Ro 31-8220 (mesylate)

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]

Product Name Alternative

Ro 31-8220 methanesulfonate; Bisindolylmaleimide IX mesylate

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

JNK; PKC

Type

Reference compound

Related Pathways

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

Applications

Cancer-Kinase/protease

Field of Research

Neurological Disease; Cardiovascular Disease; Cancer

Assay Protocol

https://www.medchemexpress.com/Ro-31-8220-mesylate.html

Concentration

10mM

Purity

99.57

Solubility

DMSO : 35.71 mg/mL (ultrasonic)

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

Precautions

H302, H315, H319, H335

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.