NU6027 is a potent and ATP-competitive inhibitor of both CDK1 and CDK2, with Kis of 2.5 µM and 1.3 µM, respectively. NU6027 is also a potent inhibitor of ATR and enhances hydroxyurea and cisplatin cytotoxicity in an ATR-dependent manner.
体外研究
NU6027 (1 nM-100 µM; 48 h) inhibits the growth of human tumor cells with a GI50 of 10±6 µM.
NU6027 (0.1-25 µM; 24 h) inhibits ATR activity with an IC50 of 2.8 µM in GM847KD cells. NU6027 (1-10 µM; 24 h) inhibits ATR activity with an IC50 of 6.7±2.3 µM in MCF7 cells.
NU6027 (4 or 10 µM; 24 h) attenuates G2/M arrest following DNA damage in MCF7 cells.
NU6027 (10 µM; 24 h) significantly reduces RAD51 foci in both control and PF-01367338-treated V-C8 B2 cells.
NU6027 (4 µM; 24 h) causes 82% suppression of the increase in RAD51 foci-positive cells treated by PF-01367338.
Western Blot Analysis
Cell Line:
MCF7 cells
Concentration:
0, 1, 5, 10 μM
Incubation Time:
24 h
Result:
Inhibited CDK2-mediated pRb by 42±27% compared with 70±12% inhibition of pCHK1 with the concentration of 10 µM.
分子式
C5H7N3O2
分子量
251.28
CAS号
220036-08-8
运输条件
Room temperature in continental US; may vary elsewhere.