產(chǎn)品屬性:
產(chǎn)品名稱 | SB-431542 (hydrate) |
規(guī)格 | 1 mg、5 mg、10 mg、25 mg |
貨號 | EY-01Y13748 |
Cas No.: N/A
別名: N/A
化學(xué)名: N/A
分子式: C22H16N4O3.XH2O
分子量: 384.4
溶解度: DMF: 20 mg/ml,DMSO: 20 mg/ml,DMSO:PBS(pH7.2) (1:1): 0.5 mg/ml,Ethanol: 2 mg/ml
儲存條件: Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
產(chǎn)品描述:
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.4,51.Callahan, J.F., Burgess, J.L., Fornwald, J.A., et al.Identification of novel inhibitors of the transforming growth factor ?1 (TGF-?1) type 1 receptor (ALK5)Journal of Medicinal Chemistry45(5)999-1001(2002)
2.Laping, N.J., Grygielko, E., Mathur, A., et al.Inhibition of Transforming Growth Factor (TGF)-?1-Induced Extracellular Matrix with a Novel Inhibitor of the TGF-? Type I Receptor Kinase Activity: SB-431542Molecular Pharmacology62(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 ALK7Molecular Pharmacology62(1)65-74(2002)
4.James, D., Levine, A.J., Besser, D., et al.TGF?/activin/nodal signaling is necessary for the maintenance of pluripotency in human embryonic stem cellsDevelopment1321273-1282(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 signalingNature Biotechnology27(3)275-280(2009)
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