846557-71-9
Chemical Structure
ML385
- CAS No.: 846557-71-9
- Formula:C29H25N3O4S
- Molecular Weight:511.59
IUPAC Name: 2-(benzo[d][1,3]dioxol-5-yl)-N-(5-methyl-4-(1-(2-methylbenzoyl)indolin-5-yl)thiazol-2-yl)acetamide
InChIKey: LINHYWKZVCNAMQ-UHFFFAOYSA-N
SMILES: O=C(NC1=NC(C2=CC=C(N(C(C3=C(C)C=CC=C3)=O)CC4)C4=C2)=C(C)S1)CC5=CC(OCO6)=C6C=C5
Biological Activity: ML385 is a potent and selective Nrf2 inhibitor with an IC50 of 1.9 μM. ML385 directly binds to the Neh1 domain of NRF2, interferes with the binding of the MAFG-NRF2 protein complex to the antioxidant response element (ARE) DNA sequence, thereby blocking the expression of downstream target genes of NRF2. ML385 can be used in studies related to adult T-cell leukemia, breast cancer, myocardial ischemia/reperfusion injury, non-small cell lung cancer, esophageal squamous cell carcinoma, head and neck squamous cell carcinoma, and lung squamous cell carcinoma[1][2][3][4][5][6][7].
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ML385 | 99.84% | ML385 is a potent and selective Nrf2 inhibitor with an IC50 of 1.9 μM. ML385 directly binds to the Neh1 domain of NRF2, interferes with the binding of the MAFG-NRF2 protein complex to the antioxidant response element (ARE) DNA sequence, thereby blocking the expression of downstream target genes of NRF2. ML385 can be used in studies related to adult T-cell leukemia, breast cancer, myocardial ischemia/reperfusion injury, non-small cell lung cancer, esophageal squamous cell carcinoma, head and neck squamous cell carcinoma, and lung squamous cell carcinoma. | ||||||||||||||||||||
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ML385 (Standard) | ≥98% | ML385 (Standard) is the analytical standard of ML385 (HY-100523). This product is intended for research and analytical applications. ML385 is a potent and selective Nrf2 inhibitor with an IC50 of 1.9 μM. ML385 directly binds to the Neh1 domain of NRF2, interferes with the binding of the MAFG-NRF2 protein complex to the antioxidant response element (ARE) DNA sequence, thereby blocking the expression of downstream target genes of NRF2. ML385 can be used in studies related to adult T-cell leukemia, breast cancer, myocardial ischemia/reperfusion injury, non-small cell lung cancer, esophageal squamous cell carcinoma, head and neck squamous cell carcinoma, and lung squamous cell carcinoma. | ||||||||||||||||||||
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References
- [1]. Singh A, et al. Small Molecule Inhibitor of NRF2 Selectively Intervenes Therapeutic Resistance in KEAP1-Deficient NSCLC Tumors. ACS chemical biology. 2016 Nov 18;11(11):3214-3225. [Content Brief]
- [2]. Ji L, et al. The NRF2 antagonist ML385 inhibits PI3K-mTOR signaling and growth of lung squamous cell carcinoma cells. Cancer medicine. 2023 Mar;12(5):5688-5702. [Content Brief]
- [3]. Yan L, et al. ML385 promotes ferroptosis and radiotherapy sensitivity by inhibiting the NRF2-SLC7A11 pathway in esophageal squamous cell carcinoma. Medical oncology (Northwood, London, England). 2024 Nov 07;41(12):309. [Content Brief]
- [4]. Ishikawa C, et al. ML385, a selective inhibitor of Nrf2, demonstrates efficacy in the treatment of adult T-cell leukemia. Leukemia & lymphoma. 2025 Apr;66(4):721-732. [Content Brief]
- [5]. Jeong EJ, et al. The Effects of ML385 on Head and Neck Squamous Cell Carcinoma: Implications for NRF2 Inhibition as a Therapeutic Strategy. International journal of molecular sciences. 2024 Jun 27;25(13):7011. [Content Brief]
- [6]. Yuan J, et al. ML385 increases ferroptosis via inhibiting Nrf2/HO-1 pathway to enhances the sensitivity of MCF-7 TAMR to tamoxifen. Naunyn-Schmiedeberg's archives of pharmacology. 2025 Nov;398(11):16081-16093. [Content Brief]
- [7]. Xu C, et al. Cardioprotective effects of melatonin against myocardial ischaemia/reperfusion injury: Activation of AMPK/Nrf2 pathway. Journal of cellular and molecular medicine. 2021 Jun 14;25(13):6455-9.
