1360705-96-9 Usage
Description
[4-[Bis(4-chlorophenyl)methyl]piperazin-1-yl]-(5-methyl-4-nitro-1,2-oxazol-3-yl)methanone, also known as ML210, is a synthetic compound with selective cytotoxicity towards HRAS expressing cells. It functions as a potent inhibitor of glutathione peroxidase 4 (GPX4), a selenoenzyme that safeguards cells from ferroptosis, a form of regulated cell death caused by iron-catalyzed formation of free radicals from lipid peroxides. ML210 has demonstrated the ability to induce ferroptosis in cancer cells, particularly in those exhibiting a high mesenchymal state and resistance to conventional treatments.
Uses
Used in Cancer Research:
ML210 is utilized as a GPX4 inhibitor to induce ferroptosis in cancer cells, particularly in treatment-resistant cell lines exhibiting a high mesenchymal state. Its application in this context aids in the study of cancer cell death mechanisms and the development of novel therapeutic strategies against cancer.
Used in Cellular Biology Studies:
ML210 serves as a tool to examine the effects of GPX4 inhibition on prominin2 expression and its impact on ferroptosis in adherent MCF10A and Hs578t cells. This application helps researchers understand the interplay between GPX4, prominin2, and cellular responses to oxidative stress, potentially leading to new insights in cellular biology and disease mechanisms.
Used in Drug Development:
As a GPX4 inhibitor, ML210 is a valuable compound in the development of new drugs targeting cancer cells with high HRAS expression. Its selective cytotoxicity and ability to induce ferroptosis make it a promising candidate for further research and potential incorporation into therapeutic agents for cancer treatment.
Biochem/physiol Actions
ML 210 induces non-apoptotic cell death in tumor cells expressing the RAS oncogene.
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
Check Digit Verification of cas no
The CAS Registry Mumber 1360705-96-9 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,3,6,0,7,0 and 5 respectively; the second part has 2 digits, 9 and 6 respectively.
Calculate Digit Verification of CAS Registry Number 1360705-96:
(9*1)+(8*3)+(7*6)+(6*0)+(5*7)+(4*0)+(3*5)+(2*9)+(1*6)=149
149 % 10 = 9
So 1360705-96-9 is a valid CAS Registry Number.
1360705-96-9Relevant articles and documents
Development of small-molecule probes that selectively kill cells induced to express mutant RAS
We?wer, Michel,Bittker, Joshua A.,Lewis, Timothy A.,Shimada, Kenichi,Yang, Wan Seok,MacPherson, Lawrence,Dandapani, Sivaraman,Palmer, Michelle,Stockwell, Brent R.,Schreiber, Stuart L.,Munoz, Benito
, p. 1822 - 1826 (2012/04/04)
Synthetic lethal screening is a chemical biology approach to identify small molecules that selectively kill oncogene-expressing cell lines with the goal of identifying pathways that provide specific targets against cancer cells. We performed a high-throughput screen of 303,282 compounds from the National Institutes of Health-Molecular Libraries Small Molecule Repository (NIH-MLSMR) against immortalized BJ fibroblasts expressing HRASG12V followed by a counterscreen of lethal compounds in a series of isogenic cells lacking the HRASG12V oncogene. This effort led to the identification of two novel molecular probes (PubChem CID 3689413, ML162 and CID 49766530, ML210) with nanomolar potencies and 4-23-fold selectivities, which can potentially be used for identifying oncogene-specific pathways and targets in cancer cells.
