Bisindolylmaleimide IV (Synonyms: Arcyriarubin A,BIM IV) |
| Catalog No.GC14716 |
Bisindolylmaleimide IV is a potent cell-permeable inhibitor of protein kinase C (PKC) with IC50 values are 0.1- 0.55μM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 119139-23-0
Sample solution is provided at 25 µL, 10mM.
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Bisindolylmaleimide IV is a potent cell-permeable inhibitor of protein kinase C (PKC) with IC50 values are 0.1- 0.55μM[1]. Bisindolylmaleimide IV inhibits the cAMP-dependent protein kinase (PKA) with IC50 ranging from 3.1-11.8μM[2]. Bisindolylmaleimide IV is primarily used in research related to cancer biology[3], cardiovascular diseases[4], and diabetes, particularly in studies investigating PKC-mediated signaling pathways and their impact on cellular functions[5].
Bisindolylmaleimide IV (20μM) down-regulates cellular caspase 8 (FLICE)-like inhibitory protein (c-FLIPL) expression and facilitates CD95-mediated apoptosis in monocyte-derived dendritic cells[6]. Bisindolylmaleimide IV (0.1-100μM) inhibits the release of reactive oxygen species (ROS) from human neutrophils stimulated by agents such as IL-3, phorbol-12-myristate-13-acetate (PMA), and sodium fluoride in a dose-dependent manner[7].
References:
[1]. Toullec D, Pianetti P, Coste H, et al. The bisindolylmaleimide GF 109203X is a potent and selective inhibitor of protein kinase C. J Biol Chem. 1991 Aug 25;266(24):15771-81. PMID: 1874734.
[2]. Fabre S, Prudhomme M, Rapp M. Protein kinase C inhibitors; structure-activity relationships in K252c-related compounds. Bioorg Med Chem. 1993 Sep;1(3):193-6. doi: 10.1016/s0968-0896(00)82121-5. PMID: 8081852.
[3]. Pajak B, Orzechowska S, Gajkowska B, Orzechowski A. Bisindolylmaleimides in anti-cancer therapy - more than PKC inhibitors. Adv Med Sci. 2008;53(1):21-31. doi: 10.2478/v10039-008-0028-6. PMID: 18635421.
[4]. Silnitsky S, Rubin SJS, Zerihun M, Qvit N. An Update on Protein Kinases as Therapeutic Targets-Part I: Protein Kinase C Activation and Its Role in Cancer and Cardiovascular Diseases. Int J Mol Sci. 2023 Dec 18;24(24):17600. doi: 10.3390/ijms242417600. PMID: 38139428; PMCID: PMC10743896.
[5].Anderson PW, McGill JB, Tuttle KR. Protein kinase C beta inhibition: the promise for treatment of diabetic nephropathy. Curr Opin Nephrol Hypertens. 2007 Sep;16(5):397-402. doi: 10.1097/MNH.0b013e3281ead025. PMID: 17693752.
[6]. Willems F, Amraoui Z, Vanderheyde N, et al. Expression of c-FLIP(L) and resistance to CD95-mediated apoptosis of monocyte-derived dendritic cells: inhibition by bisindolylmaleimide. Blood. 2000 Jun 1;95(11):3478-82. PMID: 10828032.
[7]. Krämer HJ, Kessler D, Hipler UC, et al. Pityriarubins, novel highly selective inhibitors of respiratory burst from cultures of the yeast Malassezia furfur: comparison with the bisindolylmaleimide arcyriarubin A. Chembiochem. 2005 Dec;6(12):2290-7. doi: 10.1002/cbic.200500163. PMID: 16252297.
| Cell experiment [1]: | |
Cell lines | Dendritic cells |
Preparation Method | Dendritic cells were incubated in medium in the presence of anti-CD95 mAb (0.5μg/mL) with or without Bisindolylmaleimide IV (20μM). After 18 hours, cells were fixed, DNA was stained with propidium iodide (PI), and the percentage of hypodiploid nuclei (subG1 peak) was analyzed with use of flow cytometry. |
Reaction Conditions | 20μM; 18h |
Applications | Bisindolylmaleimide IV facilitates apoptosis induced by anti-CD95 mAb. |
References: | |
| Cas No. | 119139-23-0 | SDF | |
| Synonyms | Arcyriarubin A,BIM IV | ||
| Chemical Name | 3,4-di-1H-indol-3-yl-1H-pyrrole-2,5-dione | ||
| Canonical SMILES | O=C1NC(=O)C(=C1c1c[nH]c2ccccc12)c1c[nH]c2ccccc12 | ||
| Formula | C20H13N3O2 | M.Wt | 327.3 |
| Solubility | ≤20mg/ml in ethanol;20mg/ml in DMSO;20mg/ml in dimethyl formamide | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 3.0553 mL | 15.2765 mL | 30.553 mL |
| 5 mM | 0.6111 mL | 3.0553 mL | 6.1106 mL |
| 10 mM | 0.3055 mL | 1.5277 mL | 3.0553 mL |
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >97.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 3 reference(s) in Google Scholar.)
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