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Biological Data
| Biological description | Potent and selective protein kinase C inhibitor (IC50 = 158 nM). Displays selectivity for PKC-α over PKC-β1, PKC-βII, PKC-γ and PKC-ε (IC50 values are 53, 195, 163, 213, 175 nM respectively). Facilitates Fas-mediated apoptosis and enhances DR5 mediated apoptosis. Also CDK2 antagonist (IC50 = 600 nM). |
Solubility & Handling
| Solubility overview | Soluble in DMSO or water |
| Important | This product is for RESEARCH USE ONLY and is not intended for therapeutic or diagnostic use. Not for human or veterinary use. |
Chemical Data
| Chemical name | Ro 31-7549 acetate |
| Chemical structure | |
| Molecular Formula | C24H22N4O2.C2H4O2 |
| PubChem identifier | 9868770 |
| SMILES | CC(=O)O.CN1C=C(C2=CC=CC=C21)C3=C(C(=O)NC3=O)C4=CN(C5=CC=CC=C54)CCCN |
References for Bisindolylmaleimide VIII
References are publications that support the biological activity of the product
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Proteome-wide identification of cellular targets affected by bisindolylmaleimide-type protein kinase C inhibitors.
Brehmer D et al (2004) Mol Cell Proteomics 3(5) : 490-500. -
Bisindolylmaleimide VIII enhances DR5-mediated apoptosis through the MKK4/JNK/p38 kinase and the mitochondrial pathways.
Ohtsuka T et al (2002) J Biol Chem 277(32) : 29294-303. -
Bisindolylmaleimide VIII facilitates Fas-mediated apoptosis and inhibits T cell-mediated autoimmune diseases.
Zhou T et al (1999) Nat Med 5(1) : 42-8. -
Isoenzyme specificity of bisindolylmaleimides, selective inhibitors of protein kinase C.
Wilkinson SE et al (1993) Biochem J 294 ( Pt 2) : 335-7.
Potent, selective PKC inhibitor