|
|
| | RO 31-8220 METHANESULFONATE Basic information |
| Product Name: | RO 31-8220 METHANESULFONATE | | Synonyms: | BISINDOLYLMALEIMIDE IX METHANESULFONATE;BISINDOYLMALEIMIDINE IX METHANESULFONATE;RO-31-8220;RO 31-8220 MESYLATE;RO 31-8220 METHANESULFONATE;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;3-[1-3-(AMIDINOTHIO)PROPYL-1H-INDOL-3-YL]-3-(1-METHYL-1H-INDOL-3-YL) MALEIMIDE;3-[1-[3-(AMIDINOTHIO)PROPYL-1H-INDOL-3-YL]-3-(1-METHYL-1H-INDOL-3-YL)MALEIMIDE METHANESULFONATE | | CAS: | 125314-64-9 | | MF: | C25H23N5O2S | | MW: | 457.55 | | EINECS: | | | Product Categories: | Protein Kinase | | Mol File: | 125314-64-9.mol |  |
| | RO 31-8220 METHANESULFONATE Chemical Properties |
| density | 1.42±0.1 g/cm3(Predicted) | | storage temp. | 2-8°C | | solubility | H2O: 7.3 mg/mL | | pka | 7.90±0.60(Predicted) | | form | solid | | color | orange to red |
| | RO 31-8220 METHANESULFONATE Usage And Synthesis |
| Uses | Ro 31-8220 Mesylate is a protein kinase C (PKC) inhibitor. | | Definition | ChEBI: Ro 31-8220 is an imidothiocarbamic ester, a member of indoles and a member of maleimides. It has a role as an EC 2.7.11.13 (protein kinase C) inhibitor. It is functionally related to a maleimide. | | Biological Activity | Protein kinase C inhibitor, with activity at other protein kinases (IC 50 values are 33, 3, 8, 15 and 38 nM for PKC α , MAPKAP-K1b, MSK1, GSK3 β and S6K1 respectively). Activates JNK and glycogen synthase, and inhibits MAPK and ERK2, in rat adipocytes and L6 myotubes. Also inhibits voltage-dependent Na + channels in the micromolar range. | | references | [1]. wilkinson se, parker pj, nixon js. isoenzyme specificity of bisindolylmaleimides, selective inhibitors of protein kinase c. biochem j, 1993, 294 ( pt 2): 335-337.
[2]. beltman j, mccormick f, cook sj. the selective protein kinase c inhibitor, ro-31-8220, inhibits mitogen-activated protein kinase phosphatase-1 (mkp-1) expression, induces c-jun expression, and activates jun n-terminal kinase. j biol chem, 1996, 271(43): 27018-27024.
[3]. geiselhart l, conti dj, freed bm. ro 31-8220, a novel protein kinase c inhibitor, inhibits early and late t cell activation events. transplantation, 1996, 61(11): 1637-1642.
[4]. standaert ml, bandyopadhyay g, antwi ek, et al. ro 31-8220 activates c-jun n-terminal kinase and glycogen synthase in rat adipocytes and l6 myotubes. comparison to actions of insulin. |
| | RO 31-8220 METHANESULFONATE Preparation Products And Raw materials |
|