Basic information Description Safety Supplier Related
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RO-31-8220

Basic information Description Safety Supplier Related

RO-31-8220 Basic information

Product Name:
RO-31-8220
Synonyms:
  • RO-31-8220
  • Ro 31-8220 Mesylat
  • 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)
CAS:
138489-18-6
MF:
C25H23N5O2S
MW:
457.55
Product Categories:
  • Smad
  • TGF-beta
  • Inhibitors
  • TGF-beta/Smad
  • inhibitor
Mol File:
138489-18-6.mol
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RO-31-8220 Chemical Properties

storage temp. 
2-8°C
solubility 
DMSO:52.77(Max Conc. mg/mL);95.31(Max Conc. mM)
DMF:25.0(Max Conc. mg/mL);45.15(Max Conc. mM)
DMF:PBS (pH 7.2) (1:9):0.1(Max Conc. mg/mL);0.18(Max Conc. mM)
Ethanol:2.77(Max Conc. mg/mL);5.0(Max Conc. mM)
form 
Red solid
color 
Red
biological source
synthetic (organic)
Water Solubility 
water: 1mg/mL
DMSO: 100mg/mL
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Safety Information

HS Code 
2933790090
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RO-31-8220 Usage And Synthesis

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.

Uses

Ro 31-8220 Mesylate is a protein kinase C (PKC) inhibitor.

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.

in vivo

Ro 31-8220 (6 mg/kg/d, s.c.) is well tolerated, and has half-life of 5.7 hours in mice. Ro 31-8220-treated MLP?/? mice show a dramatic rescue in fractional shortening after treatment for 6 weeks, but the WT mice shows no change[4].

IC 50

PKC-α: 5 nM (IC50); PKC-βII: 14 nM (IC50); PKC-βI: 24 nM (IC50); PKC-ε: 24 nM (IC50); PKC-γ: 27 nM (IC50); Rat Brain PKC: 23 nM (IC50); MAPKAP-K1b: 3 nM (IC50); MSK1: 8 nM (IC50); S6K1: 15 nM (IC50); GSK3β: 38 nM (IC50)

storage

+4°C

RO-31-8220Supplier

Shanghai Boyle Chemical Co., Ltd.
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Email
sales@boylechem.com
J & K SCIENTIFIC LTD.
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18210857532; 18210857532
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jkinfo@jkchemical.com
Jinan Trio PharmaTech Co., Ltd.
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0531-88811783
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sales@trio-pharmatech.com
Dalian Meilun Biotech Co., Ltd.
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0411-62910999 13889544652
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sales@meilune.com
Jiangsu Aikon Biopharmaceutical R&D co.,Ltd.
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025-66113011 17798518460
Email
cfzhang@aikonchem.com