Product Name: Calphostin C from Cladosporium cladosporioides
别名: | 抑制剂C |
CAS号: | 121263-19-2 |
分子式: | C44H38O14 |
分子量: | 790.76 |
MDL号: | MFCD00133155 |
介绍: | Calphostin C is a novel, cell permeable, potent and highly selective inhibitor of protein kinase C (IC50=0.05 μM). Calphostin C has been shown to compete at the DAG binding site and inhibit DGK (DAG kinase, DAGK). Calphostin inhibition of PKC is light dependent. At higher concentrations it inhibits myosin light chain kinase, PKA (cAMP-dependent protein kinase), protein kinase G, c-Src (pp60v-src protein TyK) (tyrosine kinase) and DGK. This compound also inhibits PC-PLD1 and -PLD2 (Phospholipase D1 and D2, PLD1 and PLD2). Calphostin C has been observed to induce apoptotic DNA fragmentation and cell death. This compound has demonstrated the ability to inhibit cardiac L-type Ca2+ channels. It has demonstrated the ability to Inhibit cardiac L-type calcium channel protein inhibitors. Calphostin C is an inhibitor of MYLK, PKA and PKD. |
用途: | 蛋白激酶C(IC50=50 nM)的高度特异性抑制剂;需要光进行激活。在较高浓度下(100 nM或更大),它已被证明在体外能抑制细胞增殖和诱导细胞凋亡。 |
特定比重: | 1.48 |
贮存: | 储存温度:-20℃ |
可溶性: | Soluble in ethanol (1 mg/ml), DMSO (1 mg/ml), and DMF (1 mg/ml). Insoluble in water., Soluble in ethanol (1 mg/ml), DMSO (1 mg/ml), and DMF (1 mg/ml). Insoluble in water. |
生化和生理学机理: | Potent, selective and photo-dependent inhibitor of protein kinase C that targets the regulatory domain (IC50 = 50 nM). Displays > 1000-fold selectivity over other protein kinases such as cAMP-dependent protein kinase and tyrosine-specific protein kinase. Inhibits cell proliferation of malignant glioma cells in light-treated conditions in vitro (IC50 ~ 40 - 60 nM). Also an antagonist of the Tcf/β-catenin complex. |
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