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Purity: ≥98%
Bisindolylmaleimide I HCl (GF109203X; Gö 6850; BIM I) is a novel, highly selective, cell-permeable, and reversible PKC inhibitor with Ki of 14 nM). It is structurally similar to the poorly selective PKC inhibitor staurosporine. It acts as a competitive inhibitor for the ATP binding site of PKC and shows high selectivity for PKCα, β1, β2, γ, δ, and ε isozymes. BIM I directly inhibits glycogen synthase kinase 3 (GSK3) in primary adipocyte lysates (IC50 = 360 nM) and in GSK3β immunoprecipitates derived from rat epididymal adipocytes (IC50 = 170 nM).2 It also competitively antagonizes the serotonin (5-HT) receptor subtype 5-HT3 with a Ki value of 61 nM.
| ln Vitro |
P47 phosphorylation produced by α-phosphatase is inhibited by bisindolylmaleimide I hydrochloride (5 μM) [1]. μM) can lower GSK-3 activity in internal substances of adipocytes to 25.1±4.3%[3]. Exosome and microvesicle (EMV) release from PC3 cells is inhibited by bisindolylmaleimide I hydrochloride (10 μM, 24 hours) [4]. Fluorouracil's 5-Cytotoxicity is enhanced by bisindolylmaleimide I hydrochloride (10 μM, 24 hours) [4].
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| ln Vivo |
In mice in the mechanically ventilated (MV) group, elevated levels of NLRP3, P-PKCɑ, and PKCɑ are reduced by intraperitoneal injection of bisindolylmaleimide I hydrochloride (0.02 mg/kg) [5].
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| Animal Protocol |
Animal/Disease Models: Quinpirole-treated shrews[2]
Doses: 0-20 mg/kg Route of Administration: ip Experimental Results: diminished quinpirole-injection) diminished the mean frequency of quinpirole-induced vomiting in shrews[ 6]. Induces vomiting. Blocks quinpirole-mediated ERK1/2 phosphorylation in the shrew brainstem. |
| References |
[1]. Toullec D, 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.
[2]. Vetri F, et al. Impairment of neurovascular coupling in Type 1 Diabetes Mellitus in rats is prevented by pancreatic islet transplantation and reversed by a semi-selective PKC inhibitor. Brain Res. 2017 Jan 15;1655:48-54. [3]. Hers I, et al. The protein kinase C inhibitors bisindolylmaleimide I (GF 109203x) and IX (Ro 31-8220) are potent inhibitors of glycogen synthase kinase-3 activity. FEBS Lett. 1999 Nov 5;460(3):433-6. [4]. Kosgodage US, et al. Chloramidine/Bisindolylmaleimide-I-Mediated Inhibition of Exosome and Microvesicle Release and Enhanced Efficacy of Cancer Chemotherapy. Int J Mol Sci. 2017 May 9;18(5):1007. [5]. Liu M, et al. Aerobic exercise alleviates ventilator-induced lung injury by inhibiting NLRP3 inflammasome activation. BMC Anesthesiol. 2022 Dec 1;22(1):369. [6]. Belkacemi L, et al. Signal transduction pathways involved in dopamine D2 receptor-evoked emesis in the least shrew (Cryptotis parva). Auton Neurosci. 2021 Jul;233:102807. |
| Molecular Formula |
C25H24N4O2.HCL
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|---|---|
| Molecular Weight |
448.9446
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| CAS # |
176504-36-2
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| Related CAS # |
Bisindolylmaleimide I;133052-90-1
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| SMILES |
O=C(C(C1=CN(CCCN(C)C)C2=C1C=CC=C2)=C3C4=CNC5=C4C=CC=C5)NC3=O.[H]Cl
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| InChi Key |
XRAMWNCMYJHGGH-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C25H24N4O2.ClH/c1-28(2)12-7-13-29-15-19(17-9-4-6-11-21(17)29)23-22(24(30)27-25(23)31)18-14-26-20-10-5-3-8-16(18)20;/h3-6,8-11,14-15,26H,7,12-13H2,1-2H3,(H,27,30,31);1H
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| Chemical Name |
3-[1-[3-(Dimethylamino)propyl]indol-3-yl]-4-(1H-indol-3-yl)pyrrole-2,5-dione Hydrochloride
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| Synonyms |
BIS-I HCl; GF-109203X HCl; GO-6860 HCl; BISI HCl; GF109203X HCl; GO6860 HCl; BIS I HCl; GF 109203X HCl; GO 6860 HCl;
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~62.5 mg/mL (~139.22 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2.08 mg/mL (4.63 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2275 mL | 11.1373 mL | 22.2747 mL | |
| 5 mM | 0.4455 mL | 2.2275 mL | 4.4549 mL | |
| 10 mM | 0.2227 mL | 1.1137 mL | 2.2275 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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