SML1833
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
Product Name
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。
ML385 通过与 Neh1 结合而抑制 Nrf2 转录因子的活性。
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
历史批次信息供参考:
分析证书(COA)
Lot/Batch Number
Yuanyuan Bian et al.
Molecular medicine reports, 25(1) (2021-11-10)
Vitiligo is a depigmentation disease commonly seen in clinical practice, mainly involving loss of functional epidermal pigment cells and hair follicle melanocytes. Narrow‑band ultraviolet B (NB‑UVB) has emerged as the first choice of treatment for vitiligo, but long‑term exposure may have
Amy M Ehrlich et al.
BMC microbiology, 20(1), 357-357 (2020-11-24)
Bifidobacterium longum subsp. infantis (B. infantis) is a commensal bacterium that colonizes the gastrointestinal tract of breast-fed infants. B. infantis can efficiently utilize the abundant supply of oligosaccharides found in human milk (HMO) to help establish residence. We hypothesized that
Etay Ziv et al.
Radiology, 297(1), 225-234 (2020-08-12)
Background Intermediate stage hepatocellular carcinomas (HCCs) are treated by inducing ischemic cell death with transarterial embolization (TAE) or transarterial chemoembolization (TACE). A subset of HCCs harbor nuclear factor E2-related factor 2 (NRF2), a major regulator of the oxidative stress response
Oxidized phospholipids regulate amino acid metabolism through MTHFD2 to facilitate nucleotide release in endothelial cells.
Hitzel J, et al.
Nature Communications, 9(1), 2292-2292 (2018)
Xi-Juan Zhang et al.
Biological & pharmaceutical bulletin, 44(3), 396-403 (2021-03-02)
Ferulic acid (FA) has potential therapeutic effects in multiple diseases including cardiovascular diseases. However, the effect and molecular basis of FA in heart failure (HF) has not been thoroughly elucidated. Herein, we investigated the roles and mechanisms of FA in
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