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.
For research use only. We do not sell to patients.
- CAS No.: 683775-59-9
- Formula: C23H21ClN4O2
- Molecular Weight:420.89
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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PKCα 0.26 μM (IC50) |
PKCδ 5.7 μM (IC50) |
PKCμ 6 μM (IC50) |
cdk2/cyclin A 1 μM (IC50) |
NQO2 16.5 μM (Ki) |
Bisindolylmaleimide III (75 min) hydrochloride potently and selectively inhibits PKCα in human IM-9 lymphocytes, reducing PDBu (HY-18985)-induced hGH-BP release with an IC50 of 0.33 μM[2].
Bisindolylmaleimide III (0.1-2.5 μM; 45 min) hydrochloride inhibits the phosphorylation of PDBu-enhanced 42, 45, 53 and 83 kDa extracellular proteins in human IM-9 lymphocytes, with IC50 values ranging from 0.23 to 0.32 μM[2].
Bisindolylmaleimide III (20 μM; 6-24 h) hydrochlorid does not sensitize human colon adenocarcinoma COLO 205 cells to TNF-α-dependent apoptosis, which is evidenced by unchanged procaspase-3 levels and only a mild decrease in cell viability within 24 hours[3].
Bisindolylmaleimide III (20 μM; 21 h) hydrochlorid does not interfere with the TNF-α-dependent apoptosis-sensitizing activity of Bisindolylmaleimide IX (HY-13866A) in human colon adenocarcinoma COLO 205 cells[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:human colon adenocarcinoma COLO 205 cells
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Concentration:20 μM (co-treated with 10 ng/mL TNF-α)
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Incubation Time:6 h, 12 h, 24 h
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Result:Moderately reduced cell viability over 24 hours, with significant decreases observed at 6, 12, and 24 h compared to controls.
Showed no reduction in procaspase-3 protein levels after co-treatment at 6, 12, or 24 h.
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Cell Line:human colon adenocarcinoma COLO 205 cells
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Concentration:20 μM (pre-incubation; followed by co-treatment with 5 μM Bisindolylmaleimide IX and 10 ng/mL TNF-α)
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Incubation Time:60 min (pre-incubation); 20 h (co-treatment)
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Result:Did not affect the ability of Bisindolylmaleimide IX to sensitize COLO 205 cells to TNF-α-dependent apoptosis.
Chemical Information
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CAS No. 683775-59-9
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Molecular Weight 420.89
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Formula C23H21ClN4O2
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SMILES
O=C1NC(C(C2=CN(CCCN)C3=C2C=CC=C3)=C1C4=CNC5=C4C=CC=C5)=O.Cl
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
[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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Bisindolylmaleimide III hydrochloride Related Classifications
HY-112454 Related Classifications
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