Product Description: Ro 31-8220 mesylate is a potent PKC inhibitor, with IC50s of 5, 24, 14, 27, 24 and 23 nM for PKCα, PKCβI, PKCβII, PKCγ, PKCε and rat brain PKC, respectively. Ro 31-8220 also significantly inhibits MAPKAP-K1b, MSK1, S6K1 and GSK3β (IC50s, 3, 8, 15, and 38 nM, respectively), with no effect on MKK3, MKK4, MKK6 and MKK7.
Applications: Cancer-Kinase/protease
Formula: C26H27N5O5S2
Citations: bioRxiv. 2024 Jul 25./EMBO Mol Med. 2022 Dec 13;e16373./Front Immunol. 2021 Feb 2;11:625542./Harvard Medical School LINCS LIBRARY/Life Metab. 2025 Jan 29./Aging Cell. 2020 Oct;19(10):e13217./Aging Cell. 2022 Feb 23;e13573./Biomolecules. 2022, 12(3), 426./FASEB J. 2019 Feb;33(2):2435-2450. /J Clin Invest. 2021 Dec 29;e150101./Mol Med Rep. 2017 Nov;16(5):5924-5930./Nat Commun. 2018 Sep 11;9(1):3688./Neurogastroenterol Motil. 2020 Oct;32(10):1514-1528.
References: [1]Wilkinson SE, et al. Isoenzyme specificity of bisindolylmaleimides, selective inhibitors of protein kinase C. Biochem J. 1993 Sep 1;294 (Pt 2):335-7./[2]Davies SP, et al. Specificity and mechanism of action of some commonly used protein kinase inhibitors. Biochem J. 2000 Oct 1;351(Pt 1):95-105./[3]Tian F, et al. Inhibition of protein kinase C protects against paraoxon-mediated neuronal cell death. Neurotoxicology. 2007 Jul;28(4):843-9. Epub 2007 Apr 20./[4]Hambleton M, et al. Pharmacological- and gene therapy-based inhibition of protein kinase Calpha/beta enhances cardiac contractility and attenuates heart failure. Circulation. 2006 Aug 8;114(6):574-82.
CAS Number: 138489-18-6
Molecular Weight: 553.65
Compound Purity: 99.57
Research Area: Neurological Disease; Cardiovascular Disease; Cancer
Solubility: DMSO : 35.71 mg/mL (ultrasonic)
Target: PKC
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