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ML385
- Soluble in DMSO
- MF: C29H25N3O4S
- MW: 511.59
Description
ML385 is an inhibitor of nuclear factor erythroid 2-related factor 2 (NRF2) (IC50 value 1.9 μM), blocks NRF2 transcriptional activity, and enhances the efficacy of carboplatin and other chemotherapeutic drugs in lung cancer cells (NSCLC). Specifically, ML385 binds to Neh1, the Cap ‘N’ Collar Basic Leucine Zipper (CNC-bZIP) domain of NRF2, and interferes with the binding of the V-Maf Avian Musculoaponeurotic Fibrosarcoma Oncogene Homologue G (MAFG)-NRF2 protein complex to regulatory DNA binding sequences. ML385 shows specificity and selectivity for NSCLC cells with KEAP1 mutation.
More Information
| Parent CAS No. | 846557-71-9 |
|---|---|
| Chemical Name | 2-(Benzo[d][1,3]dioxol-5-yl)-N-(5-methyl-4-(1-(2-methylbenzoyl)indolin-5-yl)thiazol-2-yl)acetamide |
| SMILES | C12OCOC=1C=CC(CC(NC1=NC(C3C=C4CCN(C(C5C=CC=CC=5C)=O)C4=CC=3)=C(C)S1)=O)=C2 |
| MFCD | N.A. |
| InChi | InChI=1S/C29H25N3O4S/c1-17-5-3-4-6-22(17)28(34)32-12-11-20-15-21(8-9-23(20)32)27-18(2)37-29(31-27)30-26(33)14-19-7-10-24-25(13-19)36-16-35-24/h3-10,13,15H,11-12,14,16H2,1-2H3,(H,30,31,33) |
| InChiKey | LINHYWKZVCNAMQ-UHFFFAOYSA-N |
| CID | 1383822 |
| Short Description | NRF2 inhibitor |
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