產品名稱：PKC412
產品貨號：LC  P-7600
產品規格：10 MG
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).
Not available in some countries; not available to some institutions; may not be sold for some uses.
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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