product name
ML385, ≥98% (HPLC)
质量水平
检测方案
≥98% (HPLC)
形式
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
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。
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
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