BISINDOLYLMALEIMIDE III Chemical Properties

Boiling point:

708.7±60.0 °C(Predicted)

Density 

1.41±0.1 g/cm3(Predicted)

solubility 

DMSO: soluble; Methanol: soluble

form 

A crystalline solid

pka

8.15±0.60(Predicted)

color 

Brown to reddish brown

BISINDOLYLMALEIMIDE III Usage And Synthesis

Description

Bisindolylmaleimide III was developed as a protein kinase C (PKC) inhibitor with structural similarity to the nonspecific PKC inhibitor staurosporine. At 1 μM, bisindolylmaleimide III inhibits 93% of PKCα kinase activity and also inhibits many other protein kinases including, S6K1, MAPKAP-K1, RSK2 and MSK1 with similar potency. Additionally, it inhibits PDK1, an important kinase in the insulin signaling pathway, with an IC₅₀ value of 3.8 μM.

Uses

Bisindolylmaleimide III is a protein kinase C inhibitor and was also shown to exhibit inhibitory activities towards PDK1, an important kinase in the insulin signaling pathway,

Definition

ChEBI: Bisindolylmaleimide III is a member of maleimides and a member of indoles. It has a role as an EC 2.7.11.13 (protein kinase C) inhibitor. It is functionally related to a maleimide.

IC 50

PKCα

References

[1] PETER D. DAVIS. Inhibitors of protein kinase C. 1. 2,3-bisarylmaleimides[J]. Journal of Medicinal Chemistry, 1992, 35 1: 177-184. DOI: 10.1021/jm00079a024
[2] DAVID SORIANO-CASTELL  Pamela M  Antonio Currais. Defining a pharmacological inhibitor fingerprint for oxytosis/ferroptosis[J]. Free Radical Biology and Medicine, 2021, 171: Pages 219-231. DOI: 10.1016/j.freeradbiomed.2021.05.023

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