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[CAS NO. 1035072-16-2] ML162
| Ships within | Stock | Price | Qty | Total |
Please click "REQUEST A QUOTE" button if there is no stock, or you need other sizes or custom synthesis.
| Catalog: | HY-100002 |
| Brand: | MCE |
| CAS: | 1035072-16-2 |
Overview
| MDL | - |
|---|---|
| Molecular Weight | 477.40 |
| Molecular Formula | C23H22Cl2N2O3S |
| SMILES | O=C(CCl)N(C(C1=CC=CS1)C(NCCC2=CC=CC=C2)=O)C3=CC=C(OC)C(Cl)=C3 |
1 Publications Citing Use of MCE
Summary
ML162 is a covalent glutathione peroxidase 4 (GPX4) inhibitor. ML162 has a selective lethal effect on mutant RAS oncogene-expressing cell lines [1] [2]
In Vitro
ML162 (compound 1a) shows nanomolar potencies against two HRAS
G12V
expressing cell lines, with IC
50
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]
.
MCE 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. |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 100 mg/mL ( 209.47 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 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 |
-
1.
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 2.5 mg/mL (5.24 mM); Clear solution
References
- [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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