卡弗他丁C
基本信息
产品名称 | 卡弗他丁C |
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英文名称 | Calphostin C from Cladosporium cladosporioides |
别名 | 抑制剂C |
英文别名 | UCN-1028c;Calphostin C |
应用 | 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。 |
规格或纯度 | 90% |
运输条件 | 超低温冰袋运输 |
生化机理 | 靶向调节域(IC50 = 50 nM)的有效,选择性和光依赖性蛋白激酶C抑制剂。与其他蛋白激酶(例如cAMP依赖性蛋白激酶和酪氨酸特异性蛋白激酶)相比,具有超过1000倍的选择性。体外(IC50〜40-60 nM)抑制恶性神经胶质瘤细胞的增殖。也是Tcf /β-catenin复合物的拮抗剂。 |
一般描述
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.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。
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.
相关属性
CAS编号 | 121263-19-2 |
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溶解性 | Soluble in DMSO and in ethanol} |
储存温度 | -20°C储存 |
MDL号 | MFCD00133155 |
密度 | 1.48 |
分子量 | 790.76 |
分子式 | C44H38O14 |
品牌 | Jinpan |
Smiles | COC1=C(CC(C)OC(=O)c2ccccc2)c2c3C(=C(OC)C(=O)c4c(O)cc(OC)c(c34)c3c(OC)cc(O)c(C1=O)c23)CC(C)OC(=O)Oc1ccc(O)cc1 |
PubChem CID | 2533 |