A cell-permeable pyridylthiazolyl-urea that acts as a potent, ATP site-targeting, Rho Kinase inhibitor (IC50 = 14.5 and 6.2nM against ROCK1 and ROCK2, respectively), displaying much reduced potency against PKA, PKN1/PRK1, p70S6K/RPS6kB1, AKT1, MRCKa/CDC42BPA (85.5%, 80.5%, 61.9%, 56%, and 50.4% inhibition, respectively, by 1uM RKI-1447) or 15 other kinases. Selectively inhibits ROCK-dependent, but not mTORC2-dependent, cellular phosphorylations (effective conc. 0.1-1uM in MDA-MB-231, MDA-MB-468, and H1299 cultures). Shown to be efficacious in suppressing established tumor expansion in a murine ErbB2 mammary cancer model (200mg/kg/day i.p.) in vivo.
Synonyms:1-(3-Hydroxybenzyl)-3-(4-(pyridin-4-yl)thiazol-2-yl)urea, Methanesulfonate, ROCK Inhibitor XIII, 1-(3-Hydroxybenzyl)-3-(4-(pyridin-4-yl)thiazol-2-yl)urea, Mesylate
Molecular Formula:C₁₆H₁₄N₄O₂S • CH₃SO₃H
Solubility:DMSO
Primary Target:Rho kinases 1 & 2
Primary Target IC50:14.5 and 6.2 nM against ROCK1 and ROCK2, respectively.
Molar Mass:422.5
Purity:≥98% (HPLC)
Form:Supplied as a yellowish white solid.
Storage and Stability:Store at -20°C under inert atmosphere. For maximum recovery of product, centrifuge the original vial prior to removing the cap.
