CGP60474 是一种高效的抗内毒素药物，是一种有效的细胞周期蛋白依赖性激酶 (CDK) 抑制剂（对 CDK1/B、CDK2/E、CDK2/ 的 IC50 值为 26、3、4、216、10、200 和 13 nM A、CDK4/D、CDK5/p25、CDK7/H 和 CDK9/T）。 CGP60474 是一种选择性和 ATP 竞争性 PKC 抑制剂。
| Cas No. | 164658-13-3 |
| 别名 | 3-[[4-[2-[(3-氯苯基)氨基]-4-嘧啶基]-2-吡啶基]氨基]-1-丙醇,CGP-60474;CGP 60474 |
| 化学名 | 3-[[4-[2-(3-chloroanilino)pyrimidin-4-yl]pyridin-2-yl]amino]propan-1-ol |
| Canonical SMILES | C1=CC(=CC(=C1)Cl)NC2=NC=CC(=N2)C3=CC(=NC=C3)NCCCO |
| 分子式 | C18H18ClN5O |
| 分子量 | 355.82 |
| 溶解度 | DMSO: 10 mM |
| 储存条件 | Store at -20℃ |
| 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 | CGP60474 is a potent inhibitor of cyclin-dependent kinases (CDKs) with IC50 value of 17 nM for CDK1 [1]. It is also an inhibitor of Protein Kinase C (PKC) [1].
CDKs are a family of protein kinases regulating the cell cycle. PKC plays an important role in signal transductions, cellular proliferation and differentiation [2].
CGP60474 was highly selective for PKC than other serine/threonine and tyrosine kinases and showed competitive kinetics relative to ATP [2].
References:
[1]. Kuo GH, Deangelis A, Emanuel S, et al. Synthesis and identification of [1,3,5]triazine-pyridine biheteroaryl as a novel series of potent cyclin-dependent kinase inhibitors. J Med Chem, 2005, 48(14): 4535-4546.
[2]. Stanetty P, Hattinger G, Schnürch M, et al. Novel and efficient access to phenylamino-pyrimidine type protein kinase C inhibitors utilizing a Negishi cross-coupling strategy. J Org Chem, 2005, 70(13): 5215-5220 |
