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抑制剂描述:

产品名称:SB-431542

产品别名:见爱必信官网

英文别名:SB-431542

靶点:TGF-β Receptor

CAS:301836-41-9

纯度:>98%

外观:见爱必信官网

保存方法:Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.

描述:

SB-431542 is a potent and selective inhibitor of ALK5 with IC50 of 94 nM, 100-fold more selective for ALK5 than p38 MAPK and other kinases.

溶解性: DMSO : 38.4 mg/mL(100 mM)
Ethanol : 3.8 mg/mL(10 mM)

体外研究:

SB-431542 inhibits TGF-beta1-induced fibronectin mRNA formation while displaying no measurable cytotoxicity in the 48 h XTT assay. SB-431542 (1 μM) significantly reduced the TGFβ–induced nuclear accumulation of Smad proteins. The IC50 for inhibiting TGFβ–induced nuclear fluorescence is approximately 50 nM. BMP-stimulated Smad1 nuclear fluorescence in MG63 cells was unaffected by SB-431542. the synergistic action of two inhibitors of SMAD signaling, Noggin and SB431542, is sufficient to induce rapid and complete neural conversion of >80% of hES cells under adherent culture conditions.

体内研究:SB-431542 augmented the capacity of bone marrow dendritic cells (BM-DCs) and human DCs to incorporate FITC-conjugated dextran. Intraperitoneal administration of SB-431542 initiated 3 and 7 days after the implantation of colon-26 cancer cells into the peritoneal cavity of BALB/c mice significantly induced CTL activity against colon-26. SB-431542 significantly inhibited lung metastasis from transplanted 4T1 mammary tumors in Balb/c mice.

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