Bisindolylmaleimide III
Based on 1 publication(s) in Google Scholar
Bisindolylmaleimide III 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 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 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 can be used in studies of signal transduction and colorectal cancer.
For research use only. We do not sell to patients.
- Purity: 98.95%
- CAS No.: 137592-43-9
- Formula: C23H20N4O2
- Molecular Weight:384.43
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Bisindolylmaleimide III
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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) 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) 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 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. 137592-43-9
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Appearance Solid
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Molecular Weight 384.43
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Formula C23H20N4O2
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Color Brown to reddish brown
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SMILES
O=C(C(C1=CN(CCCN)C2=C1C=CC=C2)=C3C4=CNC5=C4C=CC=C5)NC3=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
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Curr Eye Res
Kisspeptin Suppresses the Growth of Primary Pterygial Cells via Inhibiting Chemokine (C-X-C Motif) Ligands in Microenvironment. [Abstract]2025 Sep;50(9):894-902. PMID: 40555256
Solvent & Solubility
DMSO : 25 mg/mL (65.03 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 1.25 mg/mL (3.25 mM); Clear solution
This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 1.25 mg/mL (3.25 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 1.25 mg/mL.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (287 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Handling Instructions (2659 KB)
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]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 2.6013 mL | 13.0063 mL | 26.0125 mL | 65.0313 mL |
| 5 mM | 0.5203 mL | 2.6013 mL | 5.2025 mL | 13.0063 mL | |
| 10 mM | 0.2601 mL | 1.3006 mL | 2.6013 mL | 6.5031 mL | |
| 15 mM | 0.1734 mL | 0.8671 mL | 1.7342 mL | 4.3354 mL | |
| 20 mM | 0.1301 mL | 0.6503 mL | 1.3006 mL | 3.2516 mL | |
| 25 mM | 0.1041 mL | 0.5203 mL | 1.0405 mL | 2.6013 mL | |
| 30 mM | 0.0867 mL | 0.4335 mL | 0.8671 mL | 2.1677 mL | |
| 40 mM | 0.0650 mL | 0.3252 mL | 0.6503 mL | 1.6258 mL | |
| 50 mM | 0.0520 mL | 0.2601 mL | 0.5203 mL | 1.3006 mL | |
| 60 mM | 0.0434 mL | 0.2168 mL | 0.4335 mL | 1.0839 mL |
Bisindolylmaleimide III Related Classifications
HY-117393 Related Classifications
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