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GF109203X

PKC inhibitor
 
BML-EI246-0001 1 mg 75.00 USD
 
BML-EI246-0005 5 mg 177.00 USD
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Replaces Prod. #: ALX-270-049

Potent and selective protein kinase C inhibitor which has been used effectively in platelets, Swiss 3T3 fibroblasts and macrophages. Inhibitory profile: PKC, IC50=0.02µM (inhibits α, ßI, ßII and γ subtypes with similar potency); PKA, IC50=2.0µM; phosphorylase kinase, IC50=0.7µM; insulin, EGF and PDGF receptor tyrosine kinases are not inhibited at concentrations up to 50µM.

Product Specification

Alternative Name:2-[1-(3-Dimethylaminopropyl)-1H-indol-3-yl]-3-(1H-indol-3-yl)maleimide, Bisindolylmaleimide I
 
Formula:C25H24N4O2
 
MW:412.5
 
CAS:133052-90-1
 
Purity:≥98% (TLC)
 
Appearance:Red solid.
 
Solubility:Soluble in dimethyl formamide or DMSO (10mg/ml, warm to 40°C and vortex well). 
 
Shipping:Ambient
 
Long Term Storage:-20°C
 
Handling:Protect from light.
 
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Product Literature References

Connexin43 phosphorylation by PKC and MAPK signals VEGF-mediated gap junction internalization: W. Nimlamool, et al.; Mol. Biol. Cell 26, 2755 (2015), Application(s): Cell Culture, Abstract; Full Text
Elevated Serum Antibody Levels against Cyclin L2 in Patients with Esophageal Squamous Cell Carcinoma: H. Shimada, et al.; J. Cancer Sci. Ther. 7, 60 (2015), Application(s): Cell Culture, Full Text
Protein Kinase C Alpha Mediates Erlotinib Resistance in Lung Cancer Cells: M.B. Abera, et al.; Mol. Pharmacol. 87, 832 (2015), Application(s): Cell Culture, Abstract; Full Text
Trichuris suis induces human non-classical patrolling monocytes via the mannose receptor and PKC: implications for multiple sclerosis: G. Kooij, et al.; Acta. Neuropathol. Commun. 3, 45 (2015), Application(s): Cell Culture, Abstract; Full Text
Gonadotropin-inhibitory hormone inhibits GnRH-induced gonadotropin subunit gene transcriptions by inhibiting AC/cAMP/PKA-dependent ERK pathway in LβT2 cells: Y.L. Son, et al.; Endocrinology 153, 2332 (2012), Application(s): Cell culture, Abstract; Full Text
Enhanced thromboxane receptor-mediated responses and impaired endothelium-dependent relaxation in human corpus cavernosum from diabetic impotent men: role of protein kinase C activity: J. Angulo, et al.; J. Pharmacol. Exp. Ther. 319, 783 (2006), Abstract;
Cellular protein kinase C isozyme regulation by exogenously delivered physiological disulfides--implications of oxidative protein kinase C regulation to cancer prevention: F. Chu, et al.; Carcinogenesis 25, 585 (2004), Abstract;
Stimulation of the ERK pathway by GTP-loaded Rap1 requires the concomitant activation of Ras, protein kinase C, and protein kinase A in neuronal cells.: T. Bouschet et al.; J. Biol. Chem. 278, 4778 (2003), Abstract;
Anti-inflammatory properties of the protein kinase C inhibitor, 3-[1-[3-(dimethylamino)propyl]-1H-indol-3-yl]-4-(1H-indol-3-yl)-1H- pyrrole-2,5-dione monohydrochloride (GF109203X) in the PMA-mouse ear edema model.: S. Kuchera et al.; Agents Actions 39, 169 (1993), Abstract;
Reactive oxygen species are involved in the activation of cellular phospholipase A2.: R. Goldman et al.; FEBS Lett. 309, 190 (1992), Abstract;
The bisindolylmaleimide GF 109203X is a potent and selective inhibitor of protein kinase C.: D. Toullec et al.; J. Biol. Chem. 266, 15771 (1991), Abstract;

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