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PKC&ROCK

GF109203X (133052-90-1)

Bisindolylmaleimide I (GF109203X) is a highly selective, cell-permeable, and reversible protein kinase C (PKC) inhibitor with a Ki value of 14 nM.

Not Intended for Therapeutic Use. For research use only.

CAS: 133052-90-1 Category

GF109203X (133052-90-1) Description:

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.

Bisindolylmaleimide I (GF 109203X) is a staurosporine (sc-3510) inspired molecule, which has been shown to display equally potent inhibition, but with vastly superior selectivity, for all of the known isoforms of PKC (IC50 = 8-20 nM). Inhibition is competitive with respect to ATP, which suggests that Bisindolylmaleimide I occupies the ATP binding domain of the PKC isoforms. Bisindolylmaleimide I (GF 109203X) has been used to selectively probe for PKC-mediated pathways for transduction of hormone, cytokine, and growth factor signals. It inhibits PKC within intact platelets and T cells, Fas-mediated apoptosis, and T cell-mediated autoimmune diseases, as well as GSK-3. Bisindolylmaleimide I (GF 109203X) is an inhibitor of PHK/CaM, PKC α, PKC β, PKC δ, PKC ε, PKC γ and SR/HTR3.

GF109203X (133052-90-1) Specifications:

Product Name GF109203X
Synonym GF109203X; GF-109203X; GF 109203X; bisindolylmaleimide; GO 6850; GO-6850; GO6850. BIMI.
Chemical Name 3-(1-(3-(dimethylamino)propyl)-1H-indol-3-yl)-4-(1H-indol-3-yl)-1H-pyrrole-2,5-dione
Drug Class Inhibitor
Purity ≥98% (HPLC)
CAS Number 133052-90-1
Molecular Formula C25H24N4O2
Molecular Weight 412.48
Monoisotopic Mass 412.18993 g/mol
MDL number MFCD00236428
InChIKey QMGUOJYZJKLOLH-UHFFFAOYSA-N
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)
SMILES O=C(C(C1=CN(CCCN(C)C)C2=C1C=CC=C2)=C3C4=CNC5=C4C=CC=C5)NC3=O.
Form Powder
Color N/A
Solubility  Soluble in DMSO (~1 mg/ml), DMF (10 mg/ml; warm to 40°C & vortex well), and 1:10 DMSO:PBS (pH 7.2) (~0.1 mg/ml). Insoluble in water.
Storage Temp.  -20°C
Shelf life >5 years if stored properly
Handling Protect from air and moisture
Application A potent and highly selective PCK inhibitor

 

 


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RIDADR NONH for all modes of transport

References:

[1]. 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.

[2]. 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.

[3]. 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.

[4]. 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.

[5]. 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.

1 review for GF109203X (133052-90-1)

  1. Cofttek

    Never had such good experience before,The GF109203X (133052-90-1) is high purity,also customer service is pretty nice !gotta try!!

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