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产品名称 | ATPase ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
(-)-Blebbistatin | 99%+ | ||||||||||||||||||
PF 03716556 |
++++
H+/K+-ATPase, pIC50: ~6.5 |
99% | |||||||||||||||||
Esomeprazole sodium | ✔ | 98% | |||||||||||||||||
BTB06584 | ✔ | 99% | |||||||||||||||||
Ciclopirox | ✔ | 97% | |||||||||||||||||
CB-5083 |
++++
p97 AAA ATPase, IC50: 11 nM |
99%+ | |||||||||||||||||
Ciclopirox olamine | ✔ | 99% | |||||||||||||||||
Brefeldin A |
+++
ATPase (HCT 116), IC50: 0.2 μM |
99%+ | |||||||||||||||||
Oligomycin A | ✔ | 99% | |||||||||||||||||
Sodium orthovanadate |
+++
(Na,K)-ATPase, IC50: 40 nM |
99% | |||||||||||||||||
Golgicide A | ✔ | 99%+ | |||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
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 UbG76V–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] |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.52mL 0.50mL 0.25mL |
12.61mL 2.52mL 1.26mL |
25.22mL 5.04mL 2.52mL |
CAS号 | 1346527-98-7 |
分子式 | C23H20N6O |
分子量 | 396.445 |
别名 | |
运输 | 蓝冰 |
存储条件 |
In solvent -20°C:3-6个月-80°C:12个月 Pure form Keep in dark place,Inert atmosphere,Room temperature |
溶解方案 |
DMSO: 12 mg/mL(30.27 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO |
动物实验配方 |