HSD1590

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].

Research Areas >> Cancer

Signaling Pathways >> Cell Cycle/DNA Damage >> ROCK

Signaling Pathways >> Stem Cell/Wnt >> ROCK

Signaling Pathways >> TGF-beta/Smad >> ROCK

ROCK1:1.22 nM (IC50)

ROCK2:0.51 nM (IC50)

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 Concentration: 0.5-10 µM Incubation Time: 12-24 hours Result: Exhibited approximately 80% viability at 12 hours and yielded an overall viability of 63% at 24 h.

[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.