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555562 Rho Kinase Inhibitor XIII, RKI-1447 - Calbiochem

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555562-10MG
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      Description
      OverviewA cell-permeable pyridylthiazolyl-urea that acts as a potent, ATP site-targeting, Rho Kinase inhibitor (IC50 = 14.5 and 6.2 nM 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 1 µM RKI-1447) or 15 other kinases. Selectively inhibits ROCK-dependent, but not mTORC2-dependent, cellular phosphorylations (effective conc. 0.1 to 1 µM 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 (200 mg/kg/day i.p.) in vivo.
      Catalogue Number555562
      Brand Family Calbiochem®
      Synonyms1-(3-Hydroxybenzyl)-3-(4-(pyridin-4-yl)thiazol-2-yl)urea, Mesylate, 1-(3-Hydroxybenzyl)-3-(4-(pyridin-4-yl)thiazol-2-yl)urea, Methanesulfonate, ROCK Inhibitor XIII
      References
      ReferencesPatel, R.A., et al. 2012. Cancer Res. 72, 5025.
      Product Information
      FormYellowish white solid
      Hill FormulaC₁₆H₁₄N₄O₂S • CH₃SO₃H
      Chemical formulaC₁₆H₁₄N₄O₂S • CH₃SO₃H
      Hygroscopic Hygroscopic
      ReversibleY
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Biological Information
      Primary TargetRho kinases 1 & 2
      Primary Target IC<sub>50</sub>14.5 and 6.2 nM against ROCK1 and ROCK2, respectively
      Purity≥98% by HPLC
      Physicochemical Information
      Cell permeableY
      Storage and Shipping Information
      Ship Code Ambient Temperature Only
      Toxicity Standard Handling
      Storage -20°C
      Protect from Light Protect from light
      Hygroscopic Hygroscopic
      Do not freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Global Trade Item Number
      Catalogue Number GTIN
      555562-10MG 04055977268485