货号 | 13031-1mg |
描述 | SB-431542 is a potent and selective inhibitor of the TGF-β1 receptor ALK5 (IC50 = 94 nM)1. It is a less potent antagonist of ALK4 (IC50 = 140 nM)2 and ALK7.3 It does not affect the BMP receptors ALK2, ALK3, ALK6, or a panel of other kinases tested.3 SB-431542 specifically blocks Smad signaling, reducing gene expression relevant to fibrosis and cancer.3 Through its effects on ALK/Smad signaling, SB-431542 suppresses renewal in embryonic and induced pluripotent stem cells and promotes their differentiation.4,5 |
供应商 | Cayman |
应用文献 | |
1.Callahan, J.F.,Burgess, J.L.,Fornwald, J.A., et al. Identification of novel inhibitors of the transforming growth factor ß1 (TGF-ß1) type 1 receptor (ALK5). Journal of Medicinal Chemistry 45(5), 999-1001 (2002). 2.Laping, N.J.,Grygielko, E.,Mathur, A., et al. Inhibition of Transforming Growth Factor (TGF)-ß1-Induced Extracellular Matrix with a Novel Inhibitor of the TGF-ß Type I Receptor Kinase Activity: SB-431542. Molecular Pharmacology 62(1), 58-64 (2002). 3.Inman, G.J.,Nicolás, F.J.,Callahan, J.F., et al. SB-431542 is a potent and specific inhibitor of transforming growth factor-β superfamily type I activin receptor-like kinase (ALK) receptors ALK4, ALK5, and ALK7. Molecular Pharmacology 62(1), 65-74 (2002). 4.James, D.,Levine, A.J.,Besser, D., et al. TGFß/activin/nodal signaling is necessary for the maintenance of pluripotency in human embryonic stem cells. Development 132, 1273-1282 (2005). 5.Chambers, S.M.,Fasano, C.A.,Papapetrou, E.P., et al. Highly efficient neural conversion of human ES and iPS cells by dual inhibition of SMAD signaling. Nature Biotechnology 27(3), 275-280 (2009). | |
运输条件 | Room temperature in continental US; may vary elsewhere |
存放说明 | -20 |
纯度 | ≥98% |
计算分子量 | 384.4 |
分子式 | C22H16N4O3 |
CAS号 | 301836-41-9 |
稳定性 | ≥ 2 years |
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