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描述 | EN4 is a covalent ligand designed to target cysteine 171 (C171) of MYC. It exhibits selectivity for c-MYC over N-MYC and L-MYC. Moreover, EN4 effectively inhibits MYC transcriptional activity. |
体内研究 | The administration of EN4 (50 mg/kg; intraperitoneal injection; daily; for 3 weeks) led to a significant reduction in tumor growth in 231MFP breast tumor xenograft mice[1]. |
体外研究 | EN4 treatment at concentrations ranging from 1 to 50 μM for 72 hours markedly reduces proliferation of 231MFP breast cancer cells in a dose-dependent manner, achieving over 90% inhibition of proliferation at 50 μM[1]. EN4 treatment at a concentration of 50 μM for 60 hours significantly reduces the protein levels of representative MYC-regulated target genes, such as CDK2 and CDC25A. Additionally, EN4 treatment markedly decreases MYC levels[1]. EN4 demonstrates potent inhibition of both MYC/MAX binding to its DNA consensus sequence in vitro and MYC transcriptional activity in cells. It inhibits MYC/MAX binding to the E-box response element DNA consensus sequence in a dose-dependent manner, with an IC50 value of 6.7 μM. Additionally, EN4 inhibits MYC luciferase reporter activity in a dose-dependent manner, with an IC50 value of 2.8 μM[1]. EN4 treatment (50 μM; for 2 hours) resulted in a significant reduction in the thermal stability of MYC in 231MFP breast cancer cells[1]. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.40mL 0.48mL 0.24mL |
12.01mL 2.40mL 1.20mL |
24.01mL 4.80mL 2.40mL |
CAS号 | 1197824-15-9 |
分子式 | C25H24N2O4 |
分子量 | 416.469 |
别名 | |
运输 | 蓝冰 |
存储条件 |
In solvent -20°C:3-6个月-80°C:12个月 Pure form Sealed in dry,Room Temperature |
溶解度 |
DMSO: 120 mg/mL(288.14 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO |
动物实验配方 |