GSK429286A是ROCK1和ROCK2的選擇性抑制劑，IC50值分別為14 nM和63nM[1]。 rho-激酶(ROCK)是AGC(蛋白激酶A、蛋白激酶G和蛋白激酶C)家族的成員，在促進(jìn)肌動(dòng)蛋白-肌球蛋白介導(dǎo)的收縮力產(chǎn)生中發(fā)揮重要作用[2]。 GSK429286A是一種有效的巖石抑制劑，其活性與已報(bào)道的巖石抑制劑Y27632不同。使用GST方法，表明GSK429286A處理(10微米)通過(guò)抑制介導(dǎo)該磷酸化過(guò)程的ROCK來(lái)增加Thr850處的MYPT磷酸化[3]。 在患有自發(fā)性高血壓的雄性Sprague-Dawley大鼠模型中，口服GSK429286A (30 mg/kg)可顯著降低平均動(dòng)脈壓，在治療近2小時(shí)后，最大降幅為50 mmHg。

產(chǎn)品性質(zhì)：

Cas No.:864082-47-3

別名:N-(6-氟-1H-吲唑-5-基)-2-甲基-6-氧代-4-[4-(三氟甲基)苯基]-1,4,5,6-四氫-3-吡啶甲酰胺

化學(xué)名: N-(6-fluoro-1H-indazol-5-yl)-6-methyl-2-oxo-4-[4-(trifluoromethyl)phenyl]-3,4-dihydro-1H-pyridine-5-carboxamide

Canonical SMILES:CC1=C(C(CC(=O)N1)C2=CC=C(C=C2)C(F)(F)F)C(=O)NC3=C(C=C4C(=C3)C=NN4)F

分子式:C21H16F4N4O2

分子量:432.37

溶解度:≥ 21.6mg/mL in DMSO, ≥ 2.73 mg/mL in EtOH with ultrasonic and warming

儲(chǔ)存條件:Store at -20°C

注意事項(xiàng)：

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References:

[1].Nichols, R.J., et al., Substrate specificity and inhibitors of LRRK2, a protein kinase mutated in Parkinson's disease. Biochem J, 2009. 424(1): p. 47-60.

[2].Shi, J., et al., Distinct roles for ROCK1 and ROCK2 in the regulation of cell detachment. Cell Death Dis, 2013. 4: p. e483.

[3].Davis, D.A., et al., Increased therapeutic potential of an experimental anti-mitotic inhibitor SB715992 by genistein in PC-3 human prostate cancer cell line. BMC Cancer, 2006. 6: p. 22.

[4]. Goodman, K.B., et al., Development of dihydropyridone indazole amides as selective Rho-kinase inhibitors. J Med Chem, 2007. 50(1): p. 6-9.