ML-240

ML-240CAS号: 1346527-98-7分子式: C23H20N6O分子量: 396.44描述纯度储存/保存方法别名外观可溶性/溶解性靶点In vitro(体外研究)

产品描述
描述
ML-240 is am ATP-competitive inhibitor of p97 ATPase (IC50 = 110 nM).
纯度
>98%
储存/保存方法
Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
基本信息
别名
ML240
外观
white to yellow to light brown powder
可溶性/溶解性
DMSO : 12.5 mg/mL (31.53 mM; Need ultrasonic)
生物活性
靶点
p97
In vitro(体外研究)
ML240 is a potent p97 inhibitor, with an IC50 of 100 nM. ML240 is active in the UbG76V-GFP stabilization assay (IC50, 0.9 μM). ML240 inhibits p97 competitively with respect to ATP with a Ki values of 0.22 μM. ML240 also inhibits labeling of only three protein kinase domains by >50% when tested at 20 μM: PIP5 K3 (belongs to phosphoinositide-3 kinase family), JAK1 JH2 (N-terminal pseudokinase domain of JAK1), and DNAPK (DNA-dependent protein kinase). ML240 (1.1, 3.3, 10, or 20 μM) induces executioner caspases 3 and 7 and triggers cell death independently of apical caspases 8 and 9. ML240 is cytotoxic to HCT15 and SW403 cells, with GI50s of 0.76 and 0.5 μM after treatment for 24 h, and 0.54 and 0.5 μM after treatment for 72 h, respectively.

分子结构图

ML-240