ML240

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Chemical Structure| 1346527-98-7 同义名 : -
CAS号 : 1346527-98-7
货号 : A104721
分子式 : C23H20N6O
纯度 : 99%+
分子量 : 396.445
MDL号 : MFCD28137687
存储条件：

Pure form Keep in dark place,Inert atmosphere,Room temperature

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

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：
生物活性
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]
实验方案
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
参考文献

[1]Chou TF, Li K, et al. Structure-activity relationship study reveals ML240 and ML241 as potent and selective inhibitors of p97 ATPase. ChemMedChem. 2013 Feb;8(2):297-312.