138489-18-6

Basic information

• Product Name: RO-31-8220
• Synonyms: RO-31-8220;BISINDOLYLMALEIMIDE IX, METHANESULFONATE;3-[1-[3-(AMIDINOTHIO)PROPYL-1H-INDOL-3-YL]-3-(1-METHYL-1H-INDOL-3-YL)MALEIMIDE;BISINDOLYLMALEIMIDE IX METHANESULPHONATE SALT;BisindolylMaleiMide IX Mesylate;BisindolylMaleiMide IX . Methansulfonate [Ro 31-8220];Carbamimidothioic acid, 3-[3-[2,5-dihydro-4-(1-methyl-1H-indol-3-yl)-2,5-dioxo-1H-pyrrol-3-yl]-1H-indol-1-yl]propyl ester, methanesulfonate (1:1);Ro31-8220MsOH
• CAS NO: 138489-18-6
• Molecular Formula: C25H23N5O2S
• Molecular Weight: 457.55
• Product Categories: inhibitor;TGF-beta/Smad;Inhibitors;Smad;TGF-beta
• Mol File: 138489-18-6.mol
• Article Data: 2

Chemical Properties

• Appearance: /
• Storage Temp.: 0-6°C
• CAS DataBase Reference: RO-31-8220(CAS DataBase Reference)
• NIST Chemistry Reference: RO-31-8220(138489-18-6)
• EPA Substance Registry System: RO-31-8220(138489-18-6)

Safety Data

• Hazardous Substances Data: 138489-18-6(Hazardous Substances Data)

Usage

Description

Ro 31-8220 mesylate is a potent PKC inhibitor, inhibits PKCα, PKCβI, PKCβII, PKCγ, PKCε and rat brain PKC with IC50 values of 5, 24, 14, 27, 24 and 23 nM, also inhibits MAPKAP -K1b, MSK1, S6K1 and GSK3β with IC50 of 3, 8, 15, 38 nM.

General Description

Ro 31-8220 is a bisindolylmaleimide derivative of staurosporine. Ro 31-8220 blocks MAP kinase phosphatase-1 (MKP-1) expression, induces c-Jun expression and stimulates Jun N-terminal Kinase (JNK1). It has immunosuppressive properties.

Biochem/physiol Actions

Inhibitor of GRK-5 (G protein-coupled receptor kinase); PKC (protein kinase C); MAPKAP kinase 1β and p70 S6 kinase.

Upstream product

• 125315-06-2 3-(1-methyl-3-indolyl)-4-<1-<3-(methylsulfonyloxy)propyl>-3-indolyl>-1H-pyrrole-2,5-dione 
• 125314-97-8 3-<1-(3-acetoxypropyl)-3-indolyl>-4-(1-methyl-3-indolyl)-2,5-furandione 
• 125313-60-2 3-[1-(3-hydroxy-propyl)-1H-indol-3-yl)-4-(1-methyl-1H-indol-3-yl)-pyrrole-2,5-dione 
• 125314-98-9 N-(3-acetoxypropyl)-indole 
• 120-72-9 indole 
• 17356-08-0 thiourea 

Related news

Dissociation of tyrosine phosphorylation and activation of phosphoinositide phospholipase C induced by the protein kinase C inhibitor RO-31-8220 (cas 138489-18-6) in Swiss 3T3 cells treated with platelet-derived growth factor08/26/2019

Platelet-derived growth factor (PDGF) stimulates the hydrolysis of phosphatidylinositol 4,5-bisphosphate (Ptd InsP2) via phospholipase C-γ1 (PLC-γ1) in Swiss 3T3 cells. Treatment of cells with the protein kinase C (PKC) inhibitor Ro-31-8220 greatly decreased PDGF-induced tyrosine phosphorylati...detailed

Relevant articles and documents

Inhibitors of Protein Kinase C. 2. Substituted Bisindolylmaleimides with Improved Potency and Selectivity

A hypothetical mode of inhibition of protein kinase C (PKC) by the natural product staurosporine has been used as a basis for the design of substituted bisindolylmaleimides with improved potency over the parent compound.Structure-activity relationships were consistent with the interaction of a cationic group in the inhibitor with a carboxylate group in the enzyme, and the most potent compound had a Ki of 3 nM.The inhibitors were competitive with ATP but inhibited cAMP-dependent protein kinase (PKA) only at much higher concentrations despite the extensive sequence homology between ATP-binding regions of PKA and PKC.There compounds were evaluated further and found to inhibit a human allogeneic mixed lymphocyte reaction pointing to the potential utility of PKC inhibitors in immunosuppressive therapy.One of these compounds was orally absorbed in the rat and represents an attractive lead in the development of PKC inhibitors as drugs.