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25mg |
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Purity: ≥98%
GF109203X (also known as GF109203-X; bisindolylmaleimide; GO-6850; GF-109203 X; BIMI; GF-109203X) is a novel, potent, highly selective, cell-permeable, and reversible PKC (protein kinase C) inhibitor with potential antitumor activity. It inhibits PKCα, PKCβI, PKCβII, and PKCγ with IC50s of 20 nM, 17 nM, 16 nM, and 20 nM in cell-free assays, respectively. GF109203X showed > 3000-fold selectivity for PKC over EGFR, PDGFR and insulin receptor. GF-109203X inhibited GSK-3 in vitro, when assayed either in cell lysates IC50 360 nM or in GSK-3beta immunoprecipitates IC50 170 nM derived from rat epididymal adipocytes.
ln Vitro |
P47 phosphorylation caused by α-thrombin is inhibited by bisindolylmaleimide I (5 μM) [1]. In Swiss 3T3 cells at rest, bisindolylmaleimide I (0–1 μM) suppresses DNA synthesis [1]. In adipocyte lysates, bisindolylmaleimide I (5 μM) lowers GSK-3 activity to 25.1±4.3%[3]. PC3 cells are unable to release exosomes or microvesicles (EMV) when exposed to bisindolylmaleimide I (10 μM) during a 24-hour period [4]. Bisindolylmaleimide I (10 μM, 24 hours) increases 5-fluorouracil's cytotoxicity [4].
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ln Vivo |
In mice in the mechanically ventilated (MV) group, increased levels of NLRP3, P-PKCɑ, and PKCɑ are reduced by intraperitoneal injection of bisindolylmaleimide I (0.02 mg/kg) [5]. Bisindolylmaleimide I (0–20 mg/kg, i.p.) lowers the average frequency of shrew vomiting caused by quinpirole [6].
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Animal Protocol |
Animal/Disease Models: Quinpirole-treated shrews[2]
Doses: 0-20 mg/kg Route of Administration: ip Experimental Results: decreased the mean frequency of Quinpirole-induced vomiting. Blocked Quinpirole-mediated ERK1/2 phosphorylation in shrew brainstems. |
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
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Molecular Weight |
412.48
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CAS # |
133052-90-1
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SMILES |
O=C1C(=C(C(N1[H])=O)C1=C([H])N([H])C2=C([H])C([H])=C([H])C([H])=C12)C1=C([H])N(C([H])([H])C([H])([H])C([H])([H])N(C([H])([H])[H])C([H])([H])[H])C2=C([H])C([H])=C([H])C([H])=C12
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InChi Key |
QMGUOJYZJKLOLH-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C25H24N4O2/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)
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Chemical Name |
3-(1-(3-(dimethylamino)propyl)-1H-indol-3-yl)-4-(1H-indol-3-yl)-1H-pyrrole-2,5-dione
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Synonyms |
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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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) |
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Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.4244 mL | 12.1218 mL | 24.2436 mL | |
5 mM | 0.4849 mL | 2.4244 mL | 4.8487 mL | |
10 mM | 0.2424 mL | 1.2122 mL | 2.4244 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.