ML-162 |
| Katalog-Nr.GC44214 |
ML-162 ist ein kovalenter Glutathionperoxidase 4 (GPX4)-Inhibitor. ML-162 hat eine selektive tödliche Wirkung auf mutierte RAS-Onkogen-exprimierende Zelllinien
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1035072-16-2
Sample solution is provided at 25 µL, 10mM.
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ML-162 is a small molecule that inhibits Glutathione peroxidase 4 (GPX4), with an IC50 value of 1.42µM[1]. ML-162 potently suppresses thioredoxin reductase 1 (TXNRD1) with an IC50 value of 19.5µM[2]. ML-162 has been extensively used as a model compound to explore the covalent binding of ML-162 to the active and catalytic sites of GPX4 and to develop related derivatives[3].
In vitro, ML-162 treatment for 48 hours significantly inhibited the proliferation of HT1080 cells with an IC50 value of 0.6±0.09μM[4]. Treatment of HK-2 cells with 1μM ML-162 for 24 hours significantly inhibited cell viability and induced ferroptosis[5]. Treatment with 10μM ML-162 for 24h significantly caused the cell death of Pfa1 cells and blocked the inhibition of ferroptosis activity of 5mM N-acetyl-l-cysteine (NAC) [6].
In vivo, ML-162 treatment via intravenous injection at a dose of 20mg/kg/day for 19 days significantly inhibited tumor growth in a xenografted BALB/c nude mice model bearing the HT1080 tumor, and reduced GPX4 and Bcl-2 levels in tumor tissues[4]. Combined treatment with 1mg/kg of ML-162 and 10mg/kg of C7 via intraperitoneal injection twice every three days for 21 days significantly inhibited tumor growth in the mouse of HepG2 xenograft model without affecting the body weight of the mice[7]. Daily intraperitoneal injection of ML-162 at a dose of 40mg/kg/day for 2 weeks significantly induced tumor ferroptosis in a mouse model of breast cancer and resulted in increased levels of PTGS2, MDA, and 4-HNE in tumor tissues[8].
References:
[1] Kunishige R, Noguchi Y, Okamoto N, et al. Protein covariation networks for elucidating ferroptosis inducer mechanisms and potential synergistic drug targets[J]. Communications Biology, 2025, 8(1): 480.
[2] Cheff D M, Huang C, Scholzen K C, et al. The ferroptosis inducing compounds RSL3 and ML162 are not direct inhibitors of GPX4 but of TXNRD1[J]. Redox Biology, 2023, 62: 102703.
[3] Moosmayer D, Hilpmann A, Hoffmann J, et al. Crystal structures of the selenoprotein glutathione peroxidase 4 in its apo form and in complex with the covalently bound inhibitor ML162[J]. Biological Crystallography, 2021, 77(2): 237-248.
[4] Ma F, Li Y, Cai M, et al. ML162 derivatives incorporating a naphthoquinone unit as ferroptosis/apoptosis inducers: design, synthesis, anti-cancer activity, and drug-resistance reversal evaluation[J]. European Journal of Medicinal Chemistry, 2024, 270: 116387.
[5] Homma T, Tada C, Yamauchi M, et al. Identification of a novel tetrahydroxynaphthalene derivative by chemical screening with ferroptosis inhibitory activity and promising therapeutic potential[J]. Free Radical Research, 2025, 59(4): 321-331.
[6] Zheng J, Zhang W, Ito J, et al. N-acetyl-l-cysteine averts ferroptosis by fostering glutathione peroxidase 4[J]. Cell Chemical Biology, 2025, 32(5): 767-775. e5.
[7] Zhu J, Tan Q, Fan S, et al. PROTAC degraders of FSP1 act as potent GPX4 sensitizers to induce ferroptosis for hepatoma treatment[J]. Chinese Chemical Letters, 2025: 111285.
[8] Yang F, Xiao Y, Ding J H, et al. Ferroptosis heterogeneity in triple-negative breast cancer reveals an innovative immunotherapy combination strategy[J]. Cell metabolism, 2023, 35(1): 84-100. e8.
| Cell experiment [1]: | |
Cell lines | HepG2 cells |
Preparation Method | The HepG2 cells were cultured in DMEM (high glucose), supplemented with 10% fetal bovine serum (FBS), at 37℃ in a humidified atmosphere containing 5% CO2. HepG2 cells were seeded into 96-well plates and incubated for 24h. The cells were treated with either the vehicle or ML-162 (100nM) for 0, 6, 12, 18, 24h, respectively. Afterward, 10µl of CCK-8 solution was added to each well, and the absorbance was measured at 450nm. |
Reaction Conditions | 100nM; 0, 6, 12, 18, 24h |
Applications | ML-162 treatment reduced the cell viability of HepG2 cells in a time-dependent manner. |
| Animal experiment [2]: | |
Animal models | BALB/c nude mice |
Preparation Method | HT1080 xenograft model was established by subcutaneous injection of HT1080 cells (4×106/mouse) into the right abdomen of BALB/c nude mice in standard environment. When the tumor size was about 80-100mm3, the mice were randomly divided into four groups (5 mice in each group), including saline group, ML-162 (20mg/kg), GIC-20 (20mg/kg), and GIC-20 (40mg/kg). Mice were injected intravenously daily for 19 days, and tumor volume and body weight were recorded every other day during drug treatment. After treatment, the mice were painlessly sacrificed, and the tumor tissues were collected for hematoxylin-eosin (H&E) and immunohistochemistry. |
Dosage form | 20mg/kg/day for 19 days; i.v. |
Applications | ML-162 treatment significantly inhibited tumor growth in mice in vivo and reduced GPX4 and Bcl-2 levels in tumor tissues. |
References: | |
| Cas No. | 1035072-16-2 | SDF | |
| Chemical Name | α-[(2-chloroacetyl)(3-chloro-4-methoxyphenyl)amino]-N-(2-phenylethyl)-2-thiopheneacetamide | ||
| Canonical SMILES | O=C(C(N(C(CCl)=O)C1=CC=C(OC)C(Cl)=C1)C2=CC=CS2)NCCC3=CC=CC=C3 | ||
| Formula | C23H22Cl2N2O3S | M.Wt | 477.4 |
| Löslichkeit | 1mg/mL in ethanol, 25mg/ml in DMSO, 10mg/mL in DMF | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.0947 mL | 10.4734 mL | 20.9468 mL |
| 5 mM | 418.9 μL | 2.0947 mL | 4.1894 mL |
| 10 mM | 209.5 μL | 1.0473 mL | 2.0947 mL |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Quality Control & SDS
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- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
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Average Rating: 5 (Based on Reviews and 19 reference(s) in Google Scholar.)
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