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抑制劑描述：

產(chǎn)品名稱：SB-431542

產(chǎn)品別名：4-[4-(3,4-亞甲二氧基苯基)-5-(2-吡啶基)-1H-咪唑-2-基]-苯甲酰胺

英文別名：SB431542;SB 431542

靶點(diǎn)：ALK4；ALK7；ALK5

CAS：301836-41-9

純度：>98%

外觀：黃色至粉色固體

保存方法：store at -20℃ for one year（Powder）； in DMSO or others solvent store at 2-4℃ for two weeks, at -80℃ for six months.

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)

體外研究：

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.

體內(nèi)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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