HSD1590 是一种有效的 ROCK 抑制剂，对 ROCK1 和 ROCK2 的 IC50 值分别为 1.22 和 0.51 nM。HSD1590 与 ROCK 结合的 Kd 值 小于 2 nM。HSD1590 的细胞毒性低。
HSD1590 is potent ROCK inhibitor, with IC50s of 1.22 and 0.51 nM for ROCK1 and ROCK2, respectively. HSD1590 exhibits single digit nanomolar binding to ROCK (Kds<2 nM). HSD1590 displays low cytotoxicity[1].
HSD1590 (0.5-1 µM; 24 hours) exhibits an impressive attenuation in migration[1].HSD1590 (0.5-10 µM; 12-24 horus) shows that the excellent migration inhibition observed is not due to cell death, but inhibition of live cell migration[1]. Cell Viability Assay[1] Cell Line: MDA-MB-23 cells
[1]. Dayal N, et al. Potently inhibiting cancer cell migration with novel 3H-pyrazolo[4,3-f]quinoline boronic acid ROCK inhibitors. Eur J Med Chem. 2019 Oct 15;180:449-456.
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