GF-109203X
GF-109203X is a potent and highly selective PCK inhibitor, which inhibits PKC isozymes alpha, beta 1, beta 2, gamma, delta and epsilon in vitro . GF-109203X inhibited GSK-3 in vitro, when assayed either in cell lysates (IC(50) 360 nM or in GSK-3beta immunoprecipitates (IC(50) 170 nM derived from rat epididymal adipocytes. Pretreatment of adipocytes with GF-109203X (5 microM) reduced GSK-3 activity in total cell lysates, to 25.1+/-4.3% of control.
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Chemical Information
| Name | GF-109203X |
|---|---|
| Iupac Chemical Name | 3-(1-(3-(dimethylamino)propyl)-1H-indol-3-yl)-4-(1H-indol-3-yl)-1H-pyrrole-2,5-dione |
| Synonyms | GF109203X; GF-109203X; GF 109203X; bisindolylmaleimide; GO 6850; GO-6850; GO6850. BIMI. |
| Molecular Formula | C25H24N4O2 |
| Molecular Weight | 412.48 |
| Smile | O=C(C(C1=CN(CCCN(C)C)C2=C1C=CC=C2)=C3C4=CNC5=C4C=CC=C5)NC3=O. |
| InChiKey | QMGUOJYZJKLOLH-UHFFFAOYSA-N |
| InChi | 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) |
| CAS Number | 133052-90-1 |
| Related CAS |
Ordering Information
| Packaging | Price | Availability | Purity | Shipping Time |
|---|---|---|---|---|
| Bulk | Enquiry | Enquiry | Enquiry |
| Formulation | Solid powder |
|---|---|
| Purity | 98% Min. |
| Storage | Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years). |
| Solubility | Soluble in DMSO |
| Handling | |
| Shipping Condition | Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs. |
| HS Code |
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| Mechanism | |
| Cell study | |
| Animal study | |
| Clinical study |
1: Harmati G, Papp F, Szentandrássy N, Bárándi L, Ruzsnavszky F, Horváth B, Bányász T, Magyar J, Panyi G, Krasznai Z, Nánási PP. Effects of the PKC inhibitors chelerythrine and bisindolylmaleimide I (GF 109203X) on delayed rectifier K+ currents. Naunyn Schmiedebergs Arch Pharmacol. 2011 Feb;383(2):141-8. doi: 10.1007/s00210-010-0584-8. Epub 2010 Dec 1. PubMed PMID: 21120453.
2: Hers I, Tavaré JM, Denton RM. 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. PubMed PMID: 10556511.
3: Stemmelin J, Mathis C, Ungerer A. GF 109203X, a selective inhibitor of protein kinase C, impairs retention performance in an operant task. Neuroreport. 1999 Sep 9;10(13):2805-9. PubMed PMID: 10511444.
4: Alessi DR. The protein kinase C inhibitors Ro 318220 and GF 109203X are equally potent inhibitors of MAPKAP kinase-1beta (Rsk-2) and p70 S6 kinase. FEBS Lett. 1997 Feb 3;402(2-3):121-3. PubMed PMID: 9037179.
5: Gekeler V, Boer R, Uberall F, Ise W, Schubert C, Utz I, Hofmann J, Sanders KH, Schächtele C, Klemm K, Grunicke H. Effects of the selective bisindolylmaleimide protein kinase C inhibitor GF 109203X on P-glycoprotein-mediated multidrug resistance. Br J Cancer. 1996 Sep;74(6):897-905. PubMed PMID: 8826855; PubMed Central PMCID: PMC2074754.
6: Grigorova-Borsos AM, Bakillah A, Urios P, Leblond V, Guillot R, Sternberg M. Production of type IV collagen and 72-kDa gelatinase by human endothelial cells cultured in high glucose. Effects of a protein kinase C inhibitor, GF 109203X. Biochem Cell Biol. 1996;74(5):659-67. PubMed PMID: 9018373.
7: Kiss Z, Phillips H, Anderson WH. The bisindolylmaleimide GF 109203X, a selective inhibitor of protein kinase C, does not inhibit the potentiating effect of phorbol ester on ethanol-induced phospholipase C-mediated hydrolysis of phosphatidylethanolamine. Biochim Biophys Acta. 1995 Feb 16;1265(1):93-5. PubMed PMID: 7857990.
8: Gekeler V, Boer R, Ise W, Sanders KH, Schächtele C, Beck J. The specific bisindolylmaleimide PKC-inhibitor GF 109203X efficiently modulates MRP-associated multiple drug resistance. Biochem Biophys Res Commun. 1995 Jan 5;206(1):119-26. PubMed PMID: 7818510.
9: Le Panse R, Mitev V, Lebreton C, Coulomb B. Modulation of epidermal growth factor and keratinocyte growth factor effects on human keratinocyte growth by protein kinase C inhibitor, GF 109203X: comparison to fibroblast growth modulation. Biochem Biophys Res Commun. 1994 Nov 15;204(3):1081-7. PubMed PMID: 7980581.
10: Le Panse R, Coulomb B, Mitev V, Bouchard B, Lebreton C, Dubertret L. Differential modulation of human fibroblast and keratinocyte growth by the protein kinase C inhibitor GF 109203X. Mol Pharmacol. 1994 Sep;46(3):445-51. PubMed PMID: 7935324.
11: Heikkilä J, Jalava A, Eriksson K. The selective protein kinase C inhibitor GF 109203X inhibits phorbol ester-induced morphological and functional differentiation of SH-SY5Y human neuroblastoma cells. Biochem Biophys Res Commun. 1993 Dec 30;197(3):1185-93. PubMed PMID: 8280132.
12: Toullec D, Pianetti P, Coste H, Bellevergue P, Grand-Perret T, Ajakane M, Baudet V, Boissin P, Boursier E, Loriolle F, 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. PubMed PMID: 1874734.
Chemical Structure
