CCG-273220 是 G 蛋白偶联受体 (GPCR) 激酶 5 (GRK5) 的共价抑制剂,IC50 值为 220 nM。 CCG-273220 通过结合 GRK5 亚家族特异性残基 Cys474 作为共价手柄,对 GRK5 的选择性高于 GRK2 (IC50=350 μM)。
Cas No. | 1404-15-5 |
别名 | 诺拉霉素 |
Canonical SMILES | OC1=C(C(C(C(O)=CC2=C3O[C@@]4([H])[C@@H](O)[C@H](N(C)C)[C@@H](O)[C@@]2(O4)C)=C3C5=O)=O)C5=CC6=C1[C@@H](O[C@@]7([H])[C@H](OC)[C@@](OC)(C)[C@@H](OC)[C@H](C)O7)C[C@](C)(O)[C@@H]6C(OC)=O |
分子式 | C39H49NO16 |
分子量 | 787.8 |
溶解度 | DMF: Soluble,DMSO: Soluble,Ethanol: soluble,Methanol: Soluble |
储存条件 | Store at -20°C |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
产品描述 | Nogalamycin is an anthracycline originally isolated from S. nogalater and a DNA-intercalating agent. It inhibits the DNA-unwinding and ATPase activities of P. falciparum DNA helicase 60 (IC50s = 2 and 0.5 μM, respectively) and the DNA cleavage activity of vaccinia virus topoisomerase (IC50 = 0.7 μM). Nogalamycin also inhibits the growth of MCF-7 and MDA-MB-231 human breast cancer cells (IC50s = 0.242 and 0.37 μM, respectively). |