683775-59-9
Chemical Structure
Bisindolylmaleimide III hydrochloride
- CAS 番号: 683775-59-9
- Formula:C23H21ClN4O2
- Molecular Weight:420.89
IUPAC Name: 3-(1-(3-aminopropyl)-1H-indol-3-yl)-4-(1H-indol-3-yl)-1H-pyrrole-2,5-dione hydrochloride
InChIKey: NXIKRXJEVAWDAX-UHFFFAOYSA-N
SMILES: O=C1NC(C(C2=CN(CCCN)C3=C2C=CC=C3)=C1C4=CNC5=C4C=CC=C5)=O.Cl
Biological Activity: Bisindolylmaleimide III hydrochloride is a protein kinase C (PKC) inhibitor with IC50 values of 0.26, 5.7, and 6 μM against PKCα, PKCδ, and PKCμ, respectively. Bisindolylmaleimide III hydrochloride also exhibits inhibitory activity against other off-targets, with IC50 values of 0.17, 1, and 2 μM against SLK, adenosine kinase (AK), and CDK2, respectively; its Ki for NQO2 is 16.5 μM. Bisindolylmaleimide III hydrochloride selectively binds to activated Rsk1 following EGF stimulation, and serves as a tool for detecting the activation status of intracellular Rsk1 and PKCα, as well as for functional analysis of SLK. Bisindolylmaleimide III hydrochloride can be used in studies of signal transduction and colorectal cancer[1][2][3].
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Bisindolylmaleimide III hydrochloride | Bisindolylmaleimide III hydrochloride is a protein kinase C (PKC) inhibitor with IC50 values of 0.26, 5.7, and 6 μM against PKCα, PKCδ, and PKCμ, respectively. Bisindolylmaleimide III hydrochloride also exhibits inhibitory activity against other off-targets, with IC50 values of 0.17, 1, and 2 μM against SLK, adenosine kinase (AK), and CDK2, respectively; its Ki for NQO2 is 16.5 μM. Bisindolylmaleimide III hydrochloride selectively binds to activated Rsk1 following EGF stimulation, and serves as a tool for detecting the activation status of intracellular Rsk1 and PKCα, as well as for functional analysis of SLK. Bisindolylmaleimide III hydrochloride can be used in studies of signal transduction and colorectal cancer. | |||||||||||||||||||||
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- [1]. Brehmer D, et al. Proteome-wide identification of cellular targets affected by bisindolylmaleimide-type protein kinase C inhibitors. Molecular & cellular proteomics : MCP. 2004 May;3(5):490-500. [Content Brief]
- [2]. Saito Y, et al. Role of ecto-kinase in phorbol ester-enhanced growth hormone-binding protein release from human IM-9 cells. Molecular and cellular endocrinology. 1999 Jun 25;152(1-2):65-72. [Content Brief]
- [3]. Pajak B, et al. Bisindolylmaleimide IX facilitates extrinsic and initiates intrinsic apoptosis in TNF-alpha-resistant human colon adenocarcinoma COLO 205 cells. Apoptosis : an international journal on programmed cell death. 2008 Apr;13(4):509-22. [Content Brief]
