Chemical Structure : ML-385
CAS No.: 846557-71-9
Catalog No.: PC-42187Not For Human Use, Lab Use Only.
ML 385 is a first-in-class small molecule inhibitor of NRF2 that binds to Neh1 DNA binding domain of NRF2 (IC50=1.9 uM) and inhibits the downstream target gene expression.
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ML 385 is a first-in-class small molecule inhibitor of NRF2 that binds to Neh1 DNA binding domain of NRF2 (IC50=1.9 uM) and inhibits the downstream target gene expression.
ML-385 blocks the binding of the NRF2-MAFG complex to the ARE sequence in the promoter and reduces transcriptional activity.
ML-385 inhibits NRF2 signaling in lung cancer cells with KEAP1 mutations, shows selective cytotoxicity in NSCLC cells with KEAP1 mutations and potentiates the toxicity chemotherapy drugs.
ML-385 shows anti-tumor activity in NSCLC both as a single agent and in combination with carboplatin in preclinical models of NSCLC.
M.Wt | 507.6459 | |
Formula | C31H29N3O2S | |
Appearance | Solid | |
Storage |
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Solubility |
DMSO: ≥ 30 mg/mL |
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Chemical Name/SMILES |
1,3-Benzodioxole-5-acetamide, N-[4-[2,3-dihydro-1-(2-methylbenzoyl)-1H-indol-5-yl]-5-methyl-2-thiazolyl]- |
1. Singh A, et al. ACS Chem Biol. 2016 Nov 18;11(11):3214-3225.
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