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EN4
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
EN4图片
规格:98%
分子量:416.47
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议

产品介绍
EN4 是一种针对 MYC 的半胱氨酸 171 (C171) 的共价配体。EN4 对 c-MYC 的选择性高于 N-MYC 和 L-MYC。EN4 抑制 MYC 转录活性,下调 MYC 靶标,并具有抗肿瘤作用。
货号:ajcx33424
CAS:1197824-15-9
分子式:C25H24N2O4
分子量:416.47
溶解度:DMSO : 250 mg/mL (600.28 mM; Need ultrasonic)
纯度:98%
存储:Store at -20°C
库存:现货

Background:

EN4 is a covalent ligand that targets cysteine 171 (C171) of MYC. EN4 is selective for c-MYC over N-MYC and L-MYC. EN4 inhibits MYC transcriptional activity, downregulates MYC targets, and impairs tumorigenesis[1].

EN4 (1-50 μM; for 72 hours) treatment significantly impaires 231MFP breast cancer cell proliferation in a dosedependent manner, with >90% inhibition of proliferation at 50 μM[1].EN4 (50 μM; for 60 hours) treatment significantly decreases the protein levels of representative MYC-regulated target genes, including CDK2 and CDC25A. EN4 treatment also substantially reduces MYC levels[1].EN4 shows the strongest inhibition of both MYC/MAX binding to its DNA consensus sequence in vitro as well as MYC transcriptional activity in cells. EN4 inhibited MYC/MAX binding to the E-box response element DNA consensus sequence in a dose-responsive manner with an IC50 value of 6.7 μM. EN4 also inhibits MYC luciferase reporter activity in a dose-responsive manner with an IC50 value of 2.8 μM[1]. EN4 (50 μM; for 2 hours) treatment significantly reduced MYC thermal stability in 231MFP breast cancer cells[1].

EN4 (50 mg/kg; intraperitoneal injection; daily; for 3 weeks) treatment significantly attenuated tumor growth in 231MFP breast tumor xenograft mice[1].

[1]. Lydia Boike, et al. Discovery of a Functional Covalent Ligand Targeting an Intrinsically Disordered Cysteine within MYC. Cell Chem Biol. 2021 Jan 21;28(1):4-13.e17.