CAS:1346527-98-7ML240

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ML240 is a selective, ATP-competitive p97 inhibitor with IC50 values of 100 nM.

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18817579266

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18817579266

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实验数据

技术信息

CAS号

1346527-98-7

储存条件

分子式

C23H20N6O

运输

蓝冰

分子量

396.44

别名

溶解度

动物实验配方

生物活性

靶点 p97

IC50:100nM
描述ML240 is a p97 ATPase inhibitor with IC50 values of 110nM and 900nM for inhibition of p97 ATPase activity and degradation of p97-dependent reporter Ub^G76V–GFP, and inhibited p97 competitively with respect to ATP with a Ki value of 0.22 μM. Also ML240 exhibited cytotoxicity on HCT15 and SW403 cells with GI50 values of 0.54μM and 0.5μM, respectively, and synergized with the proteasome inhibitor MG132 to kill multiple colon cancer cell lines. Treatment with ML240 at concentration ranging in 5–10μM impaired the endoplasmic-reticulum-associated degradation (ERAD) pathway, causing accumulation of ubiquitin conjugates in the nuclear plus membrane and cytosolic compartments in SW403 cells. The induction of activation of caspases 3 and 7 and apoptosis could be observed in MIN and CIN colon cancer lines were treated with ML240 at concentration of 1.1, 3.3, 10, or 20μM for 7 h^[1].
作用机制ML240 can inhibit p97 in an ATP-competitive manner.^[1]