falciparum strains in vitro (IC50s = 3.98-20.36 nM) and reduces parasitemia in mice infected with P. falciparum with a curative dose (CD50) value of 140 mg/kg.{21232,37703} It also reduces P. berghei infection in mice (ED50 = 5.6 mg/kg per day).{37704} Artemisinin (100-400 μM) induces cell cycle arrest in the G0/G1 phase and apoptosis and inhibits growth of SK-N-AS, BE(2)-C, SK-N-DZ, and SHEP1 neuroblastoma cells in a time- and concentration-dependent manner.{37702} It also suppresses BE(2)-C cell colony formation in a soft agar assay and reduces tumor growth in a BE(2)-C mouse xenograft model. Formulations containing artemisinin have been used in combination therapies for the treatment of malaria.  

     

    Brand:
    Cayman
    SKU:11816 - 100 mg

    Available on backorder

  • Artemisinin is an antimalarial agent with anticancer activity.{21232,37702} It is an iron(II) oxide-reactive endoperoxide that generates reactive oxygen species (ROS) upon cleavage of its endoperoxide bridge.{35319} It reduces the growth of various P. falciparum strains in vitro (IC50s = 3.98-20.36 nM) and reduces parasitemia in mice infected with P. falciparum with a curative dose (CD50) value of 140 mg/kg.{21232,37703} It also reduces P. berghei infection in mice (ED50 = 5.6 mg/kg per day).{37704} Artemisinin (100-400 μM) induces cell cycle arrest in the G0/G1 phase and apoptosis and inhibits growth of SK-N-AS, BE(2)-C, SK-N-DZ, and SHEP1 neuroblastoma cells in a time- and concentration-dependent manner.{37702} It also suppresses BE(2)-C cell colony formation in a soft agar assay and reduces tumor growth in a BE(2)-C mouse xenograft model. Formulations containing artemisinin have been used in combination therapies for the treatment of malaria.  

     

    Brand:
    Cayman
    SKU:11816 - 500 mg

    Available on backorder

  • Artemisinin-d3 is intended for use as an internal standard for the quantification of artemisinin (Item No. 11816). Artemisinin is an endoperoxide antimalarial agent with anticancer activity.{21232,37702} It reduces the growth of various P. falciparum strains in vitro (IC50s = 3.98-20.36 nM) and reduces parasitemia in mice infected with P. falciparum with a curative dose (CD50) value of 140 mg/kg.{21232,37703} It also reduces P. berghei infection in mice (ED50 = 5.6 mg/kg per day).{37704} Artemisinin (100-400 μM) induces cell cycle arrest in the G0/G1 phase and apoptosis and inhibits growth of SK-N-AS, BE(2)-C, SK-N-DZ, and SHEP1 neuroblastoma cells in a time- and concentration-dependent manner.{37702} It also suppresses BE(2)-C cell colony formation in a soft agar assay and reduces tumor growth in a BE(2)-C mouse xenograft model. Formulations containing artemisinin have been used in combination therapies for the treatment of malaria.  

     

    Brand:
    Cayman
    SKU:25359 - 1 mg

    Available on backorder

  • Arterolane is an antimalarial agent.{52701} It is active against 10 strains of P. falciparum in vitro, including chloroquine- and pyrimethamine-resistant strains, with IC50 values ranging from 0.43 to 1.6 ng/ml. Arterolane (10 mg/kg per day for three days) is curative in 67% of mice in a model of P. berghei infection.  

     

    Brand:
    Cayman
    SKU:30676 - 1 mg

    Available on backorder

  • Arterolane is an antimalarial agent.{52701} It is active against 10 strains of P. falciparum in vitro, including chloroquine- and pyrimethamine-resistant strains, with IC50 values ranging from 0.43 to 1.6 ng/ml. Arterolane (10 mg/kg per day for three days) is curative in 67% of mice in a model of P. berghei infection.  

     

    Brand:
    Cayman
    SKU:30676 - 5 mg

    Available on backorder

  • Artesunate is a derivative of artemisinin (Item No. 11816) that is active against P. falciparum in vitro (IC50 = 1.28 nM).{21232} It is an iron(II) oxide-reactive endoperoxide that generates reactive oxygen species (ROS) upon cleavage of its endoperoxide bridge.{35319} Artesunate inhibits proliferation of germinal center B cells in vitro and prevents development of arthritis via inhibition of germinal center formation and autoantibody production in the K/BxN mouse model of rheumatoid arthritis.{42468} It also inhibits alveolitis and pulmonary fibrosis induced by bleomycin (Item No. 13877) in rats.{42469}  

     

    Brand:
    Cayman
    SKU:11817 - 1 g

    Available on backorder

  • Artesunate is a derivative of artemisinin (Item No. 11816) that is active against P. falciparum in vitro (IC50 = 1.28 nM).{21232} It is an iron(II) oxide-reactive endoperoxide that generates reactive oxygen species (ROS) upon cleavage of its endoperoxide bridge.{35319} Artesunate inhibits proliferation of germinal center B cells in vitro and prevents development of arthritis via inhibition of germinal center formation and autoantibody production in the K/BxN mouse model of rheumatoid arthritis.{42468} It also inhibits alveolitis and pulmonary fibrosis induced by bleomycin (Item No. 13877) in rats.{42469}  

     

    Brand:
    Cayman
    SKU:11817 - 100 mg

    Available on backorder

  • Artesunate is a derivative of artemisinin (Item No. 11816) that is active against P. falciparum in vitro (IC50 = 1.28 nM).{21232} It is an iron(II) oxide-reactive endoperoxide that generates reactive oxygen species (ROS) upon cleavage of its endoperoxide bridge.{35319} Artesunate inhibits proliferation of germinal center B cells in vitro and prevents development of arthritis via inhibition of germinal center formation and autoantibody production in the K/BxN mouse model of rheumatoid arthritis.{42468} It also inhibits alveolitis and pulmonary fibrosis induced by bleomycin (Item No. 13877) in rats.{42469}  

     

    Brand:
    Cayman
    SKU:11817 - 250 mg

    Available on backorder

  • Artesunate is a derivative of artemisinin (Item No. 11816) that is active against P. falciparum in vitro (IC50 = 1.28 nM).{21232} It is an iron(II) oxide-reactive endoperoxide that generates reactive oxygen species (ROS) upon cleavage of its endoperoxide bridge.{35319} Artesunate inhibits proliferation of germinal center B cells in vitro and prevents development of arthritis via inhibition of germinal center formation and autoantibody production in the K/BxN mouse model of rheumatoid arthritis.{42468} It also inhibits alveolitis and pulmonary fibrosis induced by bleomycin (Item No. 13877) in rats.{42469}  

     

    Brand:
    Cayman
    SKU:11817 - 500 mg

    Available on backorder

  • Artesunate-d4 is intended for use as an internal standard for the quantification of artesunate (Item No. 11817) by GC- or LC-MS. Artesunate is a derivative of artemisinin (Item No. 11816) that is active against P. falciparum in vitro (IC50 = 1.28 nM).{21232} It is an iron(II) oxide-reactive endoperoxide that generates reactive oxygen species (ROS) upon cleavage of its endoperoxide bridge.{35319} Artesunate inhibits proliferation of germinal center B cells in vitro and prevents development of arthritis via inhibition of germinal center formation and autoantibody production in the K/BxN mouse model of rheumatoid arthritis.{42468} It also inhibits alveolitis and pulmonary fibrosis induced by bleomycin (Item No. 13877) in rats.{42469}  

     

    Brand:
    Cayman
    SKU:28769 - 1 mg

    Available on backorder

  • Artesunate-d4 is intended for use as an internal standard for the quantification of artesunate (Item No. 11817) by GC- or LC-MS. Artesunate is a derivative of artemisinin (Item No. 11816) that is active against P. falciparum in vitro (IC50 = 1.28 nM).{21232} It is an iron(II) oxide-reactive endoperoxide that generates reactive oxygen species (ROS) upon cleavage of its endoperoxide bridge.{35319} Artesunate inhibits proliferation of germinal center B cells in vitro and prevents development of arthritis via inhibition of germinal center formation and autoantibody production in the K/BxN mouse model of rheumatoid arthritis.{42468} It also inhibits alveolitis and pulmonary fibrosis induced by bleomycin (Item No. 13877) in rats.{42469}  

     

    Brand:
    Cayman
    SKU:28769 - 500 µg

    Available on backorder

  • Most local anesthetics act by abolishing voltage-gated sodium channel currents indiscriminately in all populations of neurons. Articaine is an amide local anesthetic most commonly used in dentistry.{29049} It possesses a unique ester side chain that is metabolized rapidly by circulating esterases.{29050} Articaine is reported to modify cardiac action potentials and ion currents only at concentrations higher than the therapeutic range needed to inhibit voltage-gated sodium channels.{29050}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • Most local anesthetics act by abolishing voltage-gated sodium channel currents indiscriminately in all populations of neurons. Articaine is an amide local anesthetic most commonly used in dentistry.{29049} It possesses a unique ester side chain that is metabolized rapidly by circulating esterases.{29050} Articaine is reported to modify cardiac action potentials and ion currents only at concentrations higher than the therapeutic range needed to inhibit voltage-gated sodium channels.{29050}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • Most local anesthetics act by abolishing voltage-gated sodium channel currents indiscriminately in all populations of neurons. Articaine is an amide local anesthetic most commonly used in dentistry.{29049} It possesses a unique ester side chain that is metabolized rapidly by circulating esterases.{29050} Articaine is reported to modify cardiac action potentials and ion currents only at concentrations higher than the therapeutic range needed to inhibit voltage-gated sodium channels.{29050}  

     

    Brand:
    Cayman
    SKU:-

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  • Most local anesthetics act by abolishing voltage-gated sodium channel currents indiscriminately in all populations of neurons. Articaine is an amide local anesthetic most commonly used in dentistry.{29049} It possesses a unique ester side chain that is metabolized rapidly by circulating esterases.{29050} Articaine is reported to modify cardiac action potentials and ion currents only at concentrations higher than the therapeutic range needed to inhibit voltage-gated sodium channels.{29050}  

     

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    Cayman
    SKU:-

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  • Arundic acid is an inhibitor of astrocyte activation.{53333} It reduces increases in brain glial fibrillary acid protein (GFAP) and S100β levels, markers of astrocyte activation, in a rat model of permanent focal ischemia induced by middle cerebral artery occlusion when administered at a dose of 10 mg/kg. Arundic acid (3 and 10 mg/kg) decreases the number of TUNEL-positive neurons, reduces infarct size, and improves motor performance in the rotarod test in the same model. It also reduces descent time and time to turn in a pole test, indicating reversal of motor deficits, in a mouse model of MPTP-induced Parkinson’s disease when administered at a dose of 30 mg/kg.{53334}  

     

    Brand:
    Cayman
    SKU:29087 - 1 mg

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  • Arundic acid is an inhibitor of astrocyte activation.{53333} It reduces increases in brain glial fibrillary acid protein (GFAP) and S100β levels, markers of astrocyte activation, in a rat model of permanent focal ischemia induced by middle cerebral artery occlusion when administered at a dose of 10 mg/kg. Arundic acid (3 and 10 mg/kg) decreases the number of TUNEL-positive neurons, reduces infarct size, and improves motor performance in the rotarod test in the same model. It also reduces descent time and time to turn in a pole test, indicating reversal of motor deficits, in a mouse model of MPTP-induced Parkinson’s disease when administered at a dose of 30 mg/kg.{53334}  

     

    Brand:
    Cayman
    SKU:29087 - 10 mg

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  • Arundic acid is an inhibitor of astrocyte activation.{53333} It reduces increases in brain glial fibrillary acid protein (GFAP) and S100β levels, markers of astrocyte activation, in a rat model of permanent focal ischemia induced by middle cerebral artery occlusion when administered at a dose of 10 mg/kg. Arundic acid (3 and 10 mg/kg) decreases the number of TUNEL-positive neurons, reduces infarct size, and improves motor performance in the rotarod test in the same model. It also reduces descent time and time to turn in a pole test, indicating reversal of motor deficits, in a mouse model of MPTP-induced Parkinson’s disease when administered at a dose of 30 mg/kg.{53334}  

     

    Brand:
    Cayman
    SKU:29087 - 25 mg

    Available on backorder

  • Arundic acid is an inhibitor of astrocyte activation.{53333} It reduces increases in brain glial fibrillary acid protein (GFAP) and S100β levels, markers of astrocyte activation, in a rat model of permanent focal ischemia induced by middle cerebral artery occlusion when administered at a dose of 10 mg/kg. Arundic acid (3 and 10 mg/kg) decreases the number of TUNEL-positive neurons, reduces infarct size, and improves motor performance in the rotarod test in the same model. It also reduces descent time and time to turn in a pole test, indicating reversal of motor deficits, in a mouse model of MPTP-induced Parkinson’s disease when administered at a dose of 30 mg/kg.{53334}  

     

    Brand:
    Cayman
    SKU:29087 - 5 mg

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  • ARV-771 is a proteolysis-targeting chimera (PROTAC) that drives the degradation of bromodomain and extra terminal domain (BET) family proteins.{33349} It is comprised of a BET-binding moiety conjugated via a linker to a von Hippel-Lindau (VHL) E3 ligase-binding moiety. ARV-771 induces degradation of bromodomain-containing protein 2 (BRD2), BRD3, and BRD4 in 22Rv1 castration-resistant prostate cancer (CRPC) cells with half-maximal degradation (DC50) values of less than 5 nM for all. It inhibits proliferation of and increases poly(ADP-ribose) polymerase (PARP) cleavage in 22Rv1 cells in a concentration-dependent manner. ARV-771 reduces full-length androgen receptor protein levels and prevents increases in ERG induced by the synthetic androgen R1881 in VCaP cells in a concentration-dependent manner. ARV-771 (30 mg/kg per day, s.c.) induces tumor regression in a 22Rv1 mouse xenograft model.  

     

    Brand:
    Cayman
    SKU:21299 -

    Out of stock

  • ARV-771 is a proteolysis-targeting chimera (PROTAC) that drives the degradation of bromodomain and extra terminal domain (BET) family proteins.{33349} It is comprised of a BET-binding moiety conjugated via a linker to a von Hippel-Lindau (VHL) E3 ligase-binding moiety. ARV-771 induces degradation of bromodomain-containing protein 2 (BRD2), BRD3, and BRD4 in 22Rv1 castration-resistant prostate cancer (CRPC) cells with half-maximal degradation (DC50) values of less than 5 nM for all. It inhibits proliferation of and increases poly(ADP-ribose) polymerase (PARP) cleavage in 22Rv1 cells in a concentration-dependent manner. ARV-771 reduces full-length androgen receptor protein levels and prevents increases in ERG induced by the synthetic androgen R1881 in VCaP cells in a concentration-dependent manner. ARV-771 (30 mg/kg per day, s.c.) induces tumor regression in a 22Rv1 mouse xenograft model.  

     

    Brand:
    Cayman
    SKU:21299 -

    Out of stock

  • ARV-771 is a proteolysis-targeting chimera (PROTAC) that drives the degradation of bromodomain and extra terminal domain (BET) family proteins.{33349} It is comprised of a BET-binding moiety conjugated via a linker to a von Hippel-Lindau (VHL) E3 ligase-binding moiety. ARV-771 induces degradation of bromodomain-containing protein 2 (BRD2), BRD3, and BRD4 in 22Rv1 castration-resistant prostate cancer (CRPC) cells with half-maximal degradation (DC50) values of less than 5 nM for all. It inhibits proliferation of and increases poly(ADP-ribose) polymerase (PARP) cleavage in 22Rv1 cells in a concentration-dependent manner. ARV-771 reduces full-length androgen receptor protein levels and prevents increases in ERG induced by the synthetic androgen R1881 in VCaP cells in a concentration-dependent manner. ARV-771 (30 mg/kg per day, s.c.) induces tumor regression in a 22Rv1 mouse xenograft model.  

     

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    Cayman
    SKU:21299 -

    Out of stock

  • ARV-825 is a hetero-bifunctional molecule that is composed of a BRD4 binding moiety joined to an E3 ligase cereblon binding moiety using proteolysis targeting chimera (PROTAC) technology.{32899} ARV-825 actively recruits BRD4 to cereblon, resulting in the rapid and efficient degradation of BRD4 by the proteasome (50% maximum degradation at 14643), a competitor for binding to cereblon.{32966}  

     

    Brand:
    Cayman
    SKU:21109 -

    Out of stock

  • ARV-825 is a hetero-bifunctional molecule that is composed of a BRD4 binding moiety joined to an E3 ligase cereblon binding moiety using proteolysis targeting chimera (PROTAC) technology.{32899} ARV-825 actively recruits BRD4 to cereblon, resulting in the rapid and efficient degradation of BRD4 by the proteasome (50% maximum degradation at 14643), a competitor for binding to cereblon.{32966}  

     

    Brand:
    Cayman
    SKU:21109 -

    Out of stock

  • ARV-825 is a hetero-bifunctional molecule that is composed of a BRD4 binding moiety joined to an E3 ligase cereblon binding moiety using proteolysis targeting chimera (PROTAC) technology.{32899} ARV-825 actively recruits BRD4 to cereblon, resulting in the rapid and efficient degradation of BRD4 by the proteasome (50% maximum degradation at 14643), a competitor for binding to cereblon.{32966}  

     

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    Cayman
    SKU:21109 -

    Out of stock

  • Arvanil is a structural analog of capsaicin, which is the noxious active component of hot peppers of the Capsicum family. It is the amide of vanillylamine and arachidonic acid. Arvanil induces analgesia in rat and mouse models of pain.{7203} Arvanil has complex interactions with the cannabinoid system, in that it potentiates the agonist activity of endogenous cannabinoids by inhibiting the reuptake of arachidonoyl ethanolamide (AEA). It is an agonist at CB1 (Ki values of 0.25 to 0.52 μM), but not CB2, receptors, and is resistant to hydrolysis by FAAH.{7209} The vasodilator, analgesic, and anti-inflammatory properties of arvanil are not clearly explained by its interactions with cannabinoid and vanilloid receptors, suggesting other possible sites of action.  

     

    Brand:
    Cayman
    SKU:90052 - 10 mg

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  • Arvanil is a structural analog of capsaicin, which is the noxious active component of hot peppers of the Capsicum family. It is the amide of vanillylamine and arachidonic acid. Arvanil induces analgesia in rat and mouse models of pain.{7203} Arvanil has complex interactions with the cannabinoid system, in that it potentiates the agonist activity of endogenous cannabinoids by inhibiting the reuptake of arachidonoyl ethanolamide (AEA). It is an agonist at CB1 (Ki values of 0.25 to 0.52 μM), but not CB2, receptors, and is resistant to hydrolysis by FAAH.{7209} The vasodilator, analgesic, and anti-inflammatory properties of arvanil are not clearly explained by its interactions with cannabinoid and vanilloid receptors, suggesting other possible sites of action.  

     

    Brand:
    Cayman
    SKU:90052 - 100 mg

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  • Arvanil is a structural analog of capsaicin, which is the noxious active component of hot peppers of the Capsicum family. It is the amide of vanillylamine and arachidonic acid. Arvanil induces analgesia in rat and mouse models of pain.{7203} Arvanil has complex interactions with the cannabinoid system, in that it potentiates the agonist activity of endogenous cannabinoids by inhibiting the reuptake of arachidonoyl ethanolamide (AEA). It is an agonist at CB1 (Ki values of 0.25 to 0.52 μM), but not CB2, receptors, and is resistant to hydrolysis by FAAH.{7209} The vasodilator, analgesic, and anti-inflammatory properties of arvanil are not clearly explained by its interactions with cannabinoid and vanilloid receptors, suggesting other possible sites of action.  

     

    Brand:
    Cayman
    SKU:90052 - 5 mg

    Available on backorder

  • Arvanil is a structural analog of capsaicin, which is the noxious active component of hot peppers of the Capsicum family. It is the amide of vanillylamine and arachidonic acid. Arvanil induces analgesia in rat and mouse models of pain.{7203} Arvanil has complex interactions with the cannabinoid system, in that it potentiates the agonist activity of endogenous cannabinoids by inhibiting the reuptake of arachidonoyl ethanolamide (AEA). It is an agonist at CB1 (Ki values of 0.25 to 0.52 μM), but not CB2, receptors, and is resistant to hydrolysis by FAAH.{7209} The vasodilator, analgesic, and anti-inflammatory properties of arvanil are not clearly explained by its interactions with cannabinoid and vanilloid receptors, suggesting other possible sites of action.  

     

    Brand:
    Cayman
    SKU:90052 - 50 mg

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  • Arylquin 1 is a prostate apoptosis response-4 (Par-4) secretagogue.{27360} It binds to vimentin to displace Par-4 for secretion. Arylquin 1 induces Par-4 secretion from mouse embryonic fibroblasts (MEFs) and prostate cancer cells in vitro, effects that can be blocked by the inhibitor of vesicular transport brefeldin A (Item No. 11861). Arylquin 1 induces paracrine apoptosis of H1299, HOP92, and H460 cancer cells when co-cultured with Par-4+/+, but not Par-4-/-, MEFs.  

     

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    Cayman
    SKU:-

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  • Arylquin 1 is a prostate apoptosis response-4 (Par-4) secretagogue.{27360} It binds to vimentin to displace Par-4 for secretion. Arylquin 1 induces Par-4 secretion from mouse embryonic fibroblasts (MEFs) and prostate cancer cells in vitro, effects that can be blocked by the inhibitor of vesicular transport brefeldin A (Item No. 11861). Arylquin 1 induces paracrine apoptosis of H1299, HOP92, and H460 cancer cells when co-cultured with Par-4+/+, but not Par-4-/-, MEFs.  

     

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    Cayman
    SKU:-

    Out of stock

  • Arylquin 1 is a prostate apoptosis response-4 (Par-4) secretagogue.{27360} It binds to vimentin to displace Par-4 for secretion. Arylquin 1 induces Par-4 secretion from mouse embryonic fibroblasts (MEFs) and prostate cancer cells in vitro, effects that can be blocked by the inhibitor of vesicular transport brefeldin A (Item No. 11861). Arylquin 1 induces paracrine apoptosis of H1299, HOP92, and H460 cancer cells when co-cultured with Par-4+/+, but not Par-4-/-, MEFs.  

     

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    Cayman
    SKU:-

    Out of stock

  • The phosphatidylinositol 3-kinases (PI3Ks) are lipid and protein kinases involved in diverse biological processes, including cell growth, migration, and metabolism.{17822} AS-041164 is a potent inhibitor of PI3K with selectivity for the class IB isoform PI3Kγ (IC50 = 70 nM), compared to PI3Kα (IC50 = 240 nM), PI3Kβ (IC50 = 1.45 μM), and PI3Kδ (IC50 =1.70 μM).{17823} When tested at 1.0 μM, it shows little or no activity against 38 other common kinases.{17823} When given orally to mice, AS-041164 shows a pharmacokinetic profile that is similar to the general PI3K inhibitor LY294002 but is three times more potent (ED50 = 27.4 mg/kg for AS-041164 versus 81.6 mg/kg for LY294002) in blocking neutrophil recruitment induced by RANTES.{17823}  

     

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    Cayman
    SKU:-
  • The phosphatidylinositol 3-kinases (PI3Ks) are lipid and protein kinases involved in diverse biological processes, including cell growth, migration, and metabolism.{17822} AS-041164 is a potent inhibitor of PI3K with selectivity for the class IB isoform PI3Kγ (IC50 = 70 nM), compared to PI3Kα (IC50 = 240 nM), PI3Kβ (IC50 = 1.45 μM), and PI3Kδ (IC50 =1.70 μM).{17823} When tested at 1.0 μM, it shows little or no activity against 38 other common kinases.{17823} When given orally to mice, AS-041164 shows a pharmacokinetic profile that is similar to the general PI3K inhibitor LY294002 but is three times more potent (ED50 = 27.4 mg/kg for AS-041164 versus 81.6 mg/kg for LY294002) in blocking neutrophil recruitment induced by RANTES.{17823}  

     

    Brand:
    Cayman
    SKU:-
  • The phosphatidylinositol 3-kinases (PI3Ks) are lipid and protein kinases involved in diverse biological processes, including cell growth, migration, and metabolism.{17822} AS-041164 is a potent inhibitor of PI3K with selectivity for the class IB isoform PI3Kγ (IC50 = 70 nM), compared to PI3Kα (IC50 = 240 nM), PI3Kβ (IC50 = 1.45 μM), and PI3Kδ (IC50 =1.70 μM).{17823} When tested at 1.0 μM, it shows little or no activity against 38 other common kinases.{17823} When given orally to mice, AS-041164 shows a pharmacokinetic profile that is similar to the general PI3K inhibitor LY294002 but is three times more potent (ED50 = 27.4 mg/kg for AS-041164 versus 81.6 mg/kg for LY294002) in blocking neutrophil recruitment induced by RANTES.{17823}  

     

    Brand:
    Cayman
    SKU:-
  • The phosphatidylinositol 3-kinases (PI3Ks) are lipid and protein kinases involved in diverse biological processes, including cell growth, migration, and metabolism.{17822} AS-041164 is a potent inhibitor of PI3K with selectivity for the class IB isoform PI3Kγ (IC50 = 70 nM), compared to PI3Kα (IC50 = 240 nM), PI3Kβ (IC50 = 1.45 μM), and PI3Kδ (IC50 =1.70 μM).{17823} When tested at 1.0 μM, it shows little or no activity against 38 other common kinases.{17823} When given orally to mice, AS-041164 shows a pharmacokinetic profile that is similar to the general PI3K inhibitor LY294002 but is three times more potent (ED50 = 27.4 mg/kg for AS-041164 versus 81.6 mg/kg for LY294002) in blocking neutrophil recruitment induced by RANTES.{17823}  

     

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    Cayman
    SKU:-
  • AS-101 is an immunomodulator.{36943} It inhibits IL-10 secretion from and cell proliferation of IL-10-secreting human stomach adenocarcinoma and glioblastoma multiforme (GBM) cells when used at concentrations ranging from 0.5 to 2.5 µg/ml, an effect that can be blocked by the addition of recombinant IL-10. It reverses IL-10-induced increases in phosphorylated Stat3 and reduces the expression of Bcl-2 in B16 murine melanoma cells. AS-101 sensitizes GBM cells to paclitaxel (Item No. 10461), doxorubicin (Item No. 15007), and 5-fluorouracil (5-FU; Item No. 14416) in vitro and to paclitaxel in a GBM mouse xenograft model when administered at a dose of 0.5 mg/kg per day. AS-101 (1 mg/kg) also prevents infiltration of CD49d+ cells and decreases the expression of IL-6, TNF-α, IL-1β, and MCP-1 in the spinal cord, as well as delays onset and slows the progression of symptoms in a mouse model of experimental autoimmune encephalomyelitis (EAE).{36944}  

     

    Brand:
    Cayman
    SKU:21443 -

    Out of stock

  • AS-101 is an immunomodulator.{36943} It inhibits IL-10 secretion from and cell proliferation of IL-10-secreting human stomach adenocarcinoma and glioblastoma multiforme (GBM) cells when used at concentrations ranging from 0.5 to 2.5 µg/ml, an effect that can be blocked by the addition of recombinant IL-10. It reverses IL-10-induced increases in phosphorylated Stat3 and reduces the expression of Bcl-2 in B16 murine melanoma cells. AS-101 sensitizes GBM cells to paclitaxel (Item No. 10461), doxorubicin (Item No. 15007), and 5-fluorouracil (5-FU; Item No. 14416) in vitro and to paclitaxel in a GBM mouse xenograft model when administered at a dose of 0.5 mg/kg per day. AS-101 (1 mg/kg) also prevents infiltration of CD49d+ cells and decreases the expression of IL-6, TNF-α, IL-1β, and MCP-1 in the spinal cord, as well as delays onset and slows the progression of symptoms in a mouse model of experimental autoimmune encephalomyelitis (EAE).{36944}  

     

    Brand:
    Cayman
    SKU:21443 -

    Out of stock

  • AS-101 is an immunomodulator.{36943} It inhibits IL-10 secretion from and cell proliferation of IL-10-secreting human stomach adenocarcinoma and glioblastoma multiforme (GBM) cells when used at concentrations ranging from 0.5 to 2.5 µg/ml, an effect that can be blocked by the addition of recombinant IL-10. It reverses IL-10-induced increases in phosphorylated Stat3 and reduces the expression of Bcl-2 in B16 murine melanoma cells. AS-101 sensitizes GBM cells to paclitaxel (Item No. 10461), doxorubicin (Item No. 15007), and 5-fluorouracil (5-FU; Item No. 14416) in vitro and to paclitaxel in a GBM mouse xenograft model when administered at a dose of 0.5 mg/kg per day. AS-101 (1 mg/kg) also prevents infiltration of CD49d+ cells and decreases the expression of IL-6, TNF-α, IL-1β, and MCP-1 in the spinal cord, as well as delays onset and slows the progression of symptoms in a mouse model of experimental autoimmune encephalomyelitis (EAE).{36944}  

     

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    Cayman
    SKU:21443 -

    Out of stock

  • GPR119, a glucose-dependent insulinotropic receptor, is a Gs protein-coupled receptor that is expressed in pancreas β-cells and intestinal L-cells.{14046} Activation of GPR119 by the endogenous ligands lyso-phosphatidylcholine and oleoyl ethanolamide increases intracellular cAMP levels and promotes glucose-stimulated insulin secretion.{14046,18880} AS-1269574 is an agonist of GPR119 that is effective both in isolated cells and in vivo.{18583} It increases cAMP levels in HEK293 cells transfected with human GPR119 (EC50 = 2.5 μM) and glucose-stimulated insulin secretion in mice (100 mg/kg).{18583}  

     

    Brand:
    Cayman
    SKU:10626 - 1 mg

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  • GPR119, a glucose-dependent insulinotropic receptor, is a Gs protein-coupled receptor that is expressed in pancreas β-cells and intestinal L-cells.{14046} Activation of GPR119 by the endogenous ligands lyso-phosphatidylcholine and oleoyl ethanolamide increases intracellular cAMP levels and promotes glucose-stimulated insulin secretion.{14046,18880} AS-1269574 is an agonist of GPR119 that is effective both in isolated cells and in vivo.{18583} It increases cAMP levels in HEK293 cells transfected with human GPR119 (EC50 = 2.5 μM) and glucose-stimulated insulin secretion in mice (100 mg/kg).{18583}  

     

    Brand:
    Cayman
    SKU:10626 - 10 mg

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  • GPR119, a glucose-dependent insulinotropic receptor, is a Gs protein-coupled receptor that is expressed in pancreas β-cells and intestinal L-cells.{14046} Activation of GPR119 by the endogenous ligands lyso-phosphatidylcholine and oleoyl ethanolamide increases intracellular cAMP levels and promotes glucose-stimulated insulin secretion.{14046,18880} AS-1269574 is an agonist of GPR119 that is effective both in isolated cells and in vivo.{18583} It increases cAMP levels in HEK293 cells transfected with human GPR119 (EC50 = 2.5 μM) and glucose-stimulated insulin secretion in mice (100 mg/kg).{18583}  

     

    Brand:
    Cayman
    SKU:10626 - 25 mg

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  • GPR119, a glucose-dependent insulinotropic receptor, is a Gs protein-coupled receptor that is expressed in pancreas β-cells and intestinal L-cells.{14046} Activation of GPR119 by the endogenous ligands lyso-phosphatidylcholine and oleoyl ethanolamide increases intracellular cAMP levels and promotes glucose-stimulated insulin secretion.{14046,18880} AS-1269574 is an agonist of GPR119 that is effective both in isolated cells and in vivo.{18583} It increases cAMP levels in HEK293 cells transfected with human GPR119 (EC50 = 2.5 μM) and glucose-stimulated insulin secretion in mice (100 mg/kg).{18583}  

     

    Brand:
    Cayman
    SKU:10626 - 5 mg

    Available on backorder

  • AS-1842856 is a potent inhibitor of forkhead box class O transcription factor 1 (FoxO1; IC50 = 33 nM in HepG2 cells).{37141} Inhibition of FoxO1-mediated transactivation with AS-1842856 leads to a dose-dependent decrease in expression of glucose-6 phosphatase (G6Pase) and phosphoenolpyruvate carboxykinase (PEPCK) mRNA and inhibits glucogenesis in rat hepatoma Fao cells and a murine model of type 2 diabetes mellitus (T2DM). AS-1842856 also inhibits 3T3-L1 preadipocyte differentiation and reduces lipid droplet growth in adipocytes.{37142},{37143}  

     

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    Cayman
    SKU:-

    Out of stock

  • AS-1842856 is a potent inhibitor of forkhead box class O transcription factor 1 (FoxO1; IC50 = 33 nM in HepG2 cells).{37141} Inhibition of FoxO1-mediated transactivation with AS-1842856 leads to a dose-dependent decrease in expression of glucose-6 phosphatase (G6Pase) and phosphoenolpyruvate carboxykinase (PEPCK) mRNA and inhibits glucogenesis in rat hepatoma Fao cells and a murine model of type 2 diabetes mellitus (T2DM). AS-1842856 also inhibits 3T3-L1 preadipocyte differentiation and reduces lipid droplet growth in adipocytes.{37142},{37143}  

     

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    Cayman
    SKU:-

    Out of stock

  • AS-1842856 is a potent inhibitor of forkhead box class O transcription factor 1 (FoxO1; IC50 = 33 nM in HepG2 cells).{37141} Inhibition of FoxO1-mediated transactivation with AS-1842856 leads to a dose-dependent decrease in expression of glucose-6 phosphatase (G6Pase) and phosphoenolpyruvate carboxykinase (PEPCK) mRNA and inhibits glucogenesis in rat hepatoma Fao cells and a murine model of type 2 diabetes mellitus (T2DM). AS-1842856 also inhibits 3T3-L1 preadipocyte differentiation and reduces lipid droplet growth in adipocytes.{37142},{37143}  

     

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    Cayman
    SKU:-

    Out of stock

  • AS-1892802 is a potent inhibitor of Rho-associated serine-threonine protein kinases (ROCKs; IC50s = 122, 52, and 57 nM for human ROCK1, ROCK2, and rat ROCK2, respectively).{40426} It is selective for ROCK1 and 2 over a panel of 167 kinases and a panel of 63 ion channels, receptors, and enzymes at a concentration of 10 μM. However, AS-1892802 inhibits protein kinase catalytic subunit (PKACα) and protein kinase X gene (PRKX) with IC50 values of 200 and 325 nM, respectively. AS-1892802 reduces weight imbalance deficits (ED50 = 0.15 mg/kg) in rats in a monoiodoacetate-induced model of non-inflammatory arthritis. It also has analgesic-like effects in a rat model of diabetic neuropathy induced by streptozotocin (Item No. 13104) and reduces cartilage damage and weight imbalance deficits in a rat model of osteoarthritis.{40427,40428}  

     

    Brand:
    Cayman
    SKU:-
  • AS-1892802 is a potent inhibitor of Rho-associated serine-threonine protein kinases (ROCKs; IC50s = 122, 52, and 57 nM for human ROCK1, ROCK2, and rat ROCK2, respectively).{40426} It is selective for ROCK1 and 2 over a panel of 167 kinases and a panel of 63 ion channels, receptors, and enzymes at a concentration of 10 μM. However, AS-1892802 inhibits protein kinase catalytic subunit (PKACα) and protein kinase X gene (PRKX) with IC50 values of 200 and 325 nM, respectively. AS-1892802 reduces weight imbalance deficits (ED50 = 0.15 mg/kg) in rats in a monoiodoacetate-induced model of non-inflammatory arthritis. It also has analgesic-like effects in a rat model of diabetic neuropathy induced by streptozotocin (Item No. 13104) and reduces cartilage damage and weight imbalance deficits in a rat model of osteoarthritis.{40427,40428}  

     

    Brand:
    Cayman
    SKU:-
  • AS-1892802 is a potent inhibitor of Rho-associated serine-threonine protein kinases (ROCKs; IC50s = 122, 52, and 57 nM for human ROCK1, ROCK2, and rat ROCK2, respectively).{40426} It is selective for ROCK1 and 2 over a panel of 167 kinases and a panel of 63 ion channels, receptors, and enzymes at a concentration of 10 μM. However, AS-1892802 inhibits protein kinase catalytic subunit (PKACα) and protein kinase X gene (PRKX) with IC50 values of 200 and 325 nM, respectively. AS-1892802 reduces weight imbalance deficits (ED50 = 0.15 mg/kg) in rats in a monoiodoacetate-induced model of non-inflammatory arthritis. It also has analgesic-like effects in a rat model of diabetic neuropathy induced by streptozotocin (Item No. 13104) and reduces cartilage damage and weight imbalance deficits in a rat model of osteoarthritis.{40427,40428}  

     

    Brand:
    Cayman
    SKU:-
  • AS-1892802 is a potent inhibitor of Rho-associated serine-threonine protein kinases (ROCKs; IC50s = 122, 52, and 57 nM for human ROCK1, ROCK2, and rat ROCK2, respectively).{40426} It is selective for ROCK1 and 2 over a panel of 167 kinases and a panel of 63 ion channels, receptors, and enzymes at a concentration of 10 μM. However, AS-1892802 inhibits protein kinase catalytic subunit (PKACα) and protein kinase X gene (PRKX) with IC50 values of 200 and 325 nM, respectively. AS-1892802 reduces weight imbalance deficits (ED50 = 0.15 mg/kg) in rats in a monoiodoacetate-induced model of non-inflammatory arthritis. It also has analgesic-like effects in a rat model of diabetic neuropathy induced by streptozotocin (Item No. 13104) and reduces cartilage damage and weight imbalance deficits in a rat model of osteoarthritis.{40427,40428}  

     

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    Cayman
    SKU:-
  • AS-19 is an agonist of the serotonin (5-HT) receptor subtype 5-HT7 (Ki = 0.6 nM).{48277} It is selective for 5-HT7 over 5-HT1A, 5-HT1B, 5-HT1D, and 5-HT5A receptors (Kis = 89.7, 490, 6.6 and 98.5 nM, respectively), as well as sigma-1 and imidazoline I2 receptors (Kis = 657 and 282 nM, respectively). AS-19 increases conditioned responses and reverses amnesia induced by the muscarinic acetylcholine receptor antagonist scopolamine in rats in an autoshaping learning task when administered post-training at a dose of 5 mg/kg.{48278} It increases the paw withdrawal threshold in a mechanical pressure test in rats with chronic constriction injury when 0.3 µl of a 1.5 nM solution is injected into the ventrolateral periaqueductal gray area (vlPAG), an effect that can be blocked by the 5-HT7 receptor antagonist SB-269970 (Item No. 17081).{48279}  

     

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    Cayman
    SKU:20642 -

    Available on backorder

  • AS-19 is an agonist of the serotonin (5-HT) receptor subtype 5-HT7 (Ki = 0.6 nM).{48277} It is selective for 5-HT7 over 5-HT1A, 5-HT1B, 5-HT1D, and 5-HT5A receptors (Kis = 89.7, 490, 6.6 and 98.5 nM, respectively), as well as sigma-1 and imidazoline I2 receptors (Kis = 657 and 282 nM, respectively). AS-19 increases conditioned responses and reverses amnesia induced by the muscarinic acetylcholine receptor antagonist scopolamine in rats in an autoshaping learning task when administered post-training at a dose of 5 mg/kg.{48278} It increases the paw withdrawal threshold in a mechanical pressure test in rats with chronic constriction injury when 0.3 µl of a 1.5 nM solution is injected into the ventrolateral periaqueductal gray area (vlPAG), an effect that can be blocked by the 5-HT7 receptor antagonist SB-269970 (Item No. 17081).{48279}  

     

    Brand:
    Cayman
    SKU:20642 -

    Available on backorder

  • AS-19 is an agonist of the serotonin (5-HT) receptor subtype 5-HT7 (Ki = 0.6 nM).{48277} It is selective for 5-HT7 over 5-HT1A, 5-HT1B, 5-HT1D, and 5-HT5A receptors (Kis = 89.7, 490, 6.6 and 98.5 nM, respectively), as well as sigma-1 and imidazoline I2 receptors (Kis = 657 and 282 nM, respectively). AS-19 increases conditioned responses and reverses amnesia induced by the muscarinic acetylcholine receptor antagonist scopolamine in rats in an autoshaping learning task when administered post-training at a dose of 5 mg/kg.{48278} It increases the paw withdrawal threshold in a mechanical pressure test in rats with chronic constriction injury when 0.3 µl of a 1.5 nM solution is injected into the ventrolateral periaqueductal gray area (vlPAG), an effect that can be blocked by the 5-HT7 receptor antagonist SB-269970 (Item No. 17081).{48279}  

     

    Brand:
    Cayman
    SKU:20642 -

    Available on backorder

  • SH2 domain-containing inositol 5’-phosphatase 2 (SHIP2) negatively regulates the insulin signaling pathway by hydrolyzing phosphatidylinositol-3,4,5-trisphosphate.{22158} Its activity has been implicated in the pathogenesis of insulin resistance and type 2 diabetes.{12707} AS-1949490 is a small molecule inhibitor of SHIP2 (IC50s = 0.62 and 0.34 µM for human and mouse, respectively; Ki = 0.44 µM for hSHIP2).{28682} It is not as potent an inhibitor of SHIP1, demonstrating inhibitory values 30-fold higher than that of SHIP2, and shows little effect against the phosphatases PTEN, synaptojanin, and myotubularin (IC50s >50 µM).{28682} AS-1949490 has been shown to dose-dependently increase insulin-induced phosphorylation of Akt and to activate glucose metabolism.{28682} It has also been shown to suppress gluconeogenesis through reduced expression of PEPCK and G6Pase mRNA in normal mice and to decrease plasma glucose in diabetic db/db mice.{28682}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • SH2 domain-containing inositol 5’-phosphatase 2 (SHIP2) negatively regulates the insulin signaling pathway by hydrolyzing phosphatidylinositol-3,4,5-trisphosphate.{22158} Its activity has been implicated in the pathogenesis of insulin resistance and type 2 diabetes.{12707} AS-1949490 is a small molecule inhibitor of SHIP2 (IC50s = 0.62 and 0.34 µM for human and mouse, respectively; Ki = 0.44 µM for hSHIP2).{28682} It is not as potent an inhibitor of SHIP1, demonstrating inhibitory values 30-fold higher than that of SHIP2, and shows little effect against the phosphatases PTEN, synaptojanin, and myotubularin (IC50s >50 µM).{28682} AS-1949490 has been shown to dose-dependently increase insulin-induced phosphorylation of Akt and to activate glucose metabolism.{28682} It has also been shown to suppress gluconeogenesis through reduced expression of PEPCK and G6Pase mRNA in normal mice and to decrease plasma glucose in diabetic db/db mice.{28682}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • SH2 domain-containing inositol 5’-phosphatase 2 (SHIP2) negatively regulates the insulin signaling pathway by hydrolyzing phosphatidylinositol-3,4,5-trisphosphate.{22158} Its activity has been implicated in the pathogenesis of insulin resistance and type 2 diabetes.{12707} AS-1949490 is a small molecule inhibitor of SHIP2 (IC50s = 0.62 and 0.34 µM for human and mouse, respectively; Ki = 0.44 µM for hSHIP2).{28682} It is not as potent an inhibitor of SHIP1, demonstrating inhibitory values 30-fold higher than that of SHIP2, and shows little effect against the phosphatases PTEN, synaptojanin, and myotubularin (IC50s >50 µM).{28682} AS-1949490 has been shown to dose-dependently increase insulin-induced phosphorylation of Akt and to activate glucose metabolism.{28682} It has also been shown to suppress gluconeogenesis through reduced expression of PEPCK and G6Pase mRNA in normal mice and to decrease plasma glucose in diabetic db/db mice.{28682}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • SH2 domain-containing inositol 5’-phosphatase 2 (SHIP2) negatively regulates the insulin signaling pathway by hydrolyzing phosphatidylinositol-3,4,5-trisphosphate.{22158} Its activity has been implicated in the pathogenesis of insulin resistance and type 2 diabetes.{12707} AS-1949490 is a small molecule inhibitor of SHIP2 (IC50s = 0.62 and 0.34 µM for human and mouse, respectively; Ki = 0.44 µM for hSHIP2).{28682} It is not as potent an inhibitor of SHIP1, demonstrating inhibitory values 30-fold higher than that of SHIP2, and shows little effect against the phosphatases PTEN, synaptojanin, and myotubularin (IC50s >50 µM).{28682} AS-1949490 has been shown to dose-dependently increase insulin-induced phosphorylation of Akt and to activate glucose metabolism.{28682} It has also been shown to suppress gluconeogenesis through reduced expression of PEPCK and G6Pase mRNA in normal mice and to decrease plasma glucose in diabetic db/db mice.{28682}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • AS-2077715 is a fungal metabolite and an inhibitor of fungal mitochondrial complex III (cytochrome bc1; IC50 = 80 ng/ml for T. mentagrophytes complex III).{52421} It is selective for fungal over mammalian complex III (IC50s = 480 and 860 ng/ml for murine EL-4 cell and human Jurkat cell complex III, respectively). AS-2077715 inhibits ATP production in (IC50 = 0.33 µg/ml) and is fungicidal against T. mentagrophytes when used at concentrations of 1 and 10 µg/ml. In vivo, AS-2077715 (10 and 20 mg/kg) reduces the number of foot pad skin colony forming units (CFUs) in a guinea pig model of T. mentagrophytes infection.{52422}  

     

    Brand:
    Cayman
    SKU:29775 - 1 mg

    Available on backorder

  • AS-2444697 is an inhibitor of interleukin-1 receptor-associated kinase 4 (IRAK4; IC50 = 21 nM).{52225} It is greater than 30-fold selective for IRAK4 over a panel of 146 kinases, but is less than 10-fold selective over PDGFRα, PDGFRβ, TrkA, TrkC, CLK1, Itk, and FLT3. AS-2444697 inhibits IL-1β-induced IL-6 production and LPS-induced TNF-α production in cellular assays (IC50s = 250 and 47 nM, respectively). It is efficacious in rat models of adjuvant- and collagen-induced arthritis (ED50s = 2.7 and 1.6 mg/kg, respectively). AS-2444697 (0.3-3 mg/kg, twice daily) reduces urinary protein excretion, the development of interstitial fibrosis and glomerulosclerosis, and renal mRNA expression of genes encoding IL-1β, IL-6, TNF-α, and chemokine (C-C motif) ligand 2 (CCL2) without affecting blood pressure in the 5/6 nephrectomized rat model of chronic kidney disease.{52226}  

     

    Brand:
    Cayman
    SKU:29505 - 1 mg

    Available on backorder

  • AS-2444697 is an inhibitor of interleukin-1 receptor-associated kinase 4 (IRAK4; IC50 = 21 nM).{52225} It is greater than 30-fold selective for IRAK4 over a panel of 146 kinases, but is less than 10-fold selective over PDGFRα, PDGFRβ, TrkA, TrkC, CLK1, Itk, and FLT3. AS-2444697 inhibits IL-1β-induced IL-6 production and LPS-induced TNF-α production in cellular assays (IC50s = 250 and 47 nM, respectively). It is efficacious in rat models of adjuvant- and collagen-induced arthritis (ED50s = 2.7 and 1.6 mg/kg, respectively). AS-2444697 (0.3-3 mg/kg, twice daily) reduces urinary protein excretion, the development of interstitial fibrosis and glomerulosclerosis, and renal mRNA expression of genes encoding IL-1β, IL-6, TNF-α, and chemokine (C-C motif) ligand 2 (CCL2) without affecting blood pressure in the 5/6 nephrectomized rat model of chronic kidney disease.{52226}  

     

    Brand:
    Cayman
    SKU:29505 - 10 mg

    Available on backorder

  • AS-2444697 is an inhibitor of interleukin-1 receptor-associated kinase 4 (IRAK4; IC50 = 21 nM).{52225} It is greater than 30-fold selective for IRAK4 over a panel of 146 kinases, but is less than 10-fold selective over PDGFRα, PDGFRβ, TrkA, TrkC, CLK1, Itk, and FLT3. AS-2444697 inhibits IL-1β-induced IL-6 production and LPS-induced TNF-α production in cellular assays (IC50s = 250 and 47 nM, respectively). It is efficacious in rat models of adjuvant- and collagen-induced arthritis (ED50s = 2.7 and 1.6 mg/kg, respectively). AS-2444697 (0.3-3 mg/kg, twice daily) reduces urinary protein excretion, the development of interstitial fibrosis and glomerulosclerosis, and renal mRNA expression of genes encoding IL-1β, IL-6, TNF-α, and chemokine (C-C motif) ligand 2 (CCL2) without affecting blood pressure in the 5/6 nephrectomized rat model of chronic kidney disease.{52226}  

     

    Brand:
    Cayman
    SKU:29505 - 5 mg

    Available on backorder

  • Phosphatidylinositol 3-kinase (PI3K) catalyzes the phosphorylation of Pl at the 3 position to produce the second messengers PtdIns-(3,4)-P2 and PtdIns-(3,4,5)-P3. {8039,12235,13740} PI3Kγ is a class 1B PI3K that is composed of a p110 catalytic subunit and a p101 or p84 regulatory subunit, whereas PI3Kα, β, and δ are class 1A enzymes composed of p110 and p85 subunits. {14518} AS-252424 is a potent inhibitor of phosphatidylinositol-3-kinase PI3K with selectivity for the γ isoform. It inhibits human recombinant PI3Kγ, α, β, and δ with IC50 values of 30, 940, 20,000 and 20,000 nM, respectively. {14230} AS-252424 also inhibits C5a-mediated phosphorylation of Akt in RAW 264.7 macrophages with an IC50 value of 0.23 µM. In a murine model of peritonitis, AS-252424 inhibited neutrophil recruitment 35% at a dose of 10 mg/kg. {14230}  

     

    Brand:
    Cayman
    SKU:10009052 - 1 mg

    Available on backorder

  • Phosphatidylinositol 3-kinase (PI3K) catalyzes the phosphorylation of Pl at the 3 position to produce the second messengers PtdIns-(3,4)-P2 and PtdIns-(3,4,5)-P3. {8039,12235,13740} PI3Kγ is a class 1B PI3K that is composed of a p110 catalytic subunit and a p101 or p84 regulatory subunit, whereas PI3Kα, β, and δ are class 1A enzymes composed of p110 and p85 subunits. {14518} AS-252424 is a potent inhibitor of phosphatidylinositol-3-kinase PI3K with selectivity for the γ isoform. It inhibits human recombinant PI3Kγ, α, β, and δ with IC50 values of 30, 940, 20,000 and 20,000 nM, respectively. {14230} AS-252424 also inhibits C5a-mediated phosphorylation of Akt in RAW 264.7 macrophages with an IC50 value of 0.23 µM. In a murine model of peritonitis, AS-252424 inhibited neutrophil recruitment 35% at a dose of 10 mg/kg. {14230}  

     

    Brand:
    Cayman
    SKU:10009052 - 10 mg

    Available on backorder

  • Phosphatidylinositol 3-kinase (PI3K) catalyzes the phosphorylation of Pl at the 3 position to produce the second messengers PtdIns-(3,4)-P2 and PtdIns-(3,4,5)-P3. {8039,12235,13740} PI3Kγ is a class 1B PI3K that is composed of a p110 catalytic subunit and a p101 or p84 regulatory subunit, whereas PI3Kα, β, and δ are class 1A enzymes composed of p110 and p85 subunits. {14518} AS-252424 is a potent inhibitor of phosphatidylinositol-3-kinase PI3K with selectivity for the γ isoform. It inhibits human recombinant PI3Kγ, α, β, and δ with IC50 values of 30, 940, 20,000 and 20,000 nM, respectively. {14230} AS-252424 also inhibits C5a-mediated phosphorylation of Akt in RAW 264.7 macrophages with an IC50 value of 0.23 µM. In a murine model of peritonitis, AS-252424 inhibited neutrophil recruitment 35% at a dose of 10 mg/kg. {14230}  

     

    Brand:
    Cayman
    SKU:10009052 - 25 mg

    Available on backorder

  • Phosphatidylinositol 3-kinase (PI3K) catalyzes the phosphorylation of Pl at the 3 position to produce the second messengers PtdIns-(3,4)-P2 and PtdIns-(3,4,5)-P3. {8039,12235,13740} PI3Kγ is a class 1B PI3K that is composed of a p110 catalytic subunit and a p101 or p84 regulatory subunit, whereas PI3Kα, β, and δ are class 1A enzymes composed of p110 and p85 subunits. {14518} AS-252424 is a potent inhibitor of phosphatidylinositol-3-kinase PI3K with selectivity for the γ isoform. It inhibits human recombinant PI3Kγ, α, β, and δ with IC50 values of 30, 940, 20,000 and 20,000 nM, respectively. {14230} AS-252424 also inhibits C5a-mediated phosphorylation of Akt in RAW 264.7 macrophages with an IC50 value of 0.23 µM. In a murine model of peritonitis, AS-252424 inhibited neutrophil recruitment 35% at a dose of 10 mg/kg. {14230}  

     

    Brand:
    Cayman
    SKU:10009052 - 5 mg

    Available on backorder

  • AS-2863619 is a dual inhibitor of cyclin-dependent kinase 8 (Cdk8) and Cdk19 (IC50s = 0.6 and 4.3 nM, respectively).{58029} It induces Foxp3 expression in isolated mouse naïve T cells when used at a concentration of 1 µM alone or synergistically in combination with TGF-β. AS-2863619 (30 mg/kg) decreases ear edema and induces production of Foxp3+ regulatory T cells (Tregs) in mice. It also reduces disease severity in a mouse model of experimental autoimmune encephalomyelitis (EAE).  

     

    Brand:
    Cayman
    SKU:30976 - 1 mg

    Available on backorder

  • AS-2863619 is a dual inhibitor of cyclin-dependent kinase 8 (Cdk8) and Cdk19 (IC50s = 0.6 and 4.3 nM, respectively).{58029} It induces Foxp3 expression in isolated mouse naïve T cells when used at a concentration of 1 µM alone or synergistically in combination with TGF-β. AS-2863619 (30 mg/kg) decreases ear edema and induces production of Foxp3+ regulatory T cells (Tregs) in mice. It also reduces disease severity in a mouse model of experimental autoimmune encephalomyelitis (EAE).  

     

    Brand:
    Cayman
    SKU:30976 - 5 mg

    Available on backorder

  • AS-2863619 is a dual inhibitor of cyclin-dependent kinase 8 (Cdk8) and Cdk19 (IC50s = 0.6 and 4.3 nM, respectively).{58029} It induces Foxp3 expression in isolated mouse naïve T cells when used at a concentration of 1 µM alone or synergistically in combination with TGF-β. AS-2863619 (30 mg/kg) decreases ear edema and induces production of Foxp3+ regulatory T cells (Tregs) in mice. It also reduces disease severity in a mouse model of experimental autoimmune encephalomyelitis (EAE).  

     

    Brand:
    Cayman
    SKU:30976 - 500 µg

    Available on backorder

  • Phosphatidylinositol 3-kinase (PI3K) catalyzes the phosphorylation of PI at the three position of the inositol ring to produce the second messengers PtdIns-(3,4)-P2 and PtdIns-(3,4,5)-P3.{8039,12235,13740} PI3Kγ is a class 1B PI3K that is composed of a p110 catalytic subunit and a p101 or p84 regulatory subunit, whereas PI3Kα, β, and δ are class 1A enzymes composed of p110 and p85 subunits.{14518} AS-604850 is a selective, ATP-competitive inhibitor of PI3Kγ with IC50 values of 0.25, >20, >20, and 4.5 µM for the human recombinant γ, δ, β, and α isoforms, respectively.{13338} AS-604850 inhibited MCP-1-mediated monocyte chemotaxis with an IC50 value of 21 µM and reduced RANTES-induced peritoneal neutrophil recruitment in a murine model of leukocyte chemotaxis with an ED50 value of 42.4 mg/kg.{13338}  

     

    Brand:
    Cayman
    SKU:10010175 - 1 mg

    Available on backorder

  • Phosphatidylinositol 3-kinase (PI3K) catalyzes the phosphorylation of PI at the three position of the inositol ring to produce the second messengers PtdIns-(3,4)-P2 and PtdIns-(3,4,5)-P3.{8039,12235,13740} PI3Kγ is a class 1B PI3K that is composed of a p110 catalytic subunit and a p101 or p84 regulatory subunit, whereas PI3Kα, β, and δ are class 1A enzymes composed of p110 and p85 subunits.{14518} AS-604850 is a selective, ATP-competitive inhibitor of PI3Kγ with IC50 values of 0.25, >20, >20, and 4.5 µM for the human recombinant γ, δ, β, and α isoforms, respectively.{13338} AS-604850 inhibited MCP-1-mediated monocyte chemotaxis with an IC50 value of 21 µM and reduced RANTES-induced peritoneal neutrophil recruitment in a murine model of leukocyte chemotaxis with an ED50 value of 42.4 mg/kg.{13338}  

     

    Brand:
    Cayman
    SKU:10010175 - 10 mg

    Available on backorder

  • Phosphatidylinositol 3-kinase (PI3K) catalyzes the phosphorylation of PI at the three position of the inositol ring to produce the second messengers PtdIns-(3,4)-P2 and PtdIns-(3,4,5)-P3.{8039,12235,13740} PI3Kγ is a class 1B PI3K that is composed of a p110 catalytic subunit and a p101 or p84 regulatory subunit, whereas PI3Kα, β, and δ are class 1A enzymes composed of p110 and p85 subunits.{14518} AS-604850 is a selective, ATP-competitive inhibitor of PI3Kγ with IC50 values of 0.25, >20, >20, and 4.5 µM for the human recombinant γ, δ, β, and α isoforms, respectively.{13338} AS-604850 inhibited MCP-1-mediated monocyte chemotaxis with an IC50 value of 21 µM and reduced RANTES-induced peritoneal neutrophil recruitment in a murine model of leukocyte chemotaxis with an ED50 value of 42.4 mg/kg.{13338}  

     

    Brand:
    Cayman
    SKU:10010175 - 25 mg

    Available on backorder

  • Phosphatidylinositol 3-kinase (PI3K) catalyzes the phosphorylation of PI at the three position of the inositol ring to produce the second messengers PtdIns-(3,4)-P2 and PtdIns-(3,4,5)-P3.{8039,12235,13740} PI3Kγ is a class 1B PI3K that is composed of a p110 catalytic subunit and a p101 or p84 regulatory subunit, whereas PI3Kα, β, and δ are class 1A enzymes composed of p110 and p85 subunits.{14518} AS-604850 is a selective, ATP-competitive inhibitor of PI3Kγ with IC50 values of 0.25, >20, >20, and 4.5 µM for the human recombinant γ, δ, β, and α isoforms, respectively.{13338} AS-604850 inhibited MCP-1-mediated monocyte chemotaxis with an IC50 value of 21 µM and reduced RANTES-induced peritoneal neutrophil recruitment in a murine model of leukocyte chemotaxis with an ED50 value of 42.4 mg/kg.{13338}  

     

    Brand:
    Cayman
    SKU:10010175 - 5 mg

    Available on backorder

  • Phosphatidylinositol 3-kinase (PI3K) catalyzes the phosphorylation of phosphatidylinositol at the three position to produce the second messengers PtdIns-(3,4)-P2 and PtdIns-(3,4,5)-P3.{8039,12235,13740} PI3Kγ is a class 1B PI3K that is composed of a p110 catalytic subunit and a p101 or p84 regulatory subunit, whereas PI3Kα, β, and δ are class 1A enzymes composed of p110 and p85 subunits{14518} AS-605240 is an orally active inhibitor of PI3-kinase γ that suppresses joint inflammation in mouse models of rheumatoid arthritis.{13338} It inhibits human recombinant PI3Kγ, α, β, and δ in an ATP-competitive manner with IC50 values of 8, 60, 270, and 300 nM, respectively.{13338} AS-605240 inhibits C5a-mediated phosphorylation of protein kinase B in RAW 264 cells with an IC50 value of 90 nM. In vivo, AS-605240 reduced RANTES-induced peritoneal neutrophil recruitment in a mouse model of leukocyte chemotaxis with an ED50 value of 9.1 mg/kg.  

     

    Brand:
    Cayman
    SKU:10007707 - 1 mg

    Available on backorder

  • Phosphatidylinositol 3-kinase (PI3K) catalyzes the phosphorylation of phosphatidylinositol at the three position to produce the second messengers PtdIns-(3,4)-P2 and PtdIns-(3,4,5)-P3.{8039,12235,13740} PI3Kγ is a class 1B PI3K that is composed of a p110 catalytic subunit and a p101 or p84 regulatory subunit, whereas PI3Kα, β, and δ are class 1A enzymes composed of p110 and p85 subunits{14518} AS-605240 is an orally active inhibitor of PI3-kinase γ that suppresses joint inflammation in mouse models of rheumatoid arthritis.{13338} It inhibits human recombinant PI3Kγ, α, β, and δ in an ATP-competitive manner with IC50 values of 8, 60, 270, and 300 nM, respectively.{13338} AS-605240 inhibits C5a-mediated phosphorylation of protein kinase B in RAW 264 cells with an IC50 value of 90 nM. In vivo, AS-605240 reduced RANTES-induced peritoneal neutrophil recruitment in a mouse model of leukocyte chemotaxis with an ED50 value of 9.1 mg/kg.  

     

    Brand:
    Cayman
    SKU:10007707 - 10 mg

    Available on backorder

  • Phosphatidylinositol 3-kinase (PI3K) catalyzes the phosphorylation of phosphatidylinositol at the three position to produce the second messengers PtdIns-(3,4)-P2 and PtdIns-(3,4,5)-P3.{8039,12235,13740} PI3Kγ is a class 1B PI3K that is composed of a p110 catalytic subunit and a p101 or p84 regulatory subunit, whereas PI3Kα, β, and δ are class 1A enzymes composed of p110 and p85 subunits{14518} AS-605240 is an orally active inhibitor of PI3-kinase γ that suppresses joint inflammation in mouse models of rheumatoid arthritis.{13338} It inhibits human recombinant PI3Kγ, α, β, and δ in an ATP-competitive manner with IC50 values of 8, 60, 270, and 300 nM, respectively.{13338} AS-605240 inhibits C5a-mediated phosphorylation of protein kinase B in RAW 264 cells with an IC50 value of 90 nM. In vivo, AS-605240 reduced RANTES-induced peritoneal neutrophil recruitment in a mouse model of leukocyte chemotaxis with an ED50 value of 9.1 mg/kg.  

     

    Brand:
    Cayman
    SKU:10007707 - 25 mg

    Available on backorder

  • Phosphatidylinositol 3-kinase (PI3K) catalyzes the phosphorylation of phosphatidylinositol at the three position to produce the second messengers PtdIns-(3,4)-P2 and PtdIns-(3,4,5)-P3.{8039,12235,13740} PI3Kγ is a class 1B PI3K that is composed of a p110 catalytic subunit and a p101 or p84 regulatory subunit, whereas PI3Kα, β, and δ are class 1A enzymes composed of p110 and p85 subunits{14518} AS-605240 is an orally active inhibitor of PI3-kinase γ that suppresses joint inflammation in mouse models of rheumatoid arthritis.{13338} It inhibits human recombinant PI3Kγ, α, β, and δ in an ATP-competitive manner with IC50 values of 8, 60, 270, and 300 nM, respectively.{13338} AS-605240 inhibits C5a-mediated phosphorylation of protein kinase B in RAW 264 cells with an IC50 value of 90 nM. In vivo, AS-605240 reduced RANTES-induced peritoneal neutrophil recruitment in a mouse model of leukocyte chemotaxis with an ED50 value of 9.1 mg/kg.  

     

    Brand:
    Cayman
    SKU:10007707 - 5 mg

    Available on backorder

  • The mitogen-activated protein kinases, MEK1 and 2, are dual-specificity threonine/tyrosine kinases that play key roles in the activation of the Ras-Raf-MEK-ERK pathway and are often upregulated in a variety of cancer cell types.{15629} AS-703026 is an orally bioavailable small molecule that selectively binds to and inhibits MEK1/2, preventing the activation of downstream effector proteins and transcription factors. It potently inhibits growth and survival of human INA-6 multiple myeloma cells and cytokine-induced osteoclast differentiation with IC50 values of 10 and 18.2 nM, respectively.{20674} In mice bearing H929 MM xenograft tumors, 30 mg/kg AS-703026 reduced tumor growth significantly, which correlated with downregulated ERK1/2 activity, induced PARP cleavage, and decreased microvessels in vivo.{20674} At 10 μM, AS-703026 supressed proliferation and transformation of K-Ras mutated colorectal cancer cells resistant to EGFR antibody therapy.{20673}  

     

    Brand:
    Cayman
    SKU:11226 - 1 mg

    Available on backorder

  • The mitogen-activated protein kinases, MEK1 and 2, are dual-specificity threonine/tyrosine kinases that play key roles in the activation of the Ras-Raf-MEK-ERK pathway and are often upregulated in a variety of cancer cell types.{15629} AS-703026 is an orally bioavailable small molecule that selectively binds to and inhibits MEK1/2, preventing the activation of downstream effector proteins and transcription factors. It potently inhibits growth and survival of human INA-6 multiple myeloma cells and cytokine-induced osteoclast differentiation with IC50 values of 10 and 18.2 nM, respectively.{20674} In mice bearing H929 MM xenograft tumors, 30 mg/kg AS-703026 reduced tumor growth significantly, which correlated with downregulated ERK1/2 activity, induced PARP cleavage, and decreased microvessels in vivo.{20674} At 10 μM, AS-703026 supressed proliferation and transformation of K-Ras mutated colorectal cancer cells resistant to EGFR antibody therapy.{20673}  

     

    Brand:
    Cayman
    SKU:11226 - 10 mg

    Available on backorder

  • The mitogen-activated protein kinases, MEK1 and 2, are dual-specificity threonine/tyrosine kinases that play key roles in the activation of the Ras-Raf-MEK-ERK pathway and are often upregulated in a variety of cancer cell types.{15629} AS-703026 is an orally bioavailable small molecule that selectively binds to and inhibits MEK1/2, preventing the activation of downstream effector proteins and transcription factors. It potently inhibits growth and survival of human INA-6 multiple myeloma cells and cytokine-induced osteoclast differentiation with IC50 values of 10 and 18.2 nM, respectively.{20674} In mice bearing H929 MM xenograft tumors, 30 mg/kg AS-703026 reduced tumor growth significantly, which correlated with downregulated ERK1/2 activity, induced PARP cleavage, and decreased microvessels in vivo.{20674} At 10 μM, AS-703026 supressed proliferation and transformation of K-Ras mutated colorectal cancer cells resistant to EGFR antibody therapy.{20673}  

     

    Brand:
    Cayman
    SKU:11226 - 25 mg

    Available on backorder

  • The mitogen-activated protein kinases, MEK1 and 2, are dual-specificity threonine/tyrosine kinases that play key roles in the activation of the Ras-Raf-MEK-ERK pathway and are often upregulated in a variety of cancer cell types.{15629} AS-703026 is an orally bioavailable small molecule that selectively binds to and inhibits MEK1/2, preventing the activation of downstream effector proteins and transcription factors. It potently inhibits growth and survival of human INA-6 multiple myeloma cells and cytokine-induced osteoclast differentiation with IC50 values of 10 and 18.2 nM, respectively.{20674} In mice bearing H929 MM xenograft tumors, 30 mg/kg AS-703026 reduced tumor growth significantly, which correlated with downregulated ERK1/2 activity, induced PARP cleavage, and decreased microvessels in vivo.{20674} At 10 μM, AS-703026 supressed proliferation and transformation of K-Ras mutated colorectal cancer cells resistant to EGFR antibody therapy.{20673}  

     

    Brand:
    Cayman
    SKU:11226 - 5 mg

    Available on backorder

  • AS-8351 is a histone demethylase inhibitor. It has been used in combination with CHIR99021 (Item No. 13122), A 83-01 (Item No. 9001799), BIX01294 (Item No. 13124), SC-1 (Item No. 10009557), Y-27632 (Item No. 10005583), OAC2 (Item No. 14103), SU 16f (Item No. 19555), and JNJ-10198409 (Item No. 10008131) to induce reprogramming of human fetal lung fibroblasts into functional cardiomyocytes.{31142}  

     

    Brand:
    Cayman
    SKU:20811 -

    Available on backorder

  • AS-8351 is a histone demethylase inhibitor. It has been used in combination with CHIR99021 (Item No. 13122), A 83-01 (Item No. 9001799), BIX01294 (Item No. 13124), SC-1 (Item No. 10009557), Y-27632 (Item No. 10005583), OAC2 (Item No. 14103), SU 16f (Item No. 19555), and JNJ-10198409 (Item No. 10008131) to induce reprogramming of human fetal lung fibroblasts into functional cardiomyocytes.{31142}  

     

    Brand:
    Cayman
    SKU:20811 -

    Available on backorder