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| 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 | | EINECS: | | | 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 | | InChIKey | SAWVGDJBSPLRRB-UHFFFAOYSA-N | | SMILES | CS(O)(=O)=O.Cn1cc(C2=C(C(=O)NC2=O)c3cn(CCCSC(N)=N)c4ccccc34)c5ccccc15 |
| WGK Germany | WGK 3 | | HS Code | 2933790090 | | Storage Class | 11 - Combustible Solids |
| | 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-31-8220 Preparation Products And Raw materials |
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