ChemicalBook--->CAS DataBase List--->138489-18-6

138489-18-6

138489-18-6 Structure

138489-18-6 Structure
IdentificationBack Directory
[Name]

RO-31-8220
[CAS]

138489-18-6
[Synonyms]

CS-1132
RO-31-8220
Ro31-8220MsOH
Ro 31-8220 Mesylat
Ro 31-8220/Ro318220
RO-31-8220 USP/EP/BP
BisindolylMaleiMide IX Mesylate
BISINDOLYLMALEIMIDE IX, METHANESULFONATE
Ro-31-8220 - CAS 138489-18-6 - Calbiochem
Bisindolylmaleimide IX (Ro 31-8220 Mesylate)
BISINDOLYLMALEIMIDE IX METHANESULPHONATE SALT
BisindolylMaleiMide IX . Methansulfonate [Ro 31-8220]
RO 31-8220 METHANESULFONATE; BISINDOLYLMALEIMIDE IX MESYLATE;RO318220
3-[1-[3-(AMIDINOTHIO)PROPYL-1H-INDOL-3-YL]-3-(1-METHYL-1H-INDOL-3-YL)MALEIMIDE
3-[3-[2,5-Dihydro-4-(1-methyl-1H-indol-3-yl)-2,5-dioxo-1H-pyrrol-3-yl]-1H-indol-1-yl]propyl carbamimidothioic acid ester mesylate
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)
[Molecular Formula]

C25H23N5O2S
[MDL Number]

MFCD00236436
[MOL File]

138489-18-6.mol
[Molecular Weight]

457.55
Questions And AnswerBack Directory
[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.
Chemical PropertiesBack Directory
[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
[InChIKey]

SAWVGDJBSPLRRB-UHFFFAOYSA-N
[SMILES]

CS(O)(=O)=O.Cn1cc(C2=C(C(=O)NC2=O)c3cn(CCCSC(N)=N)c4ccccc34)c5ccccc15
Safety DataBack Directory
[WGK Germany ]

WGK 3
[HS Code ]

2933790090
[Storage Class]

11 - Combustible Solids
Hazard InformationBack Directory
[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
Spectrum DetailBack Directory
[Spectrum Detail]

RO-31-8220(138489-18-6)1HNMR
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