125313-65-7
Chemical Structure
Bisindolylmaleimide VIII
Synonym(s): Ro 31-7549; Bis VIII
- No. CAS: 125313-65-7
- Formula:C24H22N4O2
- Molecular Weight:398.46
IUPAC Name: 3-(1-(3-aminopropyl)-1H-indol-3-yl)-4-(1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione
InChIKey: UQHKJRCFSLMWIA-UHFFFAOYSA-N
SMILES: O=C(C(C1=CN(CCCN)C2=C1C=CC=C2)=C3C4=CN(C)C5=C4C=CC=C5)NC3=O
Biological Activity: Bisindolylmaleimide VIII (Ro 31-7549) is a potent and selective protein kinase C (PKC) inhibitor with an IC50 of 158 nM for rat brain PKC. Bisindolylmaleimide VIII has IC50s of 53, 195, 163, 213, and 175 nM for PKC-α, PKC-βI, PKC-βII, PKC-γ, PKC-ε, respectively[1]. Bisindolylmaleimide VIII facilitates Fas-mediated apoptosis and inhibits T cell-mediated autoimmune diseases[1][2].
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Bisindolylmaleimide VIII | Bisindolylmaleimide VIII (Ro 31-7549) is a potent and selective protein kinase C (PKC) inhibitor with an IC50 of 158 nM for rat brain PKC. Bisindolylmaleimide VIII has IC50s of 53, 195, 163, 213, and 175 nM for PKC-α, PKC-βI, PKC-βII, PKC-γ, PKC-ε, respectively. Bisindolylmaleimide VIII facilitates Fas-mediated apoptosis and inhibits T cell-mediated autoimmune diseases. | |||||||||||||||||||||
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- [1]. Wilkinson SE, et al. Isoenzyme specificity of bisindolylmaleimides, selective inhibitors of protein kinase C. Biochem J. 1993 Sep 1;294 ( Pt 2):335-7. [Content Brief]
- [2]. Ohtsuka T, et al. Bisindolylmaleimide VIII enhances DR5-mediated apoptosis through the MKK4/JNK/p38 kinase and the mitochondrial pathways. J Biol Chem. 2002 Aug 9;277(32):29294-303. [Content Brief]
Keywords
