Chemicals

Showing 35101–35250 of 41137 results

  • Smoothened (SMO) is a GPCR-like receptor which, with Patched, mediates hedgehog signaling to regulate gene expression through the Gli transcription factors.{21774} SANT 1 is a potent inhibitor of hedgehog signaling that acts by directly antagonizing SMO (IC50 = 20 nM).{21771} It counteracts SMO activation by the SMO agonist SAG but only partially competes with SAG binding to SMO.{21771,24191} SANT 1 targets inactive SMO while it is in the cytoplasm, before it relocates to the primary cilium and is activated.{22122} Through antagonism of SMO, SANT 1 represses Gli-mediated transcription in a variety of cell types.{22122,24193}  

     

    Brand:
    Cayman
    SKU:-
  • Smoothened (SMO) is a GPCR-like receptor which, with Patched, mediates hedgehog signaling to regulate gene expression through the Gli transcription factors.{21774} SANT 1 is a potent inhibitor of hedgehog signaling that acts by directly antagonizing SMO (IC50 = 20 nM).{21771} It counteracts SMO activation by the SMO agonist SAG but only partially competes with SAG binding to SMO.{21771,24191} SANT 1 targets inactive SMO while it is in the cytoplasm, before it relocates to the primary cilium and is activated.{22122} Through antagonism of SMO, SANT 1 represses Gli-mediated transcription in a variety of cell types.{22122,24193}  

     

    Brand:
    Cayman
    SKU:-
  • Smoothened (SMO) is a GPCR-like receptor which, with Patched, mediates hedgehog signaling to regulate gene expression through the Gli transcription factors.{21774} SANT 1 is a potent inhibitor of hedgehog signaling that acts by directly antagonizing SMO (IC50 = 20 nM).{21771} It counteracts SMO activation by the SMO agonist SAG but only partially competes with SAG binding to SMO.{21771,24191} SANT 1 targets inactive SMO while it is in the cytoplasm, before it relocates to the primary cilium and is activated.{22122} Through antagonism of SMO, SANT 1 represses Gli-mediated transcription in a variety of cell types.{22122,24193}  

     

    Brand:
    Cayman
    SKU:-
  • SANT-2 is a Smoothened (Smo) receptor antagonist.{21771,24191} It binds to the Smo receptor (Kd = 12 nM) and inhibits binding of the Smo receptor agonist SAG-1.3 (SAG; Item No. 11914) and antagonist cyclopamine (Item No. 11321) (Kis = 7.8 and 8.4 nM, respectively). SANT-2 inhibits hedgehog signaling induced by an N-terminal fragment of sonic hedgehog (Shh) in an Shh-LIGHT2 cellular assay (IC50 = 30 nM).{21771}  

     

    Brand:
    Cayman
    SKU:21208 -

    Out of stock

  • SANT-2 is a Smoothened (Smo) receptor antagonist.{21771,24191} It binds to the Smo receptor (Kd = 12 nM) and inhibits binding of the Smo receptor agonist SAG-1.3 (SAG; Item No. 11914) and antagonist cyclopamine (Item No. 11321) (Kis = 7.8 and 8.4 nM, respectively). SANT-2 inhibits hedgehog signaling induced by an N-terminal fragment of sonic hedgehog (Shh) in an Shh-LIGHT2 cellular assay (IC50 = 30 nM).{21771}  

     

    Brand:
    Cayman
    SKU:21208 -

    Out of stock

  • SANT-2 is a Smoothened (Smo) receptor antagonist.{21771,24191} It binds to the Smo receptor (Kd = 12 nM) and inhibits binding of the Smo receptor agonist SAG-1.3 (SAG; Item No. 11914) and antagonist cyclopamine (Item No. 11321) (Kis = 7.8 and 8.4 nM, respectively). SANT-2 inhibits hedgehog signaling induced by an N-terminal fragment of sonic hedgehog (Shh) in an Shh-LIGHT2 cellular assay (IC50 = 30 nM).{21771}  

     

    Brand:
    Cayman
    SKU:21208 -

    Out of stock

  • SANT-2 is a Smoothened (Smo) receptor antagonist.{21771,24191} It binds to the Smo receptor (Kd = 12 nM) and inhibits binding of the Smo receptor agonist SAG-1.3 (SAG; Item No. 11914) and antagonist cyclopamine (Item No. 11321) (Kis = 7.8 and 8.4 nM, respectively). SANT-2 inhibits hedgehog signaling induced by an N-terminal fragment of sonic hedgehog (Shh) in an Shh-LIGHT2 cellular assay (IC50 = 30 nM).{21771}  

     

    Brand:
    Cayman
    SKU:21208 -

    Out of stock

  • Santonin is a sesquiterpenoid lactone that has been found in Artemisia.{48410} It has been used as a building block in the synthesis of terpenoids. Santonin is an anthelmintic that induces paralysis of A. lumbricoides.{48411}  

     

    Brand:
    Cayman
    SKU:27460 - 10 g

    Available on backorder

  • Santonin is a sesquiterpenoid lactone that has been found in Artemisia.{48410} It has been used as a building block in the synthesis of terpenoids. Santonin is an anthelmintic that induces paralysis of A. lumbricoides.{48411}  

     

    Brand:
    Cayman
    SKU:27460 - 5 g

    Available on backorder

  • Sappanone A is a homoisoflavonoid with diverse biological activities that has been isolated from the aerial parts of C. pulcherrima, the heartwood of C. sappan, and the stems of H. campechianum.{41699,41700,41701,41702,41703} In vitro, sappanone A inhibits 76.2, 59.2, 37.4, and 35.4% of FGFR1, KDR, c-Met, and c-Kit kinase activity, respectively, when used at a concentration of 10 μM.{41699} It also inhibits influenza viral neuraminidase (NA) with IC50 values of 0.7, 1.1, and 1 μM for H1N1, H3N2, and H9N2 influenza viral NAs, respectively.{41700} Sappanone A has antibacterial activity against Gram-positive B. subtilis, B. sphaericus, and S. aureus as well as Gram-negative K. aerogenes and C. violaceum.{41701} It also inhibits the growth of A. niger and C. albicans fungi. Sapannone A inhibits LPS-induced inflammatory responses in vitro and in vivo, reducing nitric oxide (NO), interleukin-6 (IL-6), and prostaglandin E2 (PGE2; Item No. 14010) production in RAW264.7 cells as well as LPS-induced mortality in mice.{41702} It also attenuates airway inflammation and mucus hypersecretion via activation of the Nrf2 signaling pathway in a mouse model of ovalbumin-induced asthma.{41703}  

     

    Brand:
    Cayman
    SKU:23205 - 10 mg

    Available on backorder

  • Sappanone A is a homoisoflavonoid with diverse biological activities that has been isolated from the aerial parts of C. pulcherrima, the heartwood of C. sappan, and the stems of H. campechianum.{41699,41700,41701,41702,41703} In vitro, sappanone A inhibits 76.2, 59.2, 37.4, and 35.4% of FGFR1, KDR, c-Met, and c-Kit kinase activity, respectively, when used at a concentration of 10 μM.{41699} It also inhibits influenza viral neuraminidase (NA) with IC50 values of 0.7, 1.1, and 1 μM for H1N1, H3N2, and H9N2 influenza viral NAs, respectively.{41700} Sappanone A has antibacterial activity against Gram-positive B. subtilis, B. sphaericus, and S. aureus as well as Gram-negative K. aerogenes and C. violaceum.{41701} It also inhibits the growth of A. niger and C. albicans fungi. Sapannone A inhibits LPS-induced inflammatory responses in vitro and in vivo, reducing nitric oxide (NO), interleukin-6 (IL-6), and prostaglandin E2 (PGE2; Item No. 14010) production in RAW264.7 cells as well as LPS-induced mortality in mice.{41702} It also attenuates airway inflammation and mucus hypersecretion via activation of the Nrf2 signaling pathway in a mouse model of ovalbumin-induced asthma.{41703}  

     

    Brand:
    Cayman
    SKU:23205 - 25 mg

    Available on backorder

  • Sappanone A is a homoisoflavonoid with diverse biological activities that has been isolated from the aerial parts of C. pulcherrima, the heartwood of C. sappan, and the stems of H. campechianum.{41699,41700,41701,41702,41703} In vitro, sappanone A inhibits 76.2, 59.2, 37.4, and 35.4% of FGFR1, KDR, c-Met, and c-Kit kinase activity, respectively, when used at a concentration of 10 μM.{41699} It also inhibits influenza viral neuraminidase (NA) with IC50 values of 0.7, 1.1, and 1 μM for H1N1, H3N2, and H9N2 influenza viral NAs, respectively.{41700} Sappanone A has antibacterial activity against Gram-positive B. subtilis, B. sphaericus, and S. aureus as well as Gram-negative K. aerogenes and C. violaceum.{41701} It also inhibits the growth of A. niger and C. albicans fungi. Sapannone A inhibits LPS-induced inflammatory responses in vitro and in vivo, reducing nitric oxide (NO), interleukin-6 (IL-6), and prostaglandin E2 (PGE2; Item No. 14010) production in RAW264.7 cells as well as LPS-induced mortality in mice.{41702} It also attenuates airway inflammation and mucus hypersecretion via activation of the Nrf2 signaling pathway in a mouse model of ovalbumin-induced asthma.{41703}  

     

    Brand:
    Cayman
    SKU:23205 - 5 mg

    Available on backorder

  • Sappanone A is a homoisoflavonoid with diverse biological activities that has been isolated from the aerial parts of C. pulcherrima, the heartwood of C. sappan, and the stems of H. campechianum.{41699,41700,41701,41702,41703} In vitro, sappanone A inhibits 76.2, 59.2, 37.4, and 35.4% of FGFR1, KDR, c-Met, and c-Kit kinase activity, respectively, when used at a concentration of 10 μM.{41699} It also inhibits influenza viral neuraminidase (NA) with IC50 values of 0.7, 1.1, and 1 μM for H1N1, H3N2, and H9N2 influenza viral NAs, respectively.{41700} Sappanone A has antibacterial activity against Gram-positive B. subtilis, B. sphaericus, and S. aureus as well as Gram-negative K. aerogenes and C. violaceum.{41701} It also inhibits the growth of A. niger and C. albicans fungi. Sapannone A inhibits LPS-induced inflammatory responses in vitro and in vivo, reducing nitric oxide (NO), interleukin-6 (IL-6), and prostaglandin E2 (PGE2; Item No. 14010) production in RAW264.7 cells as well as LPS-induced mortality in mice.{41702} It also attenuates airway inflammation and mucus hypersecretion via activation of the Nrf2 signaling pathway in a mouse model of ovalbumin-induced asthma.{41703}  

     

    Brand:
    Cayman
    SKU:23205 - 50 mg

    Available on backorder

  • Saquinavir is an HIV protease inhibitor (Kis = 0.12 and 1 and HIV-2 protease, respectively) that exhibits antiviral activity with low cytotoxicity.{25841,25842} When co-administered with 50 mg/kg ritonavir (Item No. 13872), the bioavailability of 20 mg/kg saquinavir has been shown to increase 325-fold in mice through a mechanism that inhibits its metabolism by CYP3A.{25840}  

     

    Brand:
    Cayman
    SKU:9001893 - 10 mg

    Available on backorder

  • Saquinavir is an HIV protease inhibitor (Kis = 0.12 and 1 and HIV-2 protease, respectively) that exhibits antiviral activity with low cytotoxicity.{25841,25842} When co-administered with 50 mg/kg ritonavir (Item No. 13872), the bioavailability of 20 mg/kg saquinavir has been shown to increase 325-fold in mice through a mechanism that inhibits its metabolism by CYP3A.{25840}  

     

    Brand:
    Cayman
    SKU:9001893 - 25 mg

    Available on backorder

  • Saquinavir is an HIV protease inhibitor (Kis = 0.12 and 1 and HIV-2 protease, respectively) that exhibits antiviral activity with low cytotoxicity.{25841,25842} When co-administered with 50 mg/kg ritonavir (Item No. 13872), the bioavailability of 20 mg/kg saquinavir has been shown to increase 325-fold in mice through a mechanism that inhibits its metabolism by CYP3A.{25840}  

     

    Brand:
    Cayman
    SKU:9001893 - 5 mg

    Available on backorder

  • Saquinavir is an HIV protease inhibitor (Kis = 0.12 and 1 and HIV-2 protease, respectively) that exhibits antiviral activity with low cytotoxicity.{25841,25842} When co-administered with 50 mg/kg ritonavir (Item No. 13872), the bioavailability of 20 mg/kg saquinavir has been shown to increase 325-fold in mice through a mechanism that inhibits its metabolism by CYP3A.{25840}  

     

    Brand:
    Cayman
    SKU:9001893 - 50 mg

    Available on backorder

  • Sauinavir-d9 is intended for use as an internal standard for the quantification of saquinavir (Item No. 9001893) by GC- or LC-MS. Saquinavir is an HIV protease inhibitor (Kis = 0.12 and 13872), the bioavailability of saquinavir (20 mg/kg) has been shown to increase 325-fold in mice through a mechanism that inhibits its metabolism by CYP3A.{25840}  

     

    Brand:
    Cayman
    SKU:28906 - 1 mg

    Available on backorder

  • SAR131675 is an ATP-competitive inhibitor of VEGF receptor 3 (VEGFR3) with an IC50 value of 23 nM for the human recombinant receptor in a cell-free assay.{46458} It is selective for VEGFR3 over VEGFR2 and VEGFR1 (IC50s = 230 and >3,000 nM, respectively). SAR131675 inhibits survival of human lymphatic cells cultured with the VEGFR3-specific ligands VEGF-C and VEGF-D over the non-specific ligand VEGF-A in vitro (IC50s = 14, 17, and 664 nM, respectively). It decreases VEGF-C and VEGF-A-induced migration of human microvascular endothelial cells (HMVECs) when used at concentrations of 100 and 300 nM. SAR131675 (100 mg/kg) reduces tumor size, decreases the number of pancreatic angiogenic islets, and increases survival in the RIP1-Tag2 transgenic mouse model of pancreatic neuroendocrine tumors. It also decreases tumor size, levels of VEGFR3 in mammary tumor lysates, number of tumor-associated macrophages in mammary tumors, and the number of lung metastases in a 4T1 mouse allograft model when administered at a dose of 100 mg/kg.  

     

    Brand:
    Cayman
    SKU:28385 - 1 mg

    Available on backorder

  • SAR131675 is an ATP-competitive inhibitor of VEGF receptor 3 (VEGFR3) with an IC50 value of 23 nM for the human recombinant receptor in a cell-free assay.{46458} It is selective for VEGFR3 over VEGFR2 and VEGFR1 (IC50s = 230 and >3,000 nM, respectively). SAR131675 inhibits survival of human lymphatic cells cultured with the VEGFR3-specific ligands VEGF-C and VEGF-D over the non-specific ligand VEGF-A in vitro (IC50s = 14, 17, and 664 nM, respectively). It decreases VEGF-C and VEGF-A-induced migration of human microvascular endothelial cells (HMVECs) when used at concentrations of 100 and 300 nM. SAR131675 (100 mg/kg) reduces tumor size, decreases the number of pancreatic angiogenic islets, and increases survival in the RIP1-Tag2 transgenic mouse model of pancreatic neuroendocrine tumors. It also decreases tumor size, levels of VEGFR3 in mammary tumor lysates, number of tumor-associated macrophages in mammary tumors, and the number of lung metastases in a 4T1 mouse allograft model when administered at a dose of 100 mg/kg.  

     

    Brand:
    Cayman
    SKU:28385 - 10 mg

    Available on backorder

  • SAR131675 is an ATP-competitive inhibitor of VEGF receptor 3 (VEGFR3) with an IC50 value of 23 nM for the human recombinant receptor in a cell-free assay.{46458} It is selective for VEGFR3 over VEGFR2 and VEGFR1 (IC50s = 230 and >3,000 nM, respectively). SAR131675 inhibits survival of human lymphatic cells cultured with the VEGFR3-specific ligands VEGF-C and VEGF-D over the non-specific ligand VEGF-A in vitro (IC50s = 14, 17, and 664 nM, respectively). It decreases VEGF-C and VEGF-A-induced migration of human microvascular endothelial cells (HMVECs) when used at concentrations of 100 and 300 nM. SAR131675 (100 mg/kg) reduces tumor size, decreases the number of pancreatic angiogenic islets, and increases survival in the RIP1-Tag2 transgenic mouse model of pancreatic neuroendocrine tumors. It also decreases tumor size, levels of VEGFR3 in mammary tumor lysates, number of tumor-associated macrophages in mammary tumors, and the number of lung metastases in a 4T1 mouse allograft model when administered at a dose of 100 mg/kg.  

     

    Brand:
    Cayman
    SKU:28385 - 25 mg

    Available on backorder

  • SAR131675 is an ATP-competitive inhibitor of VEGF receptor 3 (VEGFR3) with an IC50 value of 23 nM for the human recombinant receptor in a cell-free assay.{46458} It is selective for VEGFR3 over VEGFR2 and VEGFR1 (IC50s = 230 and >3,000 nM, respectively). SAR131675 inhibits survival of human lymphatic cells cultured with the VEGFR3-specific ligands VEGF-C and VEGF-D over the non-specific ligand VEGF-A in vitro (IC50s = 14, 17, and 664 nM, respectively). It decreases VEGF-C and VEGF-A-induced migration of human microvascular endothelial cells (HMVECs) when used at concentrations of 100 and 300 nM. SAR131675 (100 mg/kg) reduces tumor size, decreases the number of pancreatic angiogenic islets, and increases survival in the RIP1-Tag2 transgenic mouse model of pancreatic neuroendocrine tumors. It also decreases tumor size, levels of VEGFR3 in mammary tumor lysates, number of tumor-associated macrophages in mammary tumors, and the number of lung metastases in a 4T1 mouse allograft model when administered at a dose of 100 mg/kg.  

     

    Brand:
    Cayman
    SKU:28385 - 5 mg

    Available on backorder

  • SAR20347 is an inhibitor of the JAK family kinases TYK2 and JAK1-3 (IC50s = 0.6, 23, 26, and 41 nM, respectively, in cell-free assays).{52137} It inhibits IL-12-induced TYK2-dependent phosphorylation of STAT4 in NK-92 cells (IC50 = 126 nM) and IL-6-induced JAK1-dependent STAT3 signaling in TF-1 cells (IC50 = 345 nM). SAR20347 (5 μM) inhibits IL-12-induced INF-γ production and reporter gene activity in peripheral blood mononuclear cells (PBMCs). In vivo, SAR20347 (60 mg/kg) inhibits the production of serum IFN-γ in mice. SAR20347 also reduces keratinocyte activation and skin levels of IL-12, IL-23, IL-6, IL-22, and IFN-γ in a mouse model of psoriasis induced by imiquimod (Item No. 14956).  

     

    Brand:
    Cayman
    SKU:29248 - 1 mg

    Available on backorder

  • SAR20347 is an inhibitor of the JAK family kinases TYK2 and JAK1-3 (IC50s = 0.6, 23, 26, and 41 nM, respectively, in cell-free assays).{52137} It inhibits IL-12-induced TYK2-dependent phosphorylation of STAT4 in NK-92 cells (IC50 = 126 nM) and IL-6-induced JAK1-dependent STAT3 signaling in TF-1 cells (IC50 = 345 nM). SAR20347 (5 μM) inhibits IL-12-induced INF-γ production and reporter gene activity in peripheral blood mononuclear cells (PBMCs). In vivo, SAR20347 (60 mg/kg) inhibits the production of serum IFN-γ in mice. SAR20347 also reduces keratinocyte activation and skin levels of IL-12, IL-23, IL-6, IL-22, and IFN-γ in a mouse model of psoriasis induced by imiquimod (Item No. 14956).  

     

    Brand:
    Cayman
    SKU:29248 - 10 mg

    Available on backorder

  • SAR20347 is an inhibitor of the JAK family kinases TYK2 and JAK1-3 (IC50s = 0.6, 23, 26, and 41 nM, respectively, in cell-free assays).{52137} It inhibits IL-12-induced TYK2-dependent phosphorylation of STAT4 in NK-92 cells (IC50 = 126 nM) and IL-6-induced JAK1-dependent STAT3 signaling in TF-1 cells (IC50 = 345 nM). SAR20347 (5 μM) inhibits IL-12-induced INF-γ production and reporter gene activity in peripheral blood mononuclear cells (PBMCs). In vivo, SAR20347 (60 mg/kg) inhibits the production of serum IFN-γ in mice. SAR20347 also reduces keratinocyte activation and skin levels of IL-12, IL-23, IL-6, IL-22, and IFN-γ in a mouse model of psoriasis induced by imiquimod (Item No. 14956).  

     

    Brand:
    Cayman
    SKU:29248 - 25 mg

    Available on backorder

  • SAR20347 is an inhibitor of the JAK family kinases TYK2 and JAK1-3 (IC50s = 0.6, 23, 26, and 41 nM, respectively, in cell-free assays).{52137} It inhibits IL-12-induced TYK2-dependent phosphorylation of STAT4 in NK-92 cells (IC50 = 126 nM) and IL-6-induced JAK1-dependent STAT3 signaling in TF-1 cells (IC50 = 345 nM). SAR20347 (5 μM) inhibits IL-12-induced INF-γ production and reporter gene activity in peripheral blood mononuclear cells (PBMCs). In vivo, SAR20347 (60 mg/kg) inhibits the production of serum IFN-γ in mice. SAR20347 also reduces keratinocyte activation and skin levels of IL-12, IL-23, IL-6, IL-22, and IFN-γ in a mouse model of psoriasis induced by imiquimod (Item No. 14956).  

     

    Brand:
    Cayman
    SKU:29248 - 5 mg

    Available on backorder

  • SAR260301 is an inhibitor of phosphatidylinositol 3-kinase (PI3K) isoform β (IC50 = 52 nM).{34311} It is selective for p110β over other PI3K isoforms.{34311} SAR260301 demonstrates significant in vivo activity in a UACC-62 xenograft model in mice.{34311} It has synergistic antitumor activity when combined with the BRAF inhibitor vemurafenib (PLX4032; Item No. 10618) or the MEK inhibitor selumetinib (AZD 6244; Item No. 11599) in PTEN-deficient/BRAF-mutated human melanoma tumor models.{34310}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • SAR260301 is an inhibitor of phosphatidylinositol 3-kinase (PI3K) isoform β (IC50 = 52 nM).{34311} It is selective for p110β over other PI3K isoforms.{34311} SAR260301 demonstrates significant in vivo activity in a UACC-62 xenograft model in mice.{34311} It has synergistic antitumor activity when combined with the BRAF inhibitor vemurafenib (PLX4032; Item No. 10618) or the MEK inhibitor selumetinib (AZD 6244; Item No. 11599) in PTEN-deficient/BRAF-mutated human melanoma tumor models.{34310}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • SAR260301 is an inhibitor of phosphatidylinositol 3-kinase (PI3K) isoform β (IC50 = 52 nM).{34311} It is selective for p110β over other PI3K isoforms.{34311} SAR260301 demonstrates significant in vivo activity in a UACC-62 xenograft model in mice.{34311} It has synergistic antitumor activity when combined with the BRAF inhibitor vemurafenib (PLX4032; Item No. 10618) or the MEK inhibitor selumetinib (AZD 6244; Item No. 11599) in PTEN-deficient/BRAF-mutated human melanoma tumor models.{34310}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • SAR260301 is an inhibitor of phosphatidylinositol 3-kinase (PI3K) isoform β (IC50 = 52 nM).{34311} It is selective for p110β over other PI3K isoforms.{34311} SAR260301 demonstrates significant in vivo activity in a UACC-62 xenograft model in mice.{34311} It has synergistic antitumor activity when combined with the BRAF inhibitor vemurafenib (PLX4032; Item No. 10618) or the MEK inhibitor selumetinib (AZD 6244; Item No. 11599) in PTEN-deficient/BRAF-mutated human melanoma tumor models.{34310}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • SAR405 is an inhibitor of the phosphoinositide 3-kinase (PI3K) class III isoform Vps34 (IC50 = 1.2 nM).{27429} It is without effect (IC50 > 10,000 nM) on other PI3K isoforms and mTOR. SAR405 alters vesicle trafficking and inhibits autophagy by blocking autophagosome formation.{27429} SAR405 also synergizes with the mTOR inhibitor everolimus (Item No. 11597) in preventing the proliferation of renal tumor cell lines.{27429}  

     

    Brand:
    Cayman
    SKU:-

    Out of stock

  • SAR405 is an inhibitor of the phosphoinositide 3-kinase (PI3K) class III isoform Vps34 (IC50 = 1.2 nM).{27429} It is without effect (IC50 > 10,000 nM) on other PI3K isoforms and mTOR. SAR405 alters vesicle trafficking and inhibits autophagy by blocking autophagosome formation.{27429} SAR405 also synergizes with the mTOR inhibitor everolimus (Item No. 11597) in preventing the proliferation of renal tumor cell lines.{27429}  

     

    Brand:
    Cayman
    SKU:-

    Out of stock

  • SAR405 is an inhibitor of the phosphoinositide 3-kinase (PI3K) class III isoform Vps34 (IC50 = 1.2 nM).{27429} It is without effect (IC50 > 10,000 nM) on other PI3K isoforms and mTOR. SAR405 alters vesicle trafficking and inhibits autophagy by blocking autophagosome formation.{27429} SAR405 also synergizes with the mTOR inhibitor everolimus (Item No. 11597) in preventing the proliferation of renal tumor cell lines.{27429}  

     

    Brand:
    Cayman
    SKU:-

    Out of stock

  • SAR407899 is an ATP-competitive inhibitor of the Rho-associated kinases ROCK-I and ROCK-II (IC50s = 102 and 276 nM, respectively at a concentration of 40 μM ATP).{37269} SAR407899 is selective for ROCK over 79 other kinases at IC50 values up to 10 μM but had IC50 values ranging from 1 to 10 μM for RSK, PKB, PKCδ, and MSK-1. It is also selective for ROCK over 115 receptor and enzyme targets at IC50 values up to 10 μM, but it does inhibit the serotonin transporter and µ-opioid receptors with IC50 values of 1.1 and 8.9 μM, respectively. In vitro, SAR407899 inhibits ROCK-mediated phosphorylation of myosin phosphatase (MYPT), thrombin-induced stress fiber formation, PDGF-induced proliferation, and monocyte chemotactic protein-1-stimulated chemotaxis. SAR407899 relaxes precontracted isolated arteries from various species (IC50s = 122-280 nM) and precontracted corpora cavernosa in both healthy and diabetic animals (IC50s = 0.05-0.42 μM).{37269},{37270} It inhibits constriction of rat and human arteries induced by endothelin-1 (ET-1; Emaxs = 24-83% of control).{37271}  

     

    Brand:
    Cayman
    SKU:21717 -

    Out of stock

  • SAR407899 is an ATP-competitive inhibitor of the Rho-associated kinases ROCK-I and ROCK-II (IC50s = 102 and 276 nM, respectively at a concentration of 40 μM ATP).{37269} SAR407899 is selective for ROCK over 79 other kinases at IC50 values up to 10 μM but had IC50 values ranging from 1 to 10 μM for RSK, PKB, PKCδ, and MSK-1. It is also selective for ROCK over 115 receptor and enzyme targets at IC50 values up to 10 μM, but it does inhibit the serotonin transporter and µ-opioid receptors with IC50 values of 1.1 and 8.9 μM, respectively. In vitro, SAR407899 inhibits ROCK-mediated phosphorylation of myosin phosphatase (MYPT), thrombin-induced stress fiber formation, PDGF-induced proliferation, and monocyte chemotactic protein-1-stimulated chemotaxis. SAR407899 relaxes precontracted isolated arteries from various species (IC50s = 122-280 nM) and precontracted corpora cavernosa in both healthy and diabetic animals (IC50s = 0.05-0.42 μM).{37269},{37270} It inhibits constriction of rat and human arteries induced by endothelin-1 (ET-1; Emaxs = 24-83% of control).{37271}  

     

    Brand:
    Cayman
    SKU:21717 -

    Out of stock

  • SAR407899 is an ATP-competitive inhibitor of the Rho-associated kinases ROCK-I and ROCK-II (IC50s = 102 and 276 nM, respectively at a concentration of 40 μM ATP).{37269} SAR407899 is selective for ROCK over 79 other kinases at IC50 values up to 10 μM but had IC50 values ranging from 1 to 10 μM for RSK, PKB, PKCδ, and MSK-1. It is also selective for ROCK over 115 receptor and enzyme targets at IC50 values up to 10 μM, but it does inhibit the serotonin transporter and µ-opioid receptors with IC50 values of 1.1 and 8.9 μM, respectively. In vitro, SAR407899 inhibits ROCK-mediated phosphorylation of myosin phosphatase (MYPT), thrombin-induced stress fiber formation, PDGF-induced proliferation, and monocyte chemotactic protein-1-stimulated chemotaxis. SAR407899 relaxes precontracted isolated arteries from various species (IC50s = 122-280 nM) and precontracted corpora cavernosa in both healthy and diabetic animals (IC50s = 0.05-0.42 μM).{37269},{37270} It inhibits constriction of rat and human arteries induced by endothelin-1 (ET-1; Emaxs = 24-83% of control).{37271}  

     

    Brand:
    Cayman
    SKU:21717 -

    Out of stock

  • SAR407899 is an ATP-competitive inhibitor of the Rho-associated kinases ROCK-I and ROCK-II (IC50s = 102 and 276 nM, respectively at a concentration of 40 μM ATP).{37269} SAR407899 is selective for ROCK over 79 other kinases at IC50 values up to 10 μM but had IC50 values ranging from 1 to 10 μM for RSK, PKB, PKCδ, and MSK-1. It is also selective for ROCK over 115 receptor and enzyme targets at IC50 values up to 10 μM, but it does inhibit the serotonin transporter and µ-opioid receptors with IC50 values of 1.1 and 8.9 μM, respectively. In vitro, SAR407899 inhibits ROCK-mediated phosphorylation of myosin phosphatase (MYPT), thrombin-induced stress fiber formation, PDGF-induced proliferation, and monocyte chemotactic protein-1-stimulated chemotaxis. SAR407899 relaxes precontracted isolated arteries from various species (IC50s = 122-280 nM) and precontracted corpora cavernosa in both healthy and diabetic animals (IC50s = 0.05-0.42 μM).{37269},{37270} It inhibits constriction of rat and human arteries induced by endothelin-1 (ET-1; Emaxs = 24-83% of control).{37271}  

     

    Brand:
    Cayman
    SKU:21717 -

    Out of stock

  • SAR7334 is a transient receptor potential canonical 6 (TRPC6) channel blocker (IC50 = 7.9 nM).{47571} It is selective for TRPC6 over TRPC4 and TRPC5 (IC50s = 282 and 226 nM, respectively). SAR7334 (0.2-1 μM) blocks TRPC6-dependent hypoxia-induced vasoconstriction in isolated perfused and ventilated mouse lung. It also inhibits oxidative stress-induced apoptosis and increases autophagic flux in primary mouse renal proximal tubule cells.{47572}  

     

    Brand:
    Cayman
    SKU:28292 - 1 mg

    Available on backorder

  • SAR7334 is a transient receptor potential canonical 6 (TRPC6) channel blocker (IC50 = 7.9 nM).{47571} It is selective for TRPC6 over TRPC4 and TRPC5 (IC50s = 282 and 226 nM, respectively). SAR7334 (0.2-1 μM) blocks TRPC6-dependent hypoxia-induced vasoconstriction in isolated perfused and ventilated mouse lung. It also inhibits oxidative stress-induced apoptosis and increases autophagic flux in primary mouse renal proximal tubule cells.{47572}  

     

    Brand:
    Cayman
    SKU:28292 - 5 mg

    Available on backorder

  • SAR7334 is a transient receptor potential canonical 6 (TRPC6) channel blocker (IC50 = 7.9 nM).{47571} It is selective for TRPC6 over TRPC4 and TRPC5 (IC50s = 282 and 226 nM, respectively). SAR7334 (0.2-1 μM) blocks TRPC6-dependent hypoxia-induced vasoconstriction in isolated perfused and ventilated mouse lung. It also inhibits oxidative stress-induced apoptosis and increases autophagic flux in primary mouse renal proximal tubule cells.{47572}  

     

    Brand:
    Cayman
    SKU:28292 - 500 µg

    Available on backorder

  • Saracatinib is a dual inhibitor of the tyrosine kinases c-Src and Abl (IC50 = 2.7 and 30 nM, respectively).{24595} It less effectively inhibits other receptor and non-receptor tyrosine kinases as well as assorted serine/threonine kinases.{24595,24597,24594} Saracatinib is orally available and blocks cell motility, migration, adhesion, invasion, proliferation, differentiation, and survival.{24595,24597,24598} Through its effects on c-Src, it reduces osteoclast bone resorption.{24597} Saracatinib also blocks denque virus RNA replication through its effect on Fyn kinase.{24596}  

     

    Brand:
    Cayman
    SKU:11497 - 10 mg

    Available on backorder

  • Saracatinib is a dual inhibitor of the tyrosine kinases c-Src and Abl (IC50 = 2.7 and 30 nM, respectively).{24595} It less effectively inhibits other receptor and non-receptor tyrosine kinases as well as assorted serine/threonine kinases.{24595,24597,24594} Saracatinib is orally available and blocks cell motility, migration, adhesion, invasion, proliferation, differentiation, and survival.{24595,24597,24598} Through its effects on c-Src, it reduces osteoclast bone resorption.{24597} Saracatinib also blocks denque virus RNA replication through its effect on Fyn kinase.{24596}  

     

    Brand:
    Cayman
    SKU:11497 - 25 mg

    Available on backorder

  • Saracatinib is a dual inhibitor of the tyrosine kinases c-Src and Abl (IC50 = 2.7 and 30 nM, respectively).{24595} It less effectively inhibits other receptor and non-receptor tyrosine kinases as well as assorted serine/threonine kinases.{24595,24597,24594} Saracatinib is orally available and blocks cell motility, migration, adhesion, invasion, proliferation, differentiation, and survival.{24595,24597,24598} Through its effects on c-Src, it reduces osteoclast bone resorption.{24597} Saracatinib also blocks denque virus RNA replication through its effect on Fyn kinase.{24596}  

     

    Brand:
    Cayman
    SKU:11497 - 5 mg

    Available on backorder

  • Saracatinib is a dual inhibitor of the tyrosine kinases c-Src and Abl (IC50 = 2.7 and 30 nM, respectively).{24595} It less effectively inhibits other receptor and non-receptor tyrosine kinases as well as assorted serine/threonine kinases.{24595,24597,24594} Saracatinib is orally available and blocks cell motility, migration, adhesion, invasion, proliferation, differentiation, and survival.{24595,24597,24598} Through its effects on c-Src, it reduces osteoclast bone resorption.{24597} Saracatinib also blocks denque virus RNA replication through its effect on Fyn kinase.{24596}  

     

    Brand:
    Cayman
    SKU:11497 - 50 mg

    Available on backorder

  • Sarcosine is an intermediate in the biosynthesis of glycine from choline.{48332} It is a selective inhibitor of glycine transporter 1 (GlyT1) with IC50 values of 91 and greater than 1,000 µM for GlyT1 and GlyT2, respectively, in HEK293 cells expressing the human transporters.{48333} Sarcosine levels are increased in prostate cancer cell lines with an invasive phenotype compared with non-invasive cell lines.{48334} Sarcosine increases in a progressive fashion in prostate cancer with 0, 42, and 79% of benign, localized, and metastatic prostate tissue samples containing increased levels of sarcosine.  

     

    Brand:
    Cayman
    SKU:26799 - 100 g

    Available on backorder

  • Sarcosine is an intermediate in the biosynthesis of glycine from choline.{48332} It is a selective inhibitor of glycine transporter 1 (GlyT1) with IC50 values of 91 and greater than 1,000 µM for GlyT1 and GlyT2, respectively, in HEK293 cells expressing the human transporters.{48333} Sarcosine levels are increased in prostate cancer cell lines with an invasive phenotype compared with non-invasive cell lines.{48334} Sarcosine increases in a progressive fashion in prostate cancer with 0, 42, and 79% of benign, localized, and metastatic prostate tissue samples containing increased levels of sarcosine.  

     

    Brand:
    Cayman
    SKU:26799 - 250 g

    Available on backorder

  • Sarcosine is an intermediate in the biosynthesis of glycine from choline.{48332} It is a selective inhibitor of glycine transporter 1 (GlyT1) with IC50 values of 91 and greater than 1,000 µM for GlyT1 and GlyT2, respectively, in HEK293 cells expressing the human transporters.{48333} Sarcosine levels are increased in prostate cancer cell lines with an invasive phenotype compared with non-invasive cell lines.{48334} Sarcosine increases in a progressive fashion in prostate cancer with 0, 42, and 79% of benign, localized, and metastatic prostate tissue samples containing increased levels of sarcosine.  

     

    Brand:
    Cayman
    SKU:26799 - 50 g

    Available on backorder

  • Saroglitazar is a dual agonist of PPARα and PPARγ (EC50s = 0.65 and 3,000 pM, respectively, in a transactivation assay in HepG2 cells).{49145} It decreases serum triglyceride, free fatty acid, and glucose levels in a db/db mouse model of diabetes when administered at doses ranging from 0.01 to 3 mg/kg per day for 12 days. It increases insulin sensitivity in an oral glucose challenge when administered at a dose of 1 mg/kg in db/db mice, as well as decreases LDL levels in hApoB100/hCETP mice and in hamsters fed a high-fat high-cholesterol diet. Saroglitazar (10 µM) reverses palmitic acid-induced decreases in the expression of superoxide dismutase 1 (SOD1), SOD2, glutathione peroxidase (GPX), and catalase and increases in TNF-α, IL-1β, and IL-6 expression in HepG2 cells.{49146} It decreases hepatic inflammation and steatosis in a mouse model of non-alcoholic steatohepatitis (NASH) induced by a choline-deficient high-fat diet when administered at a dose of 3 mg/kg and inhibits fibrosis in a mouse model of fibrosis induced by carbon tetrachloride.  

     

    Brand:
    Cayman
    SKU:27851 - 2.5 mg

    Available on backorder

  • Sarpogrelate is a selective antagonist of the serotonin (5-HT) receptor subtypes 5-HT2A, 5-HT2B, and 5-HT2C (Kis = 3.02, 269, and 37.2 nM, respectively, for human recombinant receptors expressed in CHO-K1 cells).{39654} It is selective for 5-HT2 (Ki = 70.8 nM) over 5-HT1 (Ki = >26,000 nM), α1-, α2-, and β-adrenergic (Kis = 640-123,800 nM), and muscarinic receptors (Ki = >40,000 nM).{39658} In vitro, it inhibits aggregation of rat whole blood induced by collagen, 5-HT (Item No. 14332) with collagen, and 5-HT with ADP (Item No. 16778; IC50s = 57.7, 0.56, and 22.7 μM, respectively).{39655} In vivo, it inhibits leukocyte-endothelial interactions in the femoral artery induced by a high-fat high-fructose diet (HFFD) in mice when administered at a dose of 5 mg/kg per day.{39656} Sarpogrelate (5 mg/kg per day) decreases ventricular hypertrophy and infarct size in a rat model of myocardial infarction.{39657}  

     

    Brand:
    Cayman
    SKU:24194 - 10 mg

    Available on backorder

  • Sarpogrelate is a selective antagonist of the serotonin (5-HT) receptor subtypes 5-HT2A, 5-HT2B, and 5-HT2C (Kis = 3.02, 269, and 37.2 nM, respectively, for human recombinant receptors expressed in CHO-K1 cells).{39654} It is selective for 5-HT2 (Ki = 70.8 nM) over 5-HT1 (Ki = >26,000 nM), α1-, α2-, and β-adrenergic (Kis = 640-123,800 nM), and muscarinic receptors (Ki = >40,000 nM).{39658} In vitro, it inhibits aggregation of rat whole blood induced by collagen, 5-HT (Item No. 14332) with collagen, and 5-HT with ADP (Item No. 16778; IC50s = 57.7, 0.56, and 22.7 μM, respectively).{39655} In vivo, it inhibits leukocyte-endothelial interactions in the femoral artery induced by a high-fat high-fructose diet (HFFD) in mice when administered at a dose of 5 mg/kg per day.{39656} Sarpogrelate (5 mg/kg per day) decreases ventricular hypertrophy and infarct size in a rat model of myocardial infarction.{39657}  

     

    Brand:
    Cayman
    SKU:24194 - 100 mg

    Available on backorder

  • Sarpogrelate is a selective antagonist of the serotonin (5-HT) receptor subtypes 5-HT2A, 5-HT2B, and 5-HT2C (Kis = 3.02, 269, and 37.2 nM, respectively, for human recombinant receptors expressed in CHO-K1 cells).{39654} It is selective for 5-HT2 (Ki = 70.8 nM) over 5-HT1 (Ki = >26,000 nM), α1-, α2-, and β-adrenergic (Kis = 640-123,800 nM), and muscarinic receptors (Ki = >40,000 nM).{39658} In vitro, it inhibits aggregation of rat whole blood induced by collagen, 5-HT (Item No. 14332) with collagen, and 5-HT with ADP (Item No. 16778; IC50s = 57.7, 0.56, and 22.7 μM, respectively).{39655} In vivo, it inhibits leukocyte-endothelial interactions in the femoral artery induced by a high-fat high-fructose diet (HFFD) in mice when administered at a dose of 5 mg/kg per day.{39656} Sarpogrelate (5 mg/kg per day) decreases ventricular hypertrophy and infarct size in a rat model of myocardial infarction.{39657}  

     

    Brand:
    Cayman
    SKU:24194 - 250 mg

    Available on backorder

  • Sarpogrelate is a selective antagonist of the serotonin (5-HT) receptor subtypes 5-HT2A, 5-HT2B, and 5-HT2C (Kis = 3.02, 269, and 37.2 nM, respectively, for human recombinant receptors expressed in CHO-K1 cells).{39654} It is selective for 5-HT2 (Ki = 70.8 nM) over 5-HT1 (Ki = >26,000 nM), α1-, α2-, and β-adrenergic (Kis = 640-123,800 nM), and muscarinic receptors (Ki = >40,000 nM).{39658} In vitro, it inhibits aggregation of rat whole blood induced by collagen, 5-HT (Item No. 14332) with collagen, and 5-HT with ADP (Item No. 16778; IC50s = 57.7, 0.56, and 22.7 μM, respectively).{39655} In vivo, it inhibits leukocyte-endothelial interactions in the femoral artery induced by a high-fat high-fructose diet (HFFD) in mice when administered at a dose of 5 mg/kg per day.{39656} Sarpogrelate (5 mg/kg per day) decreases ventricular hypertrophy and infarct size in a rat model of myocardial infarction.{39657}  

     

    Brand:
    Cayman
    SKU:24194 - 50 mg

    Available on backorder

  • Sarsasapogenin is a steroid sapogenin originally isolated from Smilax that has antiproliferative, pro-apoptotic, anti-inflammatory, neuroprotective, and antidepressant-like properties.{41855,41856,41857,36061,41858,41859} Sarsasapogenin inhibits proliferation of HeLa cervical, MCF-7 breast, HepG2 liver, A549 lung, A375.S2 melanoma, and HT-1080 fibrosarcoma cells (IC50s = 31.36-48.79 μM) and dose-dependently induces apoptosis of HeLa cells.{41856,41857} It also protects human SH-SY5Y neuroblastoma cells from hydrogen peroxide-induced death with a neuroprotective ratio of 27.3% when used at a concentration of 100 μM.{41858} In vivo, sarsasapogenin (10 mg/kg) reduces 2,3,4-trinitrobenzene sulfonic acid-induced colon shortening, myeloperoxidase activity, NF-κB activation, and IL-1β, TNF-α, and IL-6 levels in mice.{36061} It also increases the percentage of correct responses in the Y-maze test in aged rats when administered at a dose of 3.6 mg/kg per day.{41860} Sarsasapogenin (12.5 mg/kg per day) reduces the amount of time mice spend immobile in the forced swim test, indicating antidepressant-like behavior.{41859}  

     

    Brand:
    Cayman
    SKU:24973 - 100 mg

    Available on backorder

  • Sarsasapogenin is a steroid sapogenin originally isolated from Smilax that has antiproliferative, pro-apoptotic, anti-inflammatory, neuroprotective, and antidepressant-like properties.{41855,41856,41857,36061,41858,41859} Sarsasapogenin inhibits proliferation of HeLa cervical, MCF-7 breast, HepG2 liver, A549 lung, A375.S2 melanoma, and HT-1080 fibrosarcoma cells (IC50s = 31.36-48.79 μM) and dose-dependently induces apoptosis of HeLa cells.{41856,41857} It also protects human SH-SY5Y neuroblastoma cells from hydrogen peroxide-induced death with a neuroprotective ratio of 27.3% when used at a concentration of 100 μM.{41858} In vivo, sarsasapogenin (10 mg/kg) reduces 2,3,4-trinitrobenzene sulfonic acid-induced colon shortening, myeloperoxidase activity, NF-κB activation, and IL-1β, TNF-α, and IL-6 levels in mice.{36061} It also increases the percentage of correct responses in the Y-maze test in aged rats when administered at a dose of 3.6 mg/kg per day.{41860} Sarsasapogenin (12.5 mg/kg per day) reduces the amount of time mice spend immobile in the forced swim test, indicating antidepressant-like behavior.{41859}  

     

    Brand:
    Cayman
    SKU:24973 - 25 mg

    Available on backorder

  • Sarsasapogenin is a steroid sapogenin originally isolated from Smilax that has antiproliferative, pro-apoptotic, anti-inflammatory, neuroprotective, and antidepressant-like properties.{41855,41856,41857,36061,41858,41859} Sarsasapogenin inhibits proliferation of HeLa cervical, MCF-7 breast, HepG2 liver, A549 lung, A375.S2 melanoma, and HT-1080 fibrosarcoma cells (IC50s = 31.36-48.79 μM) and dose-dependently induces apoptosis of HeLa cells.{41856,41857} It also protects human SH-SY5Y neuroblastoma cells from hydrogen peroxide-induced death with a neuroprotective ratio of 27.3% when used at a concentration of 100 μM.{41858} In vivo, sarsasapogenin (10 mg/kg) reduces 2,3,4-trinitrobenzene sulfonic acid-induced colon shortening, myeloperoxidase activity, NF-κB activation, and IL-1β, TNF-α, and IL-6 levels in mice.{36061} It also increases the percentage of correct responses in the Y-maze test in aged rats when administered at a dose of 3.6 mg/kg per day.{41860} Sarsasapogenin (12.5 mg/kg per day) reduces the amount of time mice spend immobile in the forced swim test, indicating antidepressant-like behavior.{41859}  

     

    Brand:
    Cayman
    SKU:24973 - 250 mg

    Available on backorder

  • Sarsasapogenin is a steroid sapogenin originally isolated from Smilax that has antiproliferative, pro-apoptotic, anti-inflammatory, neuroprotective, and antidepressant-like properties.{41855,41856,41857,36061,41858,41859} Sarsasapogenin inhibits proliferation of HeLa cervical, MCF-7 breast, HepG2 liver, A549 lung, A375.S2 melanoma, and HT-1080 fibrosarcoma cells (IC50s = 31.36-48.79 μM) and dose-dependently induces apoptosis of HeLa cells.{41856,41857} It also protects human SH-SY5Y neuroblastoma cells from hydrogen peroxide-induced death with a neuroprotective ratio of 27.3% when used at a concentration of 100 μM.{41858} In vivo, sarsasapogenin (10 mg/kg) reduces 2,3,4-trinitrobenzene sulfonic acid-induced colon shortening, myeloperoxidase activity, NF-κB activation, and IL-1β, TNF-α, and IL-6 levels in mice.{36061} It also increases the percentage of correct responses in the Y-maze test in aged rats when administered at a dose of 3.6 mg/kg per day.{41860} Sarsasapogenin (12.5 mg/kg per day) reduces the amount of time mice spend immobile in the forced swim test, indicating antidepressant-like behavior.{41859}  

     

    Brand:
    Cayman
    SKU:24973 - 50 mg

    Available on backorder

  • Sartorypyrone A is a meroditerpene metabolite produced by Neosartorya fungal species.{41303} It inhibits the growth of MCF-7 breast, NCI-H460 lung, and A375-C5 melanoma cancer cell lines (GI50s = 46.3, 37.3, and 21.5 μM, respectively). Sartorypyrone A inhibits growth of Gram-positive bacteria, including multidrug-resistant S. aureus (MIC = 32 μg/ml), and reduces the mass of S. aureus and B. subtilis biofilms in vitro.{41304}  

     

    Brand:
    Cayman
    SKU:23863 - 1 mg

    Available on backorder

  • Sartorypyrone A is a meroditerpene metabolite produced by Neosartorya fungal species.{41303} It inhibits the growth of MCF-7 breast, NCI-H460 lung, and A375-C5 melanoma cancer cell lines (GI50s = 46.3, 37.3, and 21.5 μM, respectively). Sartorypyrone A inhibits growth of Gram-positive bacteria, including multidrug-resistant S. aureus (MIC = 32 μg/ml), and reduces the mass of S. aureus and B. subtilis biofilms in vitro.{41304}  

     

    Brand:
    Cayman
    SKU:23863 - 500 µg

    Available on backorder

  • Sartorypyrone B is a fungal metabolite that has been found in N. fischeri and has anticancer activity.{41303} It inhibits the growth of MCF-7, H460, and A375 cancer cells (GI50s = 17.8, 20.5, and 25 µM, respectively).  

     

    Brand:
    Cayman
    SKU:29949 - 1 mg

    Available on backorder

  • Sartorypyrone B is a fungal metabolite that has been found in N. fischeri and has anticancer activity.{41303} It inhibits the growth of MCF-7, H460, and A375 cancer cells (GI50s = 17.8, 20.5, and 25 µM, respectively).  

     

    Brand:
    Cayman
    SKU:29949 - 10 mg

    Available on backorder

  • Satraplatin is an orally available antineoplastic platinum(IV) complex.{32401} It is more hydrophobic than cisplatin (Item No. 13119) or oxaliplatin (Item No. 13106), which reduces transport-determined acquired resistance.{32401} Satraplatin also displays less neurotoxicity in rats than cisplatin or tetraplatin.{32402} Satraplatin has a favorable toxicity profile and appears to have clinical activity against a variety of malignancies.{32400}  

     

    Brand:
    Cayman
    SKU:20537 -

    Available on backorder

  • Satraplatin is an orally available antineoplastic platinum(IV) complex.{32401} It is more hydrophobic than cisplatin (Item No. 13119) or oxaliplatin (Item No. 13106), which reduces transport-determined acquired resistance.{32401} Satraplatin also displays less neurotoxicity in rats than cisplatin or tetraplatin.{32402} Satraplatin has a favorable toxicity profile and appears to have clinical activity against a variety of malignancies.{32400}  

     

    Brand:
    Cayman
    SKU:20537 -

    Available on backorder

  • Satraplatin is an orally available antineoplastic platinum(IV) complex.{32401} It is more hydrophobic than cisplatin (Item No. 13119) or oxaliplatin (Item No. 13106), which reduces transport-determined acquired resistance.{32401} Satraplatin also displays less neurotoxicity in rats than cisplatin or tetraplatin.{32402} Satraplatin has a favorable toxicity profile and appears to have clinical activity against a variety of malignancies.{32400}  

     

    Brand:
    Cayman
    SKU:20537 -

    Available on backorder

  • Satratoxin G is a macrocyclic trichothecene mycotoxin that has been found in S. chartarum.{53279,53280} It induces cleavage of caspase-3 and poly(ADP-ribose) polymerase (PARP) in HL-60 cells when used at a concentration of 40 nM and is cytotoxic to HepG2, Hep-2, Caco-2, A204, U937, and Jurkat cells (IC50s = 2.2-9.7 ng/ml).{53281,53282} Intranasal administration of satratoxin G (500 μg/kg) induces apoptosis of olfactory sensory neurons in olfactory epithelium and ethmoid turbinate expression of the genes encoding IL-1α, IL-1β, IL-6, TNF-α, and MIP-2 in mice.{53280} Satratoxin G induces lethality in 4 week-old male mice (LD50 = 1.23 mg/kg, i.p.).{53279}  

     

    Brand:
    Cayman
    SKU:9003415 - 1 mg

    Available on backorder

  • Satratoxin G is a macrocyclic trichothecene mycotoxin that has been found in S. chartarum.{53279,53280} It induces cleavage of caspase-3 and poly(ADP-ribose) polymerase (PARP) in HL-60 cells when used at a concentration of 40 nM and is cytotoxic to HepG2, Hep-2, Caco-2, A204, U937, and Jurkat cells (IC50s = 2.2-9.7 ng/ml).{53281,53282} Intranasal administration of satratoxin G (500 μg/kg) induces apoptosis of olfactory sensory neurons in olfactory epithelium and ethmoid turbinate expression of the genes encoding IL-1α, IL-1β, IL-6, TNF-α, and MIP-2 in mice.{53280} Satratoxin G induces lethality in 4 week-old male mice (LD50 = 1.23 mg/kg, i.p.).{53279}  

     

    Brand:
    Cayman
    SKU:9003415 - 5 mg

    Available on backorder

  • Satratoxin G is a macrocyclic trichothecene mycotoxin that has been found in S. chartarum.{53279,53280} It induces cleavage of caspase-3 and poly(ADP-ribose) polymerase (PARP) in HL-60 cells when used at a concentration of 40 nM and is cytotoxic to HepG2, Hep-2, Caco-2, A204, U937, and Jurkat cells (IC50s = 2.2-9.7 ng/ml).{53281,53282} Intranasal administration of satratoxin G (500 μg/kg) induces apoptosis of olfactory sensory neurons in olfactory epithelium and ethmoid turbinate expression of the genes encoding IL-1α, IL-1β, IL-6, TNF-α, and MIP-2 in mice.{53280} Satratoxin G induces lethality in 4 week-old male mice (LD50 = 1.23 mg/kg, i.p.).{53279}  

     

    Brand:
    Cayman
    SKU:9003415 - 500 µg

    Available on backorder

  • Satratoxin H is a trichothecene mycotoxin that has been found in Stachybotrys.{46666} It induces production of reactive oxygen species (ROS), increases in malondialdehyde (MDA) levels, and induces apoptosis in PC12 cells when used at concentrations ranging from 5 to 100 nM. Satratoxin H is cytotoxic to human umbilical vein endothelial cells (HUVECs; IC50 = 6.8 ng/ml), as well as HepG2, A549, A204, U937, and Jurkat cancer cells (IC50s = 1.2-3.4 ng/ml).{53282} In vivo, satratoxin H induces ulceration of the small intestine in, and is lethal to mice (LD50 = 5.69 mg/kg).{53279}  

     

    Brand:
    Cayman
    SKU:30199 - 1 mg

    Available on backorder

  • Satratoxin H is a trichothecene mycotoxin that has been found in Stachybotrys.{46666} It induces production of reactive oxygen species (ROS), increases in malondialdehyde (MDA) levels, and induces apoptosis in PC12 cells when used at concentrations ranging from 5 to 100 nM. Satratoxin H is cytotoxic to human umbilical vein endothelial cells (HUVECs; IC50 = 6.8 ng/ml), as well as HepG2, A549, A204, U937, and Jurkat cancer cells (IC50s = 1.2-3.4 ng/ml).{53282} In vivo, satratoxin H induces ulceration of the small intestine in, and is lethal to mice (LD50 = 5.69 mg/kg).{53279}  

     

    Brand:
    Cayman
    SKU:30199 - 5 mg

    Available on backorder

  • Satratoxin H is a trichothecene mycotoxin that has been found in Stachybotrys.{46666} It induces production of reactive oxygen species (ROS), increases in malondialdehyde (MDA) levels, and induces apoptosis in PC12 cells when used at concentrations ranging from 5 to 100 nM. Satratoxin H is cytotoxic to human umbilical vein endothelial cells (HUVECs; IC50 = 6.8 ng/ml), as well as HepG2, A549, A204, U937, and Jurkat cancer cells (IC50s = 1.2-3.4 ng/ml).{53282} In vivo, satratoxin H induces ulceration of the small intestine in, and is lethal to mice (LD50 = 5.69 mg/kg).{53279}  

     

    Brand:
    Cayman
    SKU:30199 - 500 µg

    Available on backorder

  • Sauchinone is a lignan that has been found in S. chinensis and has diverse biological activities.{12537,31525,57256,31526} It inhibits LPS-induced expression of the genes encoding inducible nitric oxide synthase (iNOS), TNF-α, and COX-2 (IC50s = ≤10 µM for all), as well as LPS-induced activation of NF-κB and nuclear translocation of NF-κB p65 in RAW 264.7 cells.{12567} Sauchinone reduces hydrogen peroxide-induced increases in heat shock protein 70 (Hsp70) levels and cell death in C2C12 mouse skeletal muscle myoblasts.{31525} In vivo, sauchinone (10 and 30 mg/kg) reduces hepatic formation of thiobarbituric acid reactive substances (TBARS), plasma levels of alanine aminotransferase (ALT), and hepatocyte cell death in a mouse model of iron overload-induced liver injury.{57256} Sauchinone (10 mg/kg) reduces infarct size and heart levels of phosphorylated p38 MAPK and JNK in a rat model of myocardial ischemia-reperfusion injury.{31526}  

     

    Brand:
    Cayman
    SKU:19577 -

    Available on backorder

  • Sauchinone is a lignan that has been found in S. chinensis and has diverse biological activities.{12537,31525,57256,31526} It inhibits LPS-induced expression of the genes encoding inducible nitric oxide synthase (iNOS), TNF-α, and COX-2 (IC50s = ≤10 µM for all), as well as LPS-induced activation of NF-κB and nuclear translocation of NF-κB p65 in RAW 264.7 cells.{12567} Sauchinone reduces hydrogen peroxide-induced increases in heat shock protein 70 (Hsp70) levels and cell death in C2C12 mouse skeletal muscle myoblasts.{31525} In vivo, sauchinone (10 and 30 mg/kg) reduces hepatic formation of thiobarbituric acid reactive substances (TBARS), plasma levels of alanine aminotransferase (ALT), and hepatocyte cell death in a mouse model of iron overload-induced liver injury.{57256} Sauchinone (10 mg/kg) reduces infarct size and heart levels of phosphorylated p38 MAPK and JNK in a rat model of myocardial ischemia-reperfusion injury.{31526}  

     

    Brand:
    Cayman
    SKU:19577 -

    Available on backorder

  • Sauchinone is a lignan that has been found in S. chinensis and has diverse biological activities.{12537,31525,57256,31526} It inhibits LPS-induced expression of the genes encoding inducible nitric oxide synthase (iNOS), TNF-α, and COX-2 (IC50s = ≤10 µM for all), as well as LPS-induced activation of NF-κB and nuclear translocation of NF-κB p65 in RAW 264.7 cells.{12567} Sauchinone reduces hydrogen peroxide-induced increases in heat shock protein 70 (Hsp70) levels and cell death in C2C12 mouse skeletal muscle myoblasts.{31525} In vivo, sauchinone (10 and 30 mg/kg) reduces hepatic formation of thiobarbituric acid reactive substances (TBARS), plasma levels of alanine aminotransferase (ALT), and hepatocyte cell death in a mouse model of iron overload-induced liver injury.{57256} Sauchinone (10 mg/kg) reduces infarct size and heart levels of phosphorylated p38 MAPK and JNK in a rat model of myocardial ischemia-reperfusion injury.{31526}  

     

    Brand:
    Cayman
    SKU:19577 -

    Available on backorder

  • Saxagliptin is a potent inhibitor of dipeptidyl peptidase 4 (DPP-4; Ki = 0.6 nM).{40437} It inhibits DPP-4 ex vivo (ED50 = 0.12 μmol/kg) in plasma from normal fasted rats. Saxagliptin (0.3-3 mg/kg) reduces plasma glucose levels in Zuckerfa/fa diabetic rats in a dose-dependent manner. Oral administration at doses ranging from 1-10 μmol/kg increases plasma insulin levels and improves glucose clearance in ob/ob mice, a transgenic model of obesity. Saxagliptin induces systolic and diastolic dysfunction, reduces contractile force, and exacerbates ischemia-reperfusion injury-induced cardiac dysfunction in isolated guinea pig hearts.{40438} Formulations containing saxagliptin have been used for the treatment of type 2 diabetes.  

     

    Brand:
    Cayman
    SKU:23697 - 10 mg

    Available on backorder

  • Saxagliptin is a potent inhibitor of dipeptidyl peptidase 4 (DPP-4; Ki = 0.6 nM).{40437} It inhibits DPP-4 ex vivo (ED50 = 0.12 μmol/kg) in plasma from normal fasted rats. Saxagliptin (0.3-3 mg/kg) reduces plasma glucose levels in Zuckerfa/fa diabetic rats in a dose-dependent manner. Oral administration at doses ranging from 1-10 μmol/kg increases plasma insulin levels and improves glucose clearance in ob/ob mice, a transgenic model of obesity. Saxagliptin induces systolic and diastolic dysfunction, reduces contractile force, and exacerbates ischemia-reperfusion injury-induced cardiac dysfunction in isolated guinea pig hearts.{40438} Formulations containing saxagliptin have been used for the treatment of type 2 diabetes.  

     

    Brand:
    Cayman
    SKU:23697 - 25 mg

    Available on backorder

  • Saxagliptin is a potent inhibitor of dipeptidyl peptidase 4 (DPP-4; Ki = 0.6 nM).{40437} It inhibits DPP-4 ex vivo (ED50 = 0.12 μmol/kg) in plasma from normal fasted rats. Saxagliptin (0.3-3 mg/kg) reduces plasma glucose levels in Zuckerfa/fa diabetic rats in a dose-dependent manner. Oral administration at doses ranging from 1-10 μmol/kg increases plasma insulin levels and improves glucose clearance in ob/ob mice, a transgenic model of obesity. Saxagliptin induces systolic and diastolic dysfunction, reduces contractile force, and exacerbates ischemia-reperfusion injury-induced cardiac dysfunction in isolated guinea pig hearts.{40438} Formulations containing saxagliptin have been used for the treatment of type 2 diabetes.  

     

    Brand:
    Cayman
    SKU:23697 - 5 mg

    Available on backorder

  • Saxagliptin is a potent inhibitor of dipeptidyl peptidase 4 (DPP-4; Ki = 0.6 nM).{40437} It inhibits DPP-4 ex vivo (ED50 = 0.12 μmol/kg) in plasma from normal fasted rats. Saxagliptin (0.3-3 mg/kg) reduces plasma glucose levels in Zuckerfa/fa diabetic rats in a dose-dependent manner. Oral administration at doses ranging from 1-10 μmol/kg increases plasma insulin levels and improves glucose clearance in ob/ob mice, a transgenic model of obesity. Saxagliptin induces systolic and diastolic dysfunction, reduces contractile force, and exacerbates ischemia-reperfusion injury-induced cardiac dysfunction in isolated guinea pig hearts.{40438} Formulations containing saxagliptin have been used for the treatment of type 2 diabetes.  

     

    Brand:
    Cayman
    SKU:23697 - 50 mg

    Available on backorder

  • SB 202190 is a selective, potent, cell-permeable inhibitor of p38 MAP kinases, inhibiting p38α (SAPK2A, MAPK14) and p38β (SAPK2B, MAPK11) with IC50 values of 50 and 100 nM, respectively.{21464,12847} When tested at 10 μM, SB 202190 has negligible effects on a range of other kinases, including other MAP kinases (ERKs, JNKs).{12847} Pyridinyl imidazole inhibitors, including this compound, directly bind p38 MAP kinases in the ATP binding pocket.{15221} Recently, SB 202190 has been used to elucidate the roles of p38 MAP kinases in inflammatory cytokine expression, nicotine-induced receptor expression, and HIV-mediated depressive disorder.{21463,21466,21467}  

     

    Brand:
    Cayman
    SKU:10010399 - 10 mg

    Available on backorder

  • SB 202190 is a selective, potent, cell-permeable inhibitor of p38 MAP kinases, inhibiting p38α (SAPK2A, MAPK14) and p38β (SAPK2B, MAPK11) with IC50 values of 50 and 100 nM, respectively.{21464,12847} When tested at 10 μM, SB 202190 has negligible effects on a range of other kinases, including other MAP kinases (ERKs, JNKs).{12847} Pyridinyl imidazole inhibitors, including this compound, directly bind p38 MAP kinases in the ATP binding pocket.{15221} Recently, SB 202190 has been used to elucidate the roles of p38 MAP kinases in inflammatory cytokine expression, nicotine-induced receptor expression, and HIV-mediated depressive disorder.{21463,21466,21467}  

     

    Brand:
    Cayman
    SKU:10010399 - 100 mg

    Available on backorder

  • SB 202190 is a selective, potent, cell-permeable inhibitor of p38 MAP kinases, inhibiting p38α (SAPK2A, MAPK14) and p38β (SAPK2B, MAPK11) with IC50 values of 50 and 100 nM, respectively.{21464,12847} When tested at 10 μM, SB 202190 has negligible effects on a range of other kinases, including other MAP kinases (ERKs, JNKs).{12847} Pyridinyl imidazole inhibitors, including this compound, directly bind p38 MAP kinases in the ATP binding pocket.{15221} Recently, SB 202190 has been used to elucidate the roles of p38 MAP kinases in inflammatory cytokine expression, nicotine-induced receptor expression, and HIV-mediated depressive disorder.{21463,21466,21467}  

     

    Brand:
    Cayman
    SKU:10010399 - 25 mg

    Available on backorder

  • SB 202190 is a selective, potent, cell-permeable inhibitor of p38 MAP kinases, inhibiting p38α (SAPK2A, MAPK14) and p38β (SAPK2B, MAPK11) with IC50 values of 50 and 100 nM, respectively.{21464,12847} When tested at 10 μM, SB 202190 has negligible effects on a range of other kinases, including other MAP kinases (ERKs, JNKs).{12847} Pyridinyl imidazole inhibitors, including this compound, directly bind p38 MAP kinases in the ATP binding pocket.{15221} Recently, SB 202190 has been used to elucidate the roles of p38 MAP kinases in inflammatory cytokine expression, nicotine-induced receptor expression, and HIV-mediated depressive disorder.{21463,21466,21467}  

     

    Brand:
    Cayman
    SKU:10010399 - 50 mg

    Available on backorder

  • SB 202190 is a potent, selective, and cell-permeable inhibitor of p38 MAP kinases, inhibiting p38α (SAPK2A, MAPK14) and p38β (SAPK2B, MAPK11) with IC50 values of 50 and 100 nM, respectively.{21464,12847} When tested at 10 μM, SB 202190 has negligible effects on a range of other kinases, including other MAP kinases such as ERK and JNK.{12847} It directly binds to the ATP binding pocket of p38 MAP kinases.{15221} SB 202190 has been used to elucidate the roles of p38 MAP kinases in inflammatory cytokine expression, nicotine-induced receptor expression, and HIV-mediated depressive disorder.{21463,21466,21467}  

     

    Brand:
    Cayman
    SKU:21201 -

    Out of stock

  • SB 202190 is a potent, selective, and cell-permeable inhibitor of p38 MAP kinases, inhibiting p38α (SAPK2A, MAPK14) and p38β (SAPK2B, MAPK11) with IC50 values of 50 and 100 nM, respectively.{21464,12847} When tested at 10 μM, SB 202190 has negligible effects on a range of other kinases, including other MAP kinases such as ERK and JNK.{12847} It directly binds to the ATP binding pocket of p38 MAP kinases.{15221} SB 202190 has been used to elucidate the roles of p38 MAP kinases in inflammatory cytokine expression, nicotine-induced receptor expression, and HIV-mediated depressive disorder.{21463,21466,21467}  

     

    Brand:
    Cayman
    SKU:21201 -

    Out of stock

  • SB 202190 is a potent, selective, and cell-permeable inhibitor of p38 MAP kinases, inhibiting p38α (SAPK2A, MAPK14) and p38β (SAPK2B, MAPK11) with IC50 values of 50 and 100 nM, respectively.{21464,12847} When tested at 10 μM, SB 202190 has negligible effects on a range of other kinases, including other MAP kinases such as ERK and JNK.{12847} It directly binds to the ATP binding pocket of p38 MAP kinases.{15221} SB 202190 has been used to elucidate the roles of p38 MAP kinases in inflammatory cytokine expression, nicotine-induced receptor expression, and HIV-mediated depressive disorder.{21463,21466,21467}  

     

    Brand:
    Cayman
    SKU:21201 -

    Out of stock

  • SB 202190 is a potent, selective, and cell-permeable inhibitor of p38 MAP kinases, inhibiting p38α (SAPK2A, MAPK14) and p38β (SAPK2B, MAPK11) with IC50 values of 50 and 100 nM, respectively.{21464,12847} When tested at 10 μM, SB 202190 has negligible effects on a range of other kinases, including other MAP kinases such as ERK and JNK.{12847} It directly binds to the ATP binding pocket of p38 MAP kinases.{15221} SB 202190 has been used to elucidate the roles of p38 MAP kinases in inflammatory cytokine expression, nicotine-induced receptor expression, and HIV-mediated depressive disorder.{21463,21466,21467}  

     

    Brand:
    Cayman
    SKU:21201 -

    Out of stock

  • SB 202190 (Item No. 10010399) and SB 203580 (Item No. 13067) are potent, selective inhibitors of the MAP kinases p38α and p38β.{21464,12847} SB 202474 is a structural analog of SB 202190 and SB 203580 that is used as a negative control in studies of p38 inhibition.{16246,30206,30205}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • Mitogen-activated protein kinases (MAPK) mediate signal transduction from cell surface receptors to the nucleus and are classified into various subtypes. p38 MAPK is activated by environmental stresses and inflammatory cytokines and is critical for normal immune and inflammatory responses as it regulates the expression of many cytokines, transcription factors, and cell surface receptors.{14980} SB 203580 is a pyridinyl imidazole inhibitor of p38 MAPK that specifically blocks its kinase activity. SB 203580 does not however, disrupt JNK activity, which is activated by similar stressors to those which activate p38 MAPK.{15737} p38 MAPK activity in heat-shocked HeLa cells and osmotically stressed PC12 cells is inhibited by SB 203580 with an IC50 value of 0.6 µM.{15737} SB 203580 also prevents the activation of PKB/Akt by inhibiting phosphoinositide-dependent protein kinase 1 (PDK1) at IC50 values of 3-5 µM.{15738}  

     

    Brand:
    Cayman
    SKU:-
  • Mitogen-activated protein kinases (MAPK) mediate signal transduction from cell surface receptors to the nucleus and are classified into various subtypes. p38 MAPK is activated by environmental stresses and inflammatory cytokines and is critical for normal immune and inflammatory responses as it regulates the expression of many cytokines, transcription factors, and cell surface receptors.{14980} SB 203580 is a pyridinyl imidazole inhibitor of p38 MAPK that specifically blocks its kinase activity. SB 203580 does not however, disrupt JNK activity, which is activated by similar stressors to those which activate p38 MAPK.{15737} p38 MAPK activity in heat-shocked HeLa cells and osmotically stressed PC12 cells is inhibited by SB 203580 with an IC50 value of 0.6 µM.{15737} SB 203580 also prevents the activation of PKB/Akt by inhibiting phosphoinositide-dependent protein kinase 1 (PDK1) at IC50 values of 3-5 µM.{15738}  

     

    Brand:
    Cayman
    SKU:-
  • Mitogen-activated protein kinases (MAPK) mediate signal transduction from cell surface receptors to the nucleus and are classified into various subtypes. p38 MAPK is activated by environmental stresses and inflammatory cytokines and is critical for normal immune and inflammatory responses as it regulates the expression of many cytokines, transcription factors, and cell surface receptors.{14980} SB 203580 is a pyridinyl imidazole inhibitor of p38 MAPK that specifically blocks its kinase activity. SB 203580 does not however, disrupt JNK activity, which is activated by similar stressors to those which activate p38 MAPK.{15737} p38 MAPK activity in heat-shocked HeLa cells and osmotically stressed PC12 cells is inhibited by SB 203580 with an IC50 value of 0.6 µM.{15737} SB 203580 also prevents the activation of PKB/Akt by inhibiting phosphoinositide-dependent protein kinase 1 (PDK1) at IC50 values of 3-5 µM.{15738}  

     

    Brand:
    Cayman
    SKU:-
  • Mitogen-activated protein kinases (MAPK) mediate signal transduction from cell surface receptors to the nucleus and are classified into various subtypes. p38 MAPK is activated by environmental stresses and inflammatory cytokines and is critical for normal immune and inflammatory responses as it regulates the expression of many cytokines, transcription factors, and cell surface receptors.{14980} SB 203580 is a pyridinyl imidazole inhibitor of p38 MAPK that specifically blocks its kinase activity. SB 203580 does not however, disrupt JNK activity, which is activated by similar stressors to those which activate p38 MAPK.{15737} p38 MAPK activity in heat-shocked HeLa cells and osmotically stressed PC12 cells is inhibited by SB 203580 with an IC50 value of 0.6 µM.{15737} SB 203580 also prevents the activation of PKB/Akt by inhibiting phosphoinositide-dependent protein kinase 1 (PDK1) at IC50 values of 3-5 µM.{15738}  

     

    Brand:
    Cayman
    SKU:-
  • Mitogen-activated protein kinases (MAPKs) mediate signal transduction from cell surface receptors to the nucleus and are classified into various subtypes. p38 MAPK is activated by environmental stresses and inflammatory cytokines and is critical for normal immune and inflammatory responses as it regulates the expression of many cytokines, transcription factors, and cell surface receptors.{14980} p38 MAPK activity in heat-shocked HeLa cells and osmotically stressed PC12 cells is inhibited by SB 203580 with an IC50 value of 0.6 µM.{15737} SB 203580 also prevents the activation of PKB/Akt by inhibiting phosphoinositide-dependent protein kinase 1 (PDK1) at IC50 values of 3-5 µM.{15738} SB 203580 (hydrochloride) has a formulation with greater solubility in organic solvents than standard SB 203580 (Item No. 13067).  

     

    Brand:
    Cayman
    SKU:-
  • Mitogen-activated protein kinases (MAPKs) mediate signal transduction from cell surface receptors to the nucleus and are classified into various subtypes. p38 MAPK is activated by environmental stresses and inflammatory cytokines and is critical for normal immune and inflammatory responses as it regulates the expression of many cytokines, transcription factors, and cell surface receptors.{14980} p38 MAPK activity in heat-shocked HeLa cells and osmotically stressed PC12 cells is inhibited by SB 203580 with an IC50 value of 0.6 µM.{15737} SB 203580 also prevents the activation of PKB/Akt by inhibiting phosphoinositide-dependent protein kinase 1 (PDK1) at IC50 values of 3-5 µM.{15738} SB 203580 (hydrochloride) has a formulation with greater solubility in organic solvents than standard SB 203580 (Item No. 13067).  

     

    Brand:
    Cayman
    SKU:-
  • Mitogen-activated protein kinases (MAPKs) mediate signal transduction from cell surface receptors to the nucleus and are classified into various subtypes. p38 MAPK is activated by environmental stresses and inflammatory cytokines and is critical for normal immune and inflammatory responses as it regulates the expression of many cytokines, transcription factors, and cell surface receptors.{14980} p38 MAPK activity in heat-shocked HeLa cells and osmotically stressed PC12 cells is inhibited by SB 203580 with an IC50 value of 0.6 µM.{15737} SB 203580 also prevents the activation of PKB/Akt by inhibiting phosphoinositide-dependent protein kinase 1 (PDK1) at IC50 values of 3-5 µM.{15738} SB 203580 (hydrochloride) has a formulation with greater solubility in organic solvents than standard SB 203580 (Item No. 13067).  

     

    Brand:
    Cayman
    SKU:-
  • Mitogen-activated protein kinases (MAPKs) mediate signal transduction from cell surface receptors to the nucleus and are classified into various subtypes. p38 MAPK is activated by environmental stresses and inflammatory cytokines and is critical for normal immune and inflammatory responses as it regulates the expression of many cytokines, transcription factors, and cell surface receptors.{14980} p38 MAPK activity in heat-shocked HeLa cells and osmotically stressed PC12 cells is inhibited by SB 203580 with an IC50 value of 0.6 µM.{15737} SB 203580 also prevents the activation of PKB/Akt by inhibiting phosphoinositide-dependent protein kinase 1 (PDK1) at IC50 values of 3-5 µM.{15738} SB 203580 (hydrochloride) has a formulation with greater solubility in organic solvents than standard SB 203580 (Item No. 13067).  

     

    Brand:
    Cayman
    SKU:-
  • SB 204990 is a cell-permeable prodrug form of SB 201076, an inhibitor of ATP citrate lyase.{37244} SB 204990 inhibits fatty acid and cholesterol synthesis in HepG2 cells in a concentration-dependent manner. Oral administration of SB 204990 (25 mg/kg) reduces plasma levels of the lipoproteins VLDL, LDL, and HDL by 21, 40, and 22%, respectively, in dogs. It also reduces VLDL synthesis and plasma cholesterol and triglyceride levels in rats in a dose-dependent manner.  

     

    Brand:
    Cayman
    SKU:-
  • SB 204990 is a cell-permeable prodrug form of SB 201076, an inhibitor of ATP citrate lyase.{37244} SB 204990 inhibits fatty acid and cholesterol synthesis in HepG2 cells in a concentration-dependent manner. Oral administration of SB 204990 (25 mg/kg) reduces plasma levels of the lipoproteins VLDL, LDL, and HDL by 21, 40, and 22%, respectively, in dogs. It also reduces VLDL synthesis and plasma cholesterol and triglyceride levels in rats in a dose-dependent manner.  

     

    Brand:
    Cayman
    SKU:-
  • SB 204990 is a cell-permeable prodrug form of SB 201076, an inhibitor of ATP citrate lyase.{37244} SB 204990 inhibits fatty acid and cholesterol synthesis in HepG2 cells in a concentration-dependent manner. Oral administration of SB 204990 (25 mg/kg) reduces plasma levels of the lipoproteins VLDL, LDL, and HDL by 21, 40, and 22%, respectively, in dogs. It also reduces VLDL synthesis and plasma cholesterol and triglyceride levels in rats in a dose-dependent manner.  

     

    Brand:
    Cayman
    SKU:-
  • SB 218078 is an inhibitor of checkpoint kinase 1 (Chk1) that blocks phosphorylation of cdc25 with an IC50 value of 15 nM.{31189} It less potently inhibits cdc2 and PKC (IC50s = 250 and 1,000 nM, respectively) and causes 85% inhibition of PKD1 at 1 µM.{31189,29520} SB 218078 releases G2 cell cycle arrest induced by γ-irradiation or the topoisomerase I inhibitor topotecan (Item No. 14129).{31189} In this way, SB 218078 enhances the cytotoxicity of DNA-damaging compounds.{24026}  

     

    Brand:
    Cayman
    SKU:-
  • SB 222200 is a neurokinin-3 (NK3) receptor antagonist (IC50 = 18.4 nM).{48780} It is selective for NK3 over NK1 and NK2 receptors (IC50s = 250 and >100,000 nM, respectively). SB 222200 decreases calcium mobilization induced by neurokinin B (Item No. 24542) with an IC50 value of 265 nM in HEK293 cells expressing the recombinant human receptor. It inhibits contractions induced by senktide (Item No. 16721) in isolated rabbit iris sphincter muscle when used at a concentration of 300 nM. SB 222200 (500 pmol, i.c.v.) decreases mean arterial pressure in spontaneously hypertensive, but not normotensive, rats.{48781} It prevents senktide-induced head shakes and tail whips in mice (ED50 = 5.6 mg/kg).{48780}  

     

    Brand:
    Cayman
    SKU:29422 - 10 mg

    Available on backorder

  • SB 222200 is a neurokinin-3 (NK3) receptor antagonist (IC50 = 18.4 nM).{48780} It is selective for NK3 over NK1 and NK2 receptors (IC50s = 250 and >100,000 nM, respectively). SB 222200 decreases calcium mobilization induced by neurokinin B (Item No. 24542) with an IC50 value of 265 nM in HEK293 cells expressing the recombinant human receptor. It inhibits contractions induced by senktide (Item No. 16721) in isolated rabbit iris sphincter muscle when used at a concentration of 300 nM. SB 222200 (500 pmol, i.c.v.) decreases mean arterial pressure in spontaneously hypertensive, but not normotensive, rats.{48781} It prevents senktide-induced head shakes and tail whips in mice (ED50 = 5.6 mg/kg).{48780}  

     

    Brand:
    Cayman
    SKU:29422 - 25 mg

    Available on backorder

  • SB 222200 is a neurokinin-3 (NK3) receptor antagonist (IC50 = 18.4 nM).{48780} It is selective for NK3 over NK1 and NK2 receptors (IC50s = 250 and >100,000 nM, respectively). SB 222200 decreases calcium mobilization induced by neurokinin B (Item No. 24542) with an IC50 value of 265 nM in HEK293 cells expressing the recombinant human receptor. It inhibits contractions induced by senktide (Item No. 16721) in isolated rabbit iris sphincter muscle when used at a concentration of 300 nM. SB 222200 (500 pmol, i.c.v.) decreases mean arterial pressure in spontaneously hypertensive, but not normotensive, rats.{48781} It prevents senktide-induced head shakes and tail whips in mice (ED50 = 5.6 mg/kg).{48780}  

     

    Brand:
    Cayman
    SKU:29422 - 5 mg

    Available on backorder

  • SB 222200 is a neurokinin-3 (NK3) receptor antagonist (IC50 = 18.4 nM).{48780} It is selective for NK3 over NK1 and NK2 receptors (IC50s = 250 and >100,000 nM, respectively). SB 222200 decreases calcium mobilization induced by neurokinin B (Item No. 24542) with an IC50 value of 265 nM in HEK293 cells expressing the recombinant human receptor. It inhibits contractions induced by senktide (Item No. 16721) in isolated rabbit iris sphincter muscle when used at a concentration of 300 nM. SB 222200 (500 pmol, i.c.v.) decreases mean arterial pressure in spontaneously hypertensive, but not normotensive, rats.{48781} It prevents senktide-induced head shakes and tail whips in mice (ED50 = 5.6 mg/kg).{48780}  

     

    Brand:
    Cayman
    SKU:29422 - 50 mg

    Available on backorder

  • CXCR2 (IL-8RB) is a seven-transmembrane G protein-coupled receptor whose physiological ligands include IL-8 (CXCL8) and growth related oncogene α (Gro-α; CXCL1). IL-8 and Gro-α are pro-inflammatory CXC chemokines that act as chemoattractants, especially for neutrophils, and promote angiogenesis. SB 225002 is a selective non-peptide inhibitor of CXCR2, inhibiting IL-8 binding to CXCR2 with an IC50 value of 22 nM.{17249} SB225002 inhibits neutrophil chemotaxis in response to IL-8 in vitro (IC50 = 20 nM) and blocks neutrophil margination induced by IL-8 in vivo (IC50 = 30 nM).{17249} Similarly, SB 225002 reduces neutrophil influx, the production of inflammatory mediators, and tissue damage in TNBS-induced colitis in mice.{17248}  

     

    Brand:
    Cayman
    SKU:-
  • CXCR2 (IL-8RB) is a seven-transmembrane G protein-coupled receptor whose physiological ligands include IL-8 (CXCL8) and growth related oncogene α (Gro-α; CXCL1). IL-8 and Gro-α are pro-inflammatory CXC chemokines that act as chemoattractants, especially for neutrophils, and promote angiogenesis. SB 225002 is a selective non-peptide inhibitor of CXCR2, inhibiting IL-8 binding to CXCR2 with an IC50 value of 22 nM.{17249} SB225002 inhibits neutrophil chemotaxis in response to IL-8 in vitro (IC50 = 20 nM) and blocks neutrophil margination induced by IL-8 in vivo (IC50 = 30 nM).{17249} Similarly, SB 225002 reduces neutrophil influx, the production of inflammatory mediators, and tissue damage in TNBS-induced colitis in mice.{17248}  

     

    Brand:
    Cayman
    SKU:-
  • CXCR2 (IL-8RB) is a seven-transmembrane G protein-coupled receptor whose physiological ligands include IL-8 (CXCL8) and growth related oncogene α (Gro-α; CXCL1). IL-8 and Gro-α are pro-inflammatory CXC chemokines that act as chemoattractants, especially for neutrophils, and promote angiogenesis. SB 225002 is a selective non-peptide inhibitor of CXCR2, inhibiting IL-8 binding to CXCR2 with an IC50 value of 22 nM.{17249} SB225002 inhibits neutrophil chemotaxis in response to IL-8 in vitro (IC50 = 20 nM) and blocks neutrophil margination induced by IL-8 in vivo (IC50 = 30 nM).{17249} Similarly, SB 225002 reduces neutrophil influx, the production of inflammatory mediators, and tissue damage in TNBS-induced colitis in mice.{17248}  

     

    Brand:
    Cayman
    SKU:-
  • CXCR2 (IL-8RB) is a seven-transmembrane G protein-coupled receptor whose physiological ligands include IL-8 (CXCL8) and growth related oncogene α (Gro-α; CXCL1). IL-8 and Gro-α are pro-inflammatory CXC chemokines that act as chemoattractants, especially for neutrophils, and promote angiogenesis. SB 225002 is a selective non-peptide inhibitor of CXCR2, inhibiting IL-8 binding to CXCR2 with an IC50 value of 22 nM.{17249} SB225002 inhibits neutrophil chemotaxis in response to IL-8 in vitro (IC50 = 20 nM) and blocks neutrophil margination induced by IL-8 in vivo (IC50 = 30 nM).{17249} Similarly, SB 225002 reduces neutrophil influx, the production of inflammatory mediators, and tissue damage in TNBS-induced colitis in mice.{17248}  

     

    Brand:
    Cayman
    SKU:-
  • SB 239063 is a selective p38 MAPK inhibitor (IC50 = 44 nM for recombinant purified p38α).{30980} It displays greater than 220-fold selectivity for p38 MAPK over ERK, JNK1, and other kinases.{30980} SB 239063 has been shown to reduce inflammatory cytokine production in lipopolysaccharide-stimulated human peripheral blood monocytes (IC50s = 0.12 and 0.35 µM, respectively for IL-1 and TNF-α) and is neuroprotective following oral administration in a rat model of cerebral focal ischemia.{30980,30979}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • SB 239063 is a selective p38 MAPK inhibitor (IC50 = 44 nM for recombinant purified p38α).{30980} It displays greater than 220-fold selectivity for p38 MAPK over ERK, JNK1, and other kinases.{30980} SB 239063 has been shown to reduce inflammatory cytokine production in lipopolysaccharide-stimulated human peripheral blood monocytes (IC50s = 0.12 and 0.35 µM, respectively for IL-1 and TNF-α) and is neuroprotective following oral administration in a rat model of cerebral focal ischemia.{30980,30979}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • SB 239063 is a selective p38 MAPK inhibitor (IC50 = 44 nM for recombinant purified p38α).{30980} It displays greater than 220-fold selectivity for p38 MAPK over ERK, JNK1, and other kinases.{30980} SB 239063 has been shown to reduce inflammatory cytokine production in lipopolysaccharide-stimulated human peripheral blood monocytes (IC50s = 0.12 and 0.35 µM, respectively for IL-1 and TNF-α) and is neuroprotective following oral administration in a rat model of cerebral focal ischemia.{30980,30979}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • CXCR2 (IL-8RB) is a seven-transmembrane G protein-coupled receptor whose physiological ligands include IL-8 (CXCL8) and many other CXC chemokines involved in the trafficking and activation of inflammatory cells. It is involved in various inflammatory diseases, including chronic obstructive pulmonary disease, psoriasis, rheumatoid arthritis, and ulcerative colitis. SB 265610 is a nonpeptide, allosteric, inverse agonist of CXCR2 (Kd = 2.51 nM) that prevents receptor activation by binding to a region distinct from the agonist binding site.{29567,29566} It does not bind to the related CXCR1 receptor.{29567} It has been shown to prevent neutrophil chemotaxis both in vitro and in a rat model of hyperoxia-induced lung injury.{29565}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • CXCR2 (IL-8RB) is a seven-transmembrane G protein-coupled receptor whose physiological ligands include IL-8 (CXCL8) and many other CXC chemokines involved in the trafficking and activation of inflammatory cells. It is involved in various inflammatory diseases, including chronic obstructive pulmonary disease, psoriasis, rheumatoid arthritis, and ulcerative colitis. SB 265610 is a nonpeptide, allosteric, inverse agonist of CXCR2 (Kd = 2.51 nM) that prevents receptor activation by binding to a region distinct from the agonist binding site.{29567,29566} It does not bind to the related CXCR1 receptor.{29567} It has been shown to prevent neutrophil chemotaxis both in vitro and in a rat model of hyperoxia-induced lung injury.{29565}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • CXCR2 (IL-8RB) is a seven-transmembrane G protein-coupled receptor whose physiological ligands include IL-8 (CXCL8) and many other CXC chemokines involved in the trafficking and activation of inflammatory cells. It is involved in various inflammatory diseases, including chronic obstructive pulmonary disease, psoriasis, rheumatoid arthritis, and ulcerative colitis. SB 265610 is a nonpeptide, allosteric, inverse agonist of CXCR2 (Kd = 2.51 nM) that prevents receptor activation by binding to a region distinct from the agonist binding site.{29567,29566} It does not bind to the related CXCR1 receptor.{29567} It has been shown to prevent neutrophil chemotaxis both in vitro and in a rat model of hyperoxia-induced lung injury.{29565}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • SB 277011A is an antagonist of the dopamine D3 receptor (pKi = 8.0) that is at least 100-fold selective for D3 over other monoamine receptors (pKis = 6.0, 5.0, and 2, 5-HT1D and 5-HT1B respectively).{31910,31909,31908} It has high oral bioavailability and enters the central nervous system of the rat.{31910} SB 277011A has been shown to have potential benefits in animal models of schizophrenia and Parkinson’s disease.{31909,31907}  

     

    Brand:
    Cayman
    SKU:11982 - 1 mg

    Available on backorder

  • SB 277011A is an antagonist of the dopamine D3 receptor (pKi = 8.0) that is at least 100-fold selective for D3 over other monoamine receptors (pKis = 6.0, 5.0, and 2, 5-HT1D and 5-HT1B respectively).{31910,31909,31908} It has high oral bioavailability and enters the central nervous system of the rat.{31910} SB 277011A has been shown to have potential benefits in animal models of schizophrenia and Parkinson’s disease.{31909,31907}  

     

    Brand:
    Cayman
    SKU:11982 - 10 mg

    Available on backorder

  • SB 277011A is an antagonist of the dopamine D3 receptor (pKi = 8.0) that is at least 100-fold selective for D3 over other monoamine receptors (pKis = 6.0, 5.0, and 2, 5-HT1D and 5-HT1B respectively).{31910,31909,31908} It has high oral bioavailability and enters the central nervous system of the rat.{31910} SB 277011A has been shown to have potential benefits in animal models of schizophrenia and Parkinson’s disease.{31909,31907}  

     

    Brand:
    Cayman
    SKU:11982 - 25 mg

    Available on backorder

  • SB 277011A is an antagonist of the dopamine D3 receptor (pKi = 8.0) that is at least 100-fold selective for D3 over other monoamine receptors (pKis = 6.0, 5.0, and 2, 5-HT1D and 5-HT1B respectively).{31910,31909,31908} It has high oral bioavailability and enters the central nervous system of the rat.{31910} SB 277011A has been shown to have potential benefits in animal models of schizophrenia and Parkinson’s disease.{31909,31907}  

     

    Brand:
    Cayman
    SKU:11982 - 5 mg

    Available on backorder

  • The anaphylatoxin C3a induces a range of responses by activating its G protein-coupled receptor, C3aR, resulting in calcium mobilization.{25900} SB 290157 is a non-peptide antagonist of C3aR, competitively blocking C3a binding with an IC50 value of 200 nM.{25894} It potently inhibits a wide variety of C3a-induced responses in cells, including calcium increase in human neutrophils (IC50 = 28 nM) and ATP release from guinea pig platelets (IC50 = 30 nM).{25894} SB 290157 is also effective in vivo, reducing inflammation in a variety of animal models.{25894,25897,25895} It also significantly reduces or reverses diet-induced obesity in rats and accelerates the mobilization of hematopoietic progenitor cells to the peripheral blood in mice.{25896,25898} Notably, SB 290157 has C3aR agonist activity in some cell systems.{25893,25899}  

     

    Brand:
    Cayman
    SKU:-
  • The anaphylatoxin C3a induces a range of responses by activating its G protein-coupled receptor, C3aR, resulting in calcium mobilization.{25900} SB 290157 is a non-peptide antagonist of C3aR, competitively blocking C3a binding with an IC50 value of 200 nM.{25894} It potently inhibits a wide variety of C3a-induced responses in cells, including calcium increase in human neutrophils (IC50 = 28 nM) and ATP release from guinea pig platelets (IC50 = 30 nM).{25894} SB 290157 is also effective in vivo, reducing inflammation in a variety of animal models.{25894,25897,25895} It also significantly reduces or reverses diet-induced obesity in rats and accelerates the mobilization of hematopoietic progenitor cells to the peripheral blood in mice.{25896,25898} Notably, SB 290157 has C3aR agonist activity in some cell systems.{25893,25899}  

     

    Brand:
    Cayman
    SKU:-
  • The anaphylatoxin C3a induces a range of responses by activating its G protein-coupled receptor, C3aR, resulting in calcium mobilization.{25900} SB 290157 is a non-peptide antagonist of C3aR, competitively blocking C3a binding with an IC50 value of 200 nM.{25894} It potently inhibits a wide variety of C3a-induced responses in cells, including calcium increase in human neutrophils (IC50 = 28 nM) and ATP release from guinea pig platelets (IC50 = 30 nM).{25894} SB 290157 is also effective in vivo, reducing inflammation in a variety of animal models.{25894,25897,25895} It also significantly reduces or reverses diet-induced obesity in rats and accelerates the mobilization of hematopoietic progenitor cells to the peripheral blood in mice.{25896,25898} Notably, SB 290157 has C3aR agonist activity in some cell systems.{25893,25899}  

     

    Brand:
    Cayman
    SKU:-
  • The anaphylatoxin C3a induces a range of responses by activating its G protein-coupled receptor, C3aR, resulting in calcium mobilization.{25900} SB 290157 is a non-peptide antagonist of C3aR, competitively blocking C3a binding with an IC50 value of 200 nM.{25894} It potently inhibits a wide variety of C3a-induced responses in cells, including calcium increase in human neutrophils (IC50 = 28 nM) and ATP release from guinea pig platelets (IC50 = 30 nM).{25894} SB 290157 is also effective in vivo, reducing inflammation in a variety of animal models.{25894,25897,25895} It also significantly reduces or reverses diet-induced obesity in rats and accelerates the mobilization of hematopoietic progenitor cells to the peripheral blood in mice.{25896,25898} Notably, SB 290157 has C3aR agonist activity in some cell systems.{25893,25899}  

     

    Brand:
    Cayman
    SKU:-
  • SB 297006 is an antagonist of C-C chemokine receptor 3 (CCR3; IC50 = 39 nM), which normally is activated by eotaxin, eotaxin-3, MCP-3, MCP-4, RANTES, and MIP-1δ.{32621} It is at least 250-fold selective for CCR3 over a panel of other chemokine receptors. SB 297006 blocks CCR3-mediated calcium mobilization induced by eotaxin, eotaxin-2, and MCP-4 in transfected cells.{32621} It suppresses antigen-induced accumulation of Th2 lymphocytes and eosinophils in lungs of mice when delivered subcutaneously (100 mg/kg).{32620}  

     

    Brand:
    Cayman
    SKU:11964 - 1 mg

    Available on backorder

  • SB 297006 is an antagonist of C-C chemokine receptor 3 (CCR3; IC50 = 39 nM), which normally is activated by eotaxin, eotaxin-3, MCP-3, MCP-4, RANTES, and MIP-1δ.{32621} It is at least 250-fold selective for CCR3 over a panel of other chemokine receptors. SB 297006 blocks CCR3-mediated calcium mobilization induced by eotaxin, eotaxin-2, and MCP-4 in transfected cells.{32621} It suppresses antigen-induced accumulation of Th2 lymphocytes and eosinophils in lungs of mice when delivered subcutaneously (100 mg/kg).{32620}  

     

    Brand:
    Cayman
    SKU:11964 - 10 mg

    Available on backorder

  • SB 297006 is an antagonist of C-C chemokine receptor 3 (CCR3; IC50 = 39 nM), which normally is activated by eotaxin, eotaxin-3, MCP-3, MCP-4, RANTES, and MIP-1δ.{32621} It is at least 250-fold selective for CCR3 over a panel of other chemokine receptors. SB 297006 blocks CCR3-mediated calcium mobilization induced by eotaxin, eotaxin-2, and MCP-4 in transfected cells.{32621} It suppresses antigen-induced accumulation of Th2 lymphocytes and eosinophils in lungs of mice when delivered subcutaneously (100 mg/kg).{32620}  

     

    Brand:
    Cayman
    SKU:11964 - 25 mg

    Available on backorder

  • SB 297006 is an antagonist of C-C chemokine receptor 3 (CCR3; IC50 = 39 nM), which normally is activated by eotaxin, eotaxin-3, MCP-3, MCP-4, RANTES, and MIP-1δ.{32621} It is at least 250-fold selective for CCR3 over a panel of other chemokine receptors. SB 297006 blocks CCR3-mediated calcium mobilization induced by eotaxin, eotaxin-2, and MCP-4 in transfected cells.{32621} It suppresses antigen-induced accumulation of Th2 lymphocytes and eosinophils in lungs of mice when delivered subcutaneously (100 mg/kg).{32620}  

     

    Brand:
    Cayman
    SKU:11964 - 5 mg

    Available on backorder

  • SB-200646 is a dual antagonist of the serotonin (5-HT) receptor subtypes 5-HT2C (Ki = 125 nM in isolated rat cortex) and 5-HT2B (pA2 = 7.5 in rat stomach fundus preparations).{54226} It is selective for 5-HT2C and 5-HT2B over 5-HT1A, 5-HT2A, 5-HT1D, 5-HT3, benzodiazepine, GABAA, α1-, α2A-, α2B-, β1-, and β2-adrenergic, dopamine D1 and D2, and histamine H1 receptors (Kis = >10 µM for all). SB-200646 (20 and 40 mg/kg) reverses mCPP-induced hypophagia and decreases in social interaction time, indicating anxiolytic-like behavior, in rats.  

     

    Brand:
    Cayman
    SKU:30973 - 1 mg

    Available on backorder

  • SB-200646 is a dual antagonist of the serotonin (5-HT) receptor subtypes 5-HT2C (Ki = 125 nM in isolated rat cortex) and 5-HT2B (pA2 = 7.5 in rat stomach fundus preparations).{54226} It is selective for 5-HT2C and 5-HT2B over 5-HT1A, 5-HT2A, 5-HT1D, 5-HT3, benzodiazepine, GABAA, α1-, α2A-, α2B-, β1-, and β2-adrenergic, dopamine D1 and D2, and histamine H1 receptors (Kis = >10 µM for all). SB-200646 (20 and 40 mg/kg) reverses mCPP-induced hypophagia and decreases in social interaction time, indicating anxiolytic-like behavior, in rats.  

     

    Brand:
    Cayman
    SKU:30973 - 10 mg

    Available on backorder

  • SB-200646 is a dual antagonist of the serotonin (5-HT) receptor subtypes 5-HT2C (Ki = 125 nM in isolated rat cortex) and 5-HT2B (pA2 = 7.5 in rat stomach fundus preparations).{54226} It is selective for 5-HT2C and 5-HT2B over 5-HT1A, 5-HT2A, 5-HT1D, 5-HT3, benzodiazepine, GABAA, α1-, α2A-, α2B-, β1-, and β2-adrenergic, dopamine D1 and D2, and histamine H1 receptors (Kis = >10 µM for all). SB-200646 (20 and 40 mg/kg) reverses mCPP-induced hypophagia and decreases in social interaction time, indicating anxiolytic-like behavior, in rats.  

     

    Brand:
    Cayman
    SKU:30973 - 5 mg

    Available on backorder

  • The indole derivative SB-207266 is a selective and potent antagonist of the serotonin (5-HT) receptor 5-HT4 with a pA2 value of 10.6 ± 0.1.{34073, 34070} In COS7 cells, 100 nM SB-207266 inhibited 5-HT4 responses to 5-HT and reduced basal agonist-independent cAMP production.{34070} In several animal models, low concentrations of SB-207266 blocked exogenous 5-HT-mediated sensitization of intestinal peristalsis.{34073, 34072, 34071} In a dog model, SB-207266 (0.1–100 pg/kg) dose-dependently reduced responses to 5-HT, with an ID50 value of 1.3 pg/kg.{34073} SB-206226 (0.5 mg/kg/24 h) improved cardiac function in a rat model of congestive heart failure.{34069}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • The indole derivative SB-207266 is a selective and potent antagonist of the serotonin (5-HT) receptor 5-HT4 with a pA2 value of 10.6 ± 0.1.{34073, 34070} In COS7 cells, 100 nM SB-207266 inhibited 5-HT4 responses to 5-HT and reduced basal agonist-independent cAMP production.{34070} In several animal models, low concentrations of SB-207266 blocked exogenous 5-HT-mediated sensitization of intestinal peristalsis.{34073, 34072, 34071} In a dog model, SB-207266 (0.1–100 pg/kg) dose-dependently reduced responses to 5-HT, with an ID50 value of 1.3 pg/kg.{34073} SB-206226 (0.5 mg/kg/24 h) improved cardiac function in a rat model of congestive heart failure.{34069}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • The indole derivative SB-207266 is a selective and potent antagonist of the serotonin (5-HT) receptor 5-HT4 with a pA2 value of 10.6 ± 0.1.{34073, 34070} In COS7 cells, 100 nM SB-207266 inhibited 5-HT4 responses to 5-HT and reduced basal agonist-independent cAMP production.{34070} In several animal models, low concentrations of SB-207266 blocked exogenous 5-HT-mediated sensitization of intestinal peristalsis.{34073, 34072, 34071} In a dog model, SB-207266 (0.1–100 pg/kg) dose-dependently reduced responses to 5-HT, with an ID50 value of 1.3 pg/kg.{34073} SB-206226 (0.5 mg/kg/24 h) improved cardiac function in a rat model of congestive heart failure.{34069}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • The indole derivative SB-207266 is a selective and potent antagonist of the serotonin (5-HT) receptor 5-HT4 with a pA2 value of 10.6 ± 0.1.{34073, 34070} In COS7 cells, 100 nM SB-207266 inhibited 5-HT4 responses to 5-HT and reduced basal agonist-independent cAMP production.{34070} In several animal models, low concentrations of SB-207266 blocked exogenous 5-HT-mediated sensitization of intestinal peristalsis.{34073, 34072, 34071} In a dog model, SB-207266 (0.1–100 pg/kg) dose-dependently reduced responses to 5-HT, with an ID50 value of 1.3 pg/kg.{34073} SB-206226 (0.5 mg/kg/24 h) improved cardiac function in a rat model of congestive heart failure.{34069}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • Glycogen synthase kinase 3 (GSK3) is a serine/threonine protein kinase that is inhibited by an assortment of extracellular stimuli including insulin, growth factors, cell specification factors, and cell adhesion. SB-216763 is a potent and selective cell permeable ATP-competitive inhibitor of GSK3α with an IC50 value of 34 nM (similar potency for GSK3β).{15623} It stimulates glycogen synthesis in Chang human liver cells with an EC50 value of 3.6 µM and induces expression of a β-catenin-LEF/Tcf regulated reporter gene in HEK293 cells.{15623} SB-216763 protects primary neurons from death induced by the PI3-kinase pathway.{15622}  

     

    Brand:
    Cayman
    SKU:10010246 - 10 mg

    Available on backorder

  • Glycogen synthase kinase 3 (GSK3) is a serine/threonine protein kinase that is inhibited by an assortment of extracellular stimuli including insulin, growth factors, cell specification factors, and cell adhesion. SB-216763 is a potent and selective cell permeable ATP-competitive inhibitor of GSK3α with an IC50 value of 34 nM (similar potency for GSK3β).{15623} It stimulates glycogen synthesis in Chang human liver cells with an EC50 value of 3.6 µM and induces expression of a β-catenin-LEF/Tcf regulated reporter gene in HEK293 cells.{15623} SB-216763 protects primary neurons from death induced by the PI3-kinase pathway.{15622}  

     

    Brand:
    Cayman
    SKU:10010246 - 100 mg

    Available on backorder

  • Glycogen synthase kinase 3 (GSK3) is a serine/threonine protein kinase that is inhibited by an assortment of extracellular stimuli including insulin, growth factors, cell specification factors, and cell adhesion. SB-216763 is a potent and selective cell permeable ATP-competitive inhibitor of GSK3α with an IC50 value of 34 nM (similar potency for GSK3β).{15623} It stimulates glycogen synthesis in Chang human liver cells with an EC50 value of 3.6 µM and induces expression of a β-catenin-LEF/Tcf regulated reporter gene in HEK293 cells.{15623} SB-216763 protects primary neurons from death induced by the PI3-kinase pathway.{15622}  

     

    Brand:
    Cayman
    SKU:10010246 - 5 mg

    Available on backorder

  • Glycogen synthase kinase 3 (GSK3) is a serine/threonine protein kinase that is inhibited by an assortment of extracellular stimuli including insulin, growth factors, cell specification factors, and cell adhesion. SB-216763 is a potent and selective cell permeable ATP-competitive inhibitor of GSK3α with an IC50 value of 34 nM (similar potency for GSK3β).{15623} It stimulates glycogen synthesis in Chang human liver cells with an EC50 value of 3.6 µM and induces expression of a β-catenin-LEF/Tcf regulated reporter gene in HEK293 cells.{15623} SB-216763 protects primary neurons from death induced by the PI3-kinase pathway.{15622}  

     

    Brand:
    Cayman
    SKU:10010246 - 50 mg

    Available on backorder

  • The transduction of neurobehavioral effects by serotonin (5-hydroxy tryptamine; 5-HT) is mediated by at least seven major 5-HT receptor subtypes. SB-224289 is a potent 5-HT1B inverse agonist (pKi = 8.16) that displays >75-fold selectivity for human 5-HT1B over all other 5-HT receptors.{27920} It has been used to study the role of 5-HT1B receptors in cocaine self-administration and cocaine-seeking behavior.{27921}  

     

    Brand:
    Cayman
    SKU:-

    Out of stock

  • The transduction of neurobehavioral effects by serotonin (5-hydroxy tryptamine; 5-HT) is mediated by at least seven major 5-HT receptor subtypes. SB-224289 is a potent 5-HT1B inverse agonist (pKi = 8.16) that displays >75-fold selectivity for human 5-HT1B over all other 5-HT receptors.{27920} It has been used to study the role of 5-HT1B receptors in cocaine self-administration and cocaine-seeking behavior.{27921}  

     

    Brand:
    Cayman
    SKU:-

    Out of stock

  • The transduction of neurobehavioral effects by serotonin (5-hydroxy tryptamine; 5-HT) is mediated by at least seven major 5-HT receptor subtypes. SB-224289 is a potent 5-HT1B inverse agonist (pKi = 8.16) that displays >75-fold selectivity for human 5-HT1B over all other 5-HT receptors.{27920} It has been used to study the role of 5-HT1B receptors in cocaine self-administration and cocaine-seeking behavior.{27921}  

     

    Brand:
    Cayman
    SKU:-

    Out of stock

  • The transduction of neurobehavioral effects by serotonin (5-hydroxy tryptamine; 5-HT) is mediated by at least seven major 5-HT receptor subtypes. SB-224289 is a potent 5-HT1B inverse agonist (pKi = 8.16) that displays >75-fold selectivity for human 5-HT1B over all other 5-HT receptors.{27920} It has been used to study the role of 5-HT1B receptors in cocaine self-administration and cocaine-seeking behavior.{27921}  

     

    Brand:
    Cayman
    SKU:-

    Out of stock

  • Serotonin (5-hydroxytryptamine, 5-HT) is a neurotransmitter that activates specific receptors located primarily in the gut and central nervous system. SB-242084 is an antagonist of the 5-HT2C receptor (pKi = 9.0), with at least 100-fold more selectivity over other 5-HT, dopamine, or adrenergic receptors.{18221,18225} In vivo, it is brain penetrant and has significant anxiolytic activity, without sedative, proconvulsant, or hyperphagic properties.{18221} SB-242084 has been used extensively in animal research to evaluate, for example, 5-HT2C receptor agonists and neurotransmitter receptor interactions in mice.{18222,18223,18224}  

     

    Brand:
    Cayman
    SKU:10096 - 1 mg

    Available on backorder

  • Serotonin (5-hydroxytryptamine, 5-HT) is a neurotransmitter that activates specific receptors located primarily in the gut and central nervous system. SB-242084 is an antagonist of the 5-HT2C receptor (pKi = 9.0), with at least 100-fold more selectivity over other 5-HT, dopamine, or adrenergic receptors.{18221,18225} In vivo, it is brain penetrant and has significant anxiolytic activity, without sedative, proconvulsant, or hyperphagic properties.{18221} SB-242084 has been used extensively in animal research to evaluate, for example, 5-HT2C receptor agonists and neurotransmitter receptor interactions in mice.{18222,18223,18224}  

     

    Brand:
    Cayman
    SKU:10096 - 10 mg

    Available on backorder

  • Serotonin (5-hydroxytryptamine, 5-HT) is a neurotransmitter that activates specific receptors located primarily in the gut and central nervous system. SB-242084 is an antagonist of the 5-HT2C receptor (pKi = 9.0), with at least 100-fold more selectivity over other 5-HT, dopamine, or adrenergic receptors.{18221,18225} In vivo, it is brain penetrant and has significant anxiolytic activity, without sedative, proconvulsant, or hyperphagic properties.{18221} SB-242084 has been used extensively in animal research to evaluate, for example, 5-HT2C receptor agonists and neurotransmitter receptor interactions in mice.{18222,18223,18224}  

     

    Brand:
    Cayman
    SKU:10096 - 5 mg

    Available on backorder

  • SB-258585 is a potent, selective antagonist of the serotonin 5-HT6 receptor (pKi = 8.53).{30745} It displays over 100-fold selectivity for 5-HT6 over other 5-HT, dopamine, and α-adrenergic receptors. Radiolabeled forms of SB-258585 have been used to evaluate other potential ligands of the 5-HT6 receptor.{29781} SB-258585 has been used in cells and in animals to evaluate the role of the 5-HT6 receptor in diverse processes.{30747,30744,30746}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • SB-258585 is a potent, selective antagonist of the serotonin 5-HT6 receptor (pKi = 8.53).{30745} It displays over 100-fold selectivity for 5-HT6 over other 5-HT, dopamine, and α-adrenergic receptors. Radiolabeled forms of SB-258585 have been used to evaluate other potential ligands of the 5-HT6 receptor.{29781} SB-258585 has been used in cells and in animals to evaluate the role of the 5-HT6 receptor in diverse processes.{30747,30744,30746}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • SB-258585 is a potent, selective antagonist of the serotonin 5-HT6 receptor (pKi = 8.53).{30745} It displays over 100-fold selectivity for 5-HT6 over other 5-HT, dopamine, and α-adrenergic receptors. Radiolabeled forms of SB-258585 have been used to evaluate other potential ligands of the 5-HT6 receptor.{29781} SB-258585 has been used in cells and in animals to evaluate the role of the 5-HT6 receptor in diverse processes.{30747,30744,30746}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • SB-258585 is a potent, selective antagonist of the serotonin 5-HT6 receptor (pKi = 8.53).{30745} It displays over 100-fold selectivity for 5-HT6 over other 5-HT, dopamine, and α-adrenergic receptors. Radiolabeled forms of SB-258585 have been used to evaluate other potential ligands of the 5-HT6 receptor.{29781} SB-258585 has been used in cells and in animals to evaluate the role of the 5-HT6 receptor in diverse processes.{30747,30744,30746}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • The transduction of neurobehavioral effects by serotonin (5-hydroxy tryptamine; 5-HT) is mediated by at least seven major 5-HT receptor subtypes. SB-269970 is a potent 5-HT7A antagonist (pKi = 8.9) that demonstrates >50-fold binding selectivity over 5-HT5A and >250-fold selectivity over 5-HT1, 5-HT2, 5-HT4, 5-HT6, adrenergic α1, dopamine D2, and dopamine D3 receptors.{27806} It is also reported to block adrenergic α2 receptors in guinea pig vas deferens.{27807} SB-269970 has been used to target the 5-HT7 receptor in the study of schizophrenia-like cognitive deficits.{27808}  

     

    Brand:
    Cayman
    SKU:-

    Out of stock

  • The transduction of neurobehavioral effects by serotonin (5-hydroxy tryptamine; 5-HT) is mediated by at least seven major 5-HT receptor subtypes. SB-269970 is a potent 5-HT7A antagonist (pKi = 8.9) that demonstrates >50-fold binding selectivity over 5-HT5A and >250-fold selectivity over 5-HT1, 5-HT2, 5-HT4, 5-HT6, adrenergic α1, dopamine D2, and dopamine D3 receptors.{27806} It is also reported to block adrenergic α2 receptors in guinea pig vas deferens.{27807} SB-269970 has been used to target the 5-HT7 receptor in the study of schizophrenia-like cognitive deficits.{27808}  

     

    Brand:
    Cayman
    SKU:-

    Out of stock

  • The transduction of neurobehavioral effects by serotonin (5-hydroxy tryptamine; 5-HT) is mediated by at least seven major 5-HT receptor subtypes. SB-269970 is a potent 5-HT7A antagonist (pKi = 8.9) that demonstrates >50-fold binding selectivity over 5-HT5A and >250-fold selectivity over 5-HT1, 5-HT2, 5-HT4, 5-HT6, adrenergic α1, dopamine D2, and dopamine D3 receptors.{27806} It is also reported to block adrenergic α2 receptors in guinea pig vas deferens.{27807} SB-269970 has been used to target the 5-HT7 receptor in the study of schizophrenia-like cognitive deficits.{27808}  

     

    Brand:
    Cayman
    SKU:-

    Out of stock

  • The transduction of neurobehavioral effects by serotonin (5-hydroxy tryptamine; 5-HT) is mediated by at least seven major 5-HT receptor subtypes. SB-269970 is a potent 5-HT7A antagonist (pKi = 8.9) that demonstrates >50-fold binding selectivity over 5-HT5A and >250-fold selectivity over 5-HT1, 5-HT2, 5-HT4, 5-HT6, adrenergic α1, dopamine D2, and dopamine D3 receptors.{27806} It is also reported to block adrenergic α2 receptors in guinea pig vas deferens.{27807} SB-269970 has been used to target the 5-HT7 receptor in the study of schizophrenia-like cognitive deficits.{27808}  

     

    Brand:
    Cayman
    SKU:-

    Out of stock

  • SB-271046 is an orally-available antagonist of the serotonin (5-hydroxytryptamine, or 5-HT; Item No. 14332) receptor 5-HT6 (pKi = 9.02-8.92).{29779,29781} It is at least 100-fold selective for 5-HT6 over other 5-HT receptors, as well as 55 other receptors, enzymes, and ion channels.{29781} While it does not alter basal levels of 5-HT, dopamine, or noradrenaline, SB-271046 produces a significant increase in extracellular levels of glutamate and aspartate within the frontal cortex.{29780} It has been used to evaluate the role of 5-HT6 in learning and memory.{29782}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder