Bisindolylmaleimide IV (Synonyms: Arcyriarubin A,BIM IV) |
| Catalog No.GC14716 |
Bisindolylmaleimide IV est un puissant inhibiteur cellule - perméable de la protéine kinase C (PKC), ce que les valeurs d'IC50 sont 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 est un puissant inhibiteur cellule - perméable de la protéine kinase C (PKC), ce que les valeurs d'IC50 sont 0.1- 0.55μM[1]. Bisindolylmaleimide IV inhibe la protéine kinase cAMP - dépendante (PKA), ce que la valeur d'IC50 est entre 3,1 et 11,8μM[2]. Bisindolylmaleimide IV est principalement utilisé dans la recherche qui est relative à la biologie du cancer[3], aux maladies cardiovasculaires[4], et au diabète, particulièrement dans les recherches des voies de signalisation PKC-médiée et leur impact sur les fonctions cellulaires[5].
Bisindolylmaleimide IV (20μM) réduit la régulation l'expression de la protéine d'inhibition de la capase 8 (FLICE) cellulaire (c-FLIPL) et facilite l'apoptose CD95-médiiée dans les cellules dendritiques dérivées de monocytes[6]. Bisindolylmaleimide IV (0.1-100μM) inhibe la libération d'espèces réactives de l'oxygène (ROS) à partir de neutrophiles humains qui sont stimulés de manière dose - dépendante par les agents comme IL-3, phorbol-12-myristate-13-acétate (PMA), et le fluorure de sodium[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.
| Expériences cellulaires [1]: | |
Lignées cellulaires | Cellules dendritiques |
Méthode de préparation | Les cellules dentritiques ont été incubées dans un substrat en présence d'anticorps monoclonaux anti-CD95 (0,5µg/mL), avec ou sans Bisindolylmaleimide IV (20μM). Après 18 heures, les cellules ont été fixées, DNA a été coloré par l'iode de propidium (PI), et le pourcentage de noyaux hypodiploïdes (pic subG1) a été analysé par utiliser le cytométrie en flux. |
Conditions de réaction | 20μM; 18h |
Domaines d'application | Bisindolylmaleimide IV facilite l'apoptose induite par l'anticorps monoclonal anti-CD95. |
References: | |
| Cas No. | 119139-23-0 | SDF | |
| Synonymes | 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 | 611.1 μL | 3.0553 mL | 6.1106 mL |
| 10 mM | 305.5 μL | 1.5277 mL | 3.0553 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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Working concentration: mg/ml;
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
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- 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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