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

Catalog No. 55556210MG Shop All MilliporeSigma Products
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Catalog No. 55-556-210MG Supplier MilliporeSigma™ Supplier No. 55556210MG

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 .
TRUSTED_SUSTAINABILITY

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
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