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ML385

Chemical Structure : ML385

CAS No.: 846557-71-9

ML385 (ML 385, ML-385)

Catalog No.: PC-42187Not For Human Use, Lab Use Only.

ML385 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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Biological Activity

ML385 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.
ML385 blocks the binding of the NRF2-MAFG complex to the ARE sequence in the promoter and reduces transcriptional activity.
ML385 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.
ML385 shows anti-tumor activity in NSCLC both as a single agent and in combination with carboplatin in preclinical models of NSCLC.

Physicochemical Properties

M.Wt 507.6459
Formula C31H29N3O2S
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

DMSO: ≥ 30 mg/mL

Chemical Name/SMILES

1,3-Benzodioxole-5-acetamide, N-[4-[2,3-dihydro-1-(2-methylbenzoyl)-1H-indol-5-yl]-5-methyl-2-thiazolyl]-

References

1. Singh A, et al. ACS Chem Biol. 2016 Nov 18;11(11):3214-3225.

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