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ML-210

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Chemical Structure| 1360705-96-9 同义名 : DPI10;CID 49766530;SML 0521;DPI compound 10
CAS号 : 1360705-96-9
货号 : A824339
分子式 : C22H20Cl2N4O4
纯度 : 99%+
分子量 : 475.325
MDL号 : MFCD22666407
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 25 mg/mL(52.6 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 GPX4 (glutathione peroxidase 4) is a selenoprotein that plays a critical role in protecting cells from lipid peroxidation and ferroptosis by reducing lipid hydroperoxides to their corresponding lipid alcohols. It is unique in its ability to reduce complex lipid hydroperoxides. ML210 is a selective covalent inhibitor of cellular GPX4 with an EC50 value of 0.04 μM. It exhibits a pattern of cell killing across 821 cancer cell lines. Furthermore, ML210 may be a prodrug that undergoes chemical transformation in cells to covalently modify GPX4. Treatment of cells with ML210 (10 μM, 90 min) led to accumulation of lipid hydroperoxides in LOX-IMVI cells[1]. Moreover, ML-210 has IC50 values of 71, 107 and 272 nM for BJeLR (HRASV12), DRD and BJeH-LT (without HRASV12) cell lines, respectively[2].
作用机制 In cells, ML210 reacts with cysteine and glutathione to form +434 Da ML210-GPX4 adduct[1].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.10mL

0.42mL

0.21mL

10.52mL

2.10mL

1.05mL

21.04mL

4.21mL

2.10mL
参考文献

[1]Selective covalent targeting of GPX4 using masked nitrile-oxide electrophiles

[2]Weïwer M, Bittker JA, Lewis TA, et al. Development of small-molecule probes that selectively kill cells induced to express mutant RAS. Bioorg Med Chem Lett. 2012;22(4):1822-1826