RO-31-8220
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
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
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
- Tel
- sales@boylechem.com
- Tel
- 18210857532; 18210857532
- jkinfo@jkchemical.com
- Tel
- 0531-88811783
- sales@trio-pharmatech.com
- Tel
- 0411-62910999 13889544652
- sales@meilune.com
- Tel
- 025-66113011 17798518460
- cfzhang@aikonchem.com
RO-31-8220(138489-18-6)Related Product Information
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- GANGLIOSIDE GD1A DISODIUM SALT
- BISINDOLYLMALEIMIDE VII
- 2,2',3,3',4,4'-hexahydroxy-1,1'-biphenyl-6,6'-dimethanol dimethyl ether
- 3,4-Di-1H-indol-3-yl-1H-pyrrole-2,5-dione
- RO-31-8220
- 1-METHYLINDOLE-3-ACETAMIDE
- RO-31-8220,RO 31-8220 METHANESULFONATE,RO 31-8220 MESYLATE
- 3-Isopropenyl-1-methyl-1H-pyrrole
- RO 31-8220 (BISINDOYLMALEIMIDINE IX)