| Identification | Back Directory | [Name]
RO 31-8220 METHANESULFONATE | [CAS]
125314-64-9 | [Synonyms]
RO-31-8220
RO 31-8220 MESYLATE
BisindolylMaleiMide IX
Bisindoylmaleimidine IX
RO 31-8220 METHANESULFONATE
Ro 31-8220 methanesulfonate salt
BISINDOLYLMALEIMIDE IX METHANESULFONATE
BISINDOYLMALEIMIDINE IX METHANESULFONATE
Ro 31-8220 mesylate (Bisindolylmaleimide IX)
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] meslate
2-[1-[3-(AMIDINOTHIO)PROPYL]-1H-INDOL-3-YL]-3-(1-METHYLINDOL-3-YL)-MALEIMIDE METHANESULFONATE
3-[1-[3-(AMIDINOTHIO)PROPYL-1H-INDOL-3-YL]-3-(1-METHYL-1H-INDOL-3-YL)MALEIMIDE METHANESULFONATE
2-{1-[3-(Amidinothio)propyl]-1H-indol-3-yl}-3-(1-methylindol-3-yl)maleimide methanesulfonate salt
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
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 | [Molecular Formula]
C25H23N5O2S | [MDL Number]
MFCD03788207 | [MOL File]
125314-64-9.mol | [Molecular Weight]
457.55 |
| Chemical Properties | Back Directory | [density ]
1.42±0.1 g/cm3(Predicted) | [storage temp. ]
2-8°C
| [solubility ]
H2O: 7.3 mg/mL
| [form ]
solid
| [pka]
7.90±0.60(Predicted) | [color ]
orange to red
|
| Hazard Information | Back Directory | [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. | [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) | [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. |
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