ML162

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ML162  纯度: 99.52%

ML162 是一种共价谷胱甘肽过氧化物酶 4 (GPX4) 抑制剂。ML162 对表达突变 RAS 癌基因的细胞系具有选择性的致死作用。

ML162

ML162 Chemical Structure

CAS No. : 1035072-16-2

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生物活性

ML162 is a covalent glutathione peroxidase 4 (GPX4) inhibitor. ML162 has a selective lethal effect on mutant RAS oncogene-expressing cell lines[1][2]

体外研究
(In Vitro)

ML162 (compound 1a) shows nanomolar potencies against two HRASG12V expressing cell lines, with IC50 values of 25 nM and 578 nM for HRASG12V-expressing and wild-type BJ fibroblasts, respectively[1].
ML162 (8 μM; 24 hours) treatment increases the expression of p62 and Nrf2 in chemoresistant HN3R and HN3-rslR cells, inactivates Keap1, and increases expression of the phospho-PERK-ATF4-SESN2 pathway[2].
ML162 induces the head and neck cancer (HNC) cell death to varying degrees, with parental HN3 cells more sensitive and cisplatin-resistant (HN3R) and acquired RSL3-resistant (HN3-rslR) cells less sensitive[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[2]

Cell Line: HN3R cells
Concentration: 8 μM
Incubation Time: 24 hours
Result: Increased the expression of p62 and Nrf2 in chemoresistant HN3R and HN3-rslR cells.

分子量

477.40

Formula

C23H22Cl2N2O3S

CAS 号

1035072-16-2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 100 mg/mL (209.47 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.0947 mL 10.4734 mL 20.9468 mL
5 mM 0.4189 mL 2.0947 mL 4.1894 mL
10 mM 0.2095 mL 1.0473 mL 2.0947 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.24 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.24 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. Michel Weïwer, et al. Development of small-molecule probes that selectively kill cells induced to express mutant RAS. Bioorg Med Chem Lett. 2012 Feb 15;22(4):1822-6.

    [2]. Daiha Shin, et al. Nrf2 inhibition reverses resistance to GPX4 inhibitor-induced ferroptosis in head and neck cancer. Free Radic Biol Med. 2018 Dec;129:454-462.

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