Ro 31-8220 (mesylate) (Standard)

Ro 31-8220 mesylate (Standard) is the analytical standard of Ro 31-8220 mesylate (HY-13866) . This product is intended for research and analytical applications. 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. Ro 31-8220 mesylate can also inhibit the expression of MKP-1, induce the expression of c-Jun, and activate JNK, and these effects possess pharmacological properties independent of PKC[1][2][3][4][5].

Product Specifications

CAS Number

[138489-18-6]

UNSPSC

12352100

Target

JNK; PKC; Reference Standards

Related Pathways

Epigenetics; MAPK/ERK Pathway; Others; TGF-beta/Smad

Field of Research

Neurological Disease; Cardiovascular Disease; Cancer

Smiles

NC(SCCCN1C=C(C2=C(C3=CN(C)C4=C3C=CC=C4)C(NC2=O)=O)C5=C1C=CC=C5)=N.CS(=O)(O)=O

Molecular Formula

C26H27N5O5S2

Molecular Weight

553.65

References & Citations

[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.|[5]Beltman J, et al. The selective protein kinase C inhibitor, Ro-31-8220, inhibits mitogen-activated protein kinase phosphatase-1 (MKP-1) expression, induces c-Jun expression, and activates Jun N-terminal kinase. J Biol Chem. 1996 Oct 25;271 (43) :27018-24.