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 Details
| Alternative Name: | 2-[1-(3-Dimethylaminopropyl)-1H-indol-3-yl]-3-(1H-indol-3-yl)maleimide, Bisindolylmaleimide I |
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| Formula: | C25H24N4O2 |
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| MW: | 412.5 |
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| CAS: | 133052-90-1 |
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| Purity: | ≥98% (HPLC) |
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| Appearance: | Red solid. |
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| Solubility: | Soluble in dimethyl formamide or DMSO (10mg/ml, warm to 40°C and vortex well). |
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| Shipping: | Ambient |
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| Long Term Storage: | -20°C |
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| Handling: | Protect from light. |
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| Regulatory Status: | RUO - Research Use Only |
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Product Literature References
Effect of selective serotonin (5-HT)2B receptor agonist BW723C86 on epidermal growth factor/transforming growth factor-α receptor tyrosine kinase and ribosomal p70 S6 kinase activities in primary cultures of adult rat hepatocytes: K. Naito, et al.; Biol. Pharm. Bull.
42, 631 (2019),
Application(s): used w. adult rat liver hepatocytes,
Abstract;
Full Text
Feedback Regulation of Syk by Protein Kinase C in Human Platelets: S. Makhoul, et al.; Int. J. Mol. Sci.
21, 176 (2019),
Abstract;
Osmotic activation of a Ca2+-dependent phospholipase C pathway that regulates ∆N TRPV1-mediated currents in rat supraoptic neurons: V. Bansai & T.E. Fisher; Physiol. Rep.
5, e13259 (2017),
Abstract;
Full Text
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;
