[4-[Bis(4-chlorophenyl)methyl]piperazin-1-yl]-(5-methyl-4-nitro-1,2-oxazol-3-yl)methanone Chemical Properties

Boiling point:

644.7±55.0 °C(Predicted)

Density 

1.415±0.06 g/cm3(Predicted)

storage temp. 

2-8°C

solubility 

Soluble in DMSO (up to 30 mg/ml)

form 

powder

pka

4.69±0.10(Predicted)

color 

white to beige

Stability:

Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.

Safety Information

WGK Germany 

3

[4-[Bis(4-chlorophenyl)methyl]piperazin-1-yl]-(5-methyl-4-nitro-1,2-oxazol-3-yl)methanone Usage And Synthesis

Description

ML210 (CAS 1360705-96-9) is selectively synthetic lethal to HRAS expressing cells compared to isogenic non-HRAS cells (IC50?= 7.1 nM for BJeLR (expressing HRASg12v) cells vs IC50?= 272 nM for BJeH-LT (non-HRAS expressing) cells.1?ML210 is able to inhibit glutathione peroxidase 4 (GPX4), an important selenoenzyme that protects cells from ferroptosis caused by iron catalyzed formation of free radicals from lipid peroxides.2,3?Treatment of several treatment-resistant cancer cell lines exhibiting a high mesenchymal state with ML210 resulted in selective induction of ferroptosis.3

Uses

ML 210 has been used as a glutathione peroxidase 4 (GPX4) inhibitor to induce ferroptosis in cancer cells. It has also been used as a GPX4 inhibitor to examine whether pharmacological inhibition of GPX4 altered prominin2 expression and impacted ferroptosis in adherent MCF10A and Hs578t cells.

Biochem/physiol Actions

ML 210 induces non-apoptotic cell death in tumor cells expressing the RAS oncogene.

storage

Store at -20°C

References

1) Weiwer?et al.?(2012),?Development of small-molecule probes that selectively kill cells induced to express mutant RAS; Bioorg. Med. Chem. Lett.?22?1822 2) Yang?et al.?(2014),?Regulation of Ferroptotic Cancer Cell Death by GPX4; Cell?156?317 3) Viswanathan?et al.?(2017),?Dependency of a therapy-resistant state of cancer cells on a lipid peroxidase pathway; Nature?547?453

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