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EN4

CAS No. : 1197824-15-9

MCE 站：EN4

产品活性：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。

研究领域：Apoptosis

作用靶点：c-Myc

In Vitro: 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.
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.
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.
EN4 (50 μM; for 2 hours) treatment significantly reduced MYC thermal stability in 231MFP breast cancer cells.

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

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