P-7600 PKC412, >99%

Storage: Store at or below -20 ºC. Solubility: Soluble in DMSO at 100 mg/mL; soluble in ethanol at 5 mg/mL with warming; very poorly soluble in water; maximum solubility in plain water is estimated to be about 10-20 µM; buffers, serum, or other additives may increase or decrease the aqueous solubility. Disposal: A.

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• The staurosporine analog, PKC412, inhibits a variety of serine/threonine and tyrosine kinases including PKC (IC50 = 50 nM), cyclic AMP-dependent protein kinase (IC50 = 2.4 µM), S6 kinase (IC50 = 5.0 µM), and EGFR (epidermal growth factor receptor) tyrosine-kinase activity (IC50 = 3.0 µM). Meyer, T., et al. "A derivative of staurosporine (CGP 41 251) shows selectivity for protein kinase C inhibition and in vitro anti-proliferative as well as in vivo anti-tumor activity." Int. J. Cancer 43: 851-856 (1989).
• PKC412 inhibits autophosphorylation of platelet-derived growth factor (PDGF) receptor in BALB/c 3T3 cells at submicromolar concentrations. Andrejauskas-Buchdunger, E. and Regenass, U. "Differential inhibition of the epidermal growth factor-, platelet-derived growth factor-, and protein kinase C-mediated signal transduction pathways by the staurosporine derivative CGP 41251." Cancer Research, 52: 5353-5358 (1992).
• PKC412 strongly blocks the proliferation of ras-transformed pancreatic cancer cells (TUC-3) by causing apoptosis and induction of phenotypic reversion. Way, D., et al. "A protein kinase C inhibitor induces phenotypic reversion of ras-transformed pancreatic cancer cells and cooperatively blocks tumor cell proliferation with an anti-ras peptide." Cancer Chemother. Pharmacol. 49: 429-437 (2002).
• PKC412 suppresses Akt activity by blocking serine phosphorylation in the kinase activation loop and induces apoptosis in myeloma cell lines. Bahlis, N.J., et al. "N-Benzoylstaurosporine (PKC412) inhibits Akt kinase inducing apoptosis in multiple myeloma cells." Leuk. Lymphoma 46: 899-908 (2005).
• PKC412 selectively inhibits T lymphocyte production of TNF-α (tumor necrosis factor - alpha) with an IC50 of 0.5 µM. Si, M.S., et al. "Effects of the kinase inhibitor CGP41251 (PKC 412) on lymphocyte activation and TNF-alpha production." Int. Immunopharmacol. 5: 1141-11419 (2005).
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