MilliporeSigma™ Calbiochem™ Rho Kinase Inhibitor XIII, RKI-1447

Description

A cell-permeable pyridylthiazolyl-urea that acts as a potent, ATP site-targeting, Rho Kinase inhibitor (IC₅₀ =

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%, 56.0%, and 50.4% inhibition, respectively, by 1μM RKI-1447) or 15 other kinases. Selectively inhibits ROCK-dependent, but not mTORC2-dependent, cellular phosphorylations (effective conc. 0.1 to 1μM 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 .

Specifications

• Color: Yellowish White
• Description: 98% by HPLC
• Target Proteins: Rho kinases 1 & 2
• Molecular Formula: C₁₆H₁₄N₄O₂S·CH₃SO₃H
• Formula Weight: 422.5g/mol
• Solubility: DMSO
• Content And Storage: Hygroscopic, Protect from light
• Form: Solid
• Quantity: 10 mg