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Merck
CN

SML1833

Sigma-Aldrich

ML385

≥98% (HPLC), powder, Nrf2 transcription factor inhibitor

别名:

N- [4- [2,3-二氢-1-(2-甲基苯甲酰基)-1H-吲哚-5-基] -5-甲基-2-噻唑基] -1,3-苯并二氧杂环戊-5-基 -乙酰胺

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About This Item

经验公式(希尔记法):
C29H25N3O4S
分子量:
511.59
UNSPSC代码:
12352200
NACRES:
NA.77

产品名称

ML385, ≥98% (HPLC)

质量水平

方案

≥98% (HPLC)

表单

powder

颜色

white to beige

溶解性

DMSO: 10 mg/mL, clear

储存温度

2-8°C

SMILES字符串

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

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)

InChI key

LINHYWKZVCNAMQ-UHFFFAOYSA-N

生化/生理作用

ML385 通过与 Neh1 结合来抑制 Nrf2 转录因子的活性,Neh1 是一个 CNC-bZIP 结构域,其能够使 Nrf2 与小 Maf 蛋白异二聚化,从而阻断 NRF2 转录活性。人们已对激活 Nrf2 进行了大量研究,因为它诱导细胞保护抗氧化基因的表达。然而,一些癌细胞可能以类似的方式利用 Nrf2 来使其存活。Nrf2 在某些癌症(例如非小细胞肺癌(NSCLC))中过表达,这通常是由于 KEAP1 功能缺失突变引起的,KEAP1 靶向 Nrf2 导致其发生蛋白酶体降解。研究发现 ML385 对带有 KEAP1 突变的 NSCLC 细胞具有特异性和选择性的抗肿瘤活性。

储存分类代码

11 - Combustible Solids

WGK

WGK 3

闪点(°F)

Not applicable

闪点(°C)

Not applicable


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