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首页-小分子抑制剂&激动剂-Nuclear Receptor/Transcription Factor-Keap1-Nrf2-ML385
ML385

Chemical Structure : ML385

CAS No.: 846557-71-9

ML385 (ML 385, ML-385)

货号: 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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10 mg ¥1280 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

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.

物理化学性质&存储条件

分子量 507.6459
分子式 C31H29N3O2S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
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]-

参考文献

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

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