Bisindolylmaleimide VIIIA selective PKC inhibitor

Bisindolylmaleimide VIII (CAS 138516-31-1)

Bisindolylmaleimide VIII | CAS 138516-31-1 is rated 5.0 out of 5 by 1.
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Synonym: Ro 31-7549 acetate
Application: A selective PKC inhibitor
CAS Number: 138516-31-1
Purity: ≥98%
Molecular Weight: 458.60
Molecular Formula: C24H22N4O2•C2H4O2
* Refer to Certificate of Analysis for lot specific data (including water content).
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Bisindolylmaleimide VIII is a selective PKC (protein kinase C) inhibitor, with observed binding activity to dystrophia myotonica protein kinase (DMPK). Bisindolylmaleimide VIII is suggested as being slightly more specific for PKC α over PKC β, PKC γ, and PKC ε isozymes (IC50 = 53, 195, 213, and 275 respectively). The compound has been shown to improve DR5-mediated apoptosis through the MKK4/JNK/p38 kinase. When bisindolylmaleimide VIII is combined with TRA-8 it can activate c-Jun N-terminal kinase (JNK) and p38 mitogen-activated protein kinase. Studies have shown that bisindolylmaleimide VIII enhance Fas-mediated apoptosis in both human astrocytoma 1321N1 cells and in Molt-4T cells.


References

1. Zhou, T., et al. 1999. Nat. Med. 5: 42-48. PMID: 9883838
2. Ohtsuka, T. and Zhou, T. 2002. J. Biol. Chem. 277: 29294-29303. PMID: 12034736
3. Lautrette, C., et al. 2006. Apoptosis. 11: 1195-1204. PMID: 16699962
4. Elkins, J.M., et al. 2009. Protein Sci. 18: 782-791. PMID: 19309729

Appearance :
Crystalline
Physical State :
Solid
Solubility :
Soluble in DMSO, methanol, water, and 100% ethanol (slightly).
Storage :
Store at -20° C
Boiling Point :
693° C at 760 mmHg (Predicted)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
PubChem CID :
9868770
MDL Number :
MFCD00909467
SMILES :
CC(=O)O.CN1C=C(C2=CC=CC=C21)C3=C(C(=O)NC3=O)C4=CN(C5=CC=CC=C54)CCCN

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Certificate of Analysis

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Bisindolylmaleimide VIII  Product Citations

See how others have used Bisindolylmaleimide VIII. Click on the entry to view the PubMed entry .

Citations 1 to 2 of 2 total

PMID: # 25355318  Wang, Y. et al. 2014. The Journal of biological chemistry. 289: 35795-805.

PMID: # 19309729  Elkins, JM. et al. 2009. Protein Sci. 18: 782-791.

Citations 1 to 2 of 2 total
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Rated 5 out of 5 by from Elkins JM; et al Elkins JM; et al. (PubMed ID: 19309729) determined that the Dystrophia myotonica protein kinase bound to its inhibitor, bisindolylmaleimide VIII (BIM-8), occupies the ATP site and has analogous binding mode as observed in PDK1. -SCBT Publication Review
Date published: 2015-01-22
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