10074-G5

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Chemical Structure| 413611-93-5 同义名 : -
CAS号 : 413611-93-5
货号 : A188479
分子式 : C18H12N4O3
纯度 : 99%
分子量 : 332.31
MDL号 : MFCD00576774
存储条件：

Pure form Keep in dark place, sealed in dry, room temperature

In solvent -20°C:3-6个月-80°C:12个月
溶解度 : -
动物实验配方：
生物活性
描述 10074-G5 is effective in hindering the proliferation of Daudi Burkitt's lymphoma cells and in interfering with the dimerization of c-Myc/Max. It exhibits IC50 values of 15.6 μM for Daudi cells and 13.5 μM for HL-60 cells[1]. 10074-G5 interacts with the Myc peptide Myc353-437, exhibiting a Kd value of 2.8 μM within the Arg363-Ile381 region. It attaches within a pocket formed by a bend (Asp379-Ile381) at the N-terminal end of an induced helical segment (Leu370–Arg378)[2].
作用机制 10074-G5 can disrupt the dimeric complex formed between its basic helix-loop-helix leucine zipper (bHLHZip) domain and a similar domain on its dimerization partner, Max. Similar to 10058-F4, 10074-G5 binds to c-Myc, but a distinct region[1]. [1] [2] [3] [4] [5]
细胞研究
细胞系 浓度 检测类型 检测时间 活性说明 数据源
Daudi cells Cytotoxicity assay 3 to 5 days Cytotoxicity against human Daudi cells assessed as growth inhibition after 3 to 5 days by MTT assay, IC50=10 Μm 23177256
HL60 cells Cytotoxicity assay 3 to 5 days Cytotoxicity against human HL60 cells assessed as growth inhibition after 3 to 5 days by MTT assay, IC50=30 μM 23177256
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.01mL

0.60mL

0.30mL

15.05mL

3.01mL

1.50mL

30.09mL

6.02mL

3.01mL
参考文献

[1]Hammoudeh DI, Follis AV, et al. Multiple independent binding sites for small-molecule inhibitors on the oncoprotein c-Myc. J Am Chem Soc. 2009 Jun 3;131(21):7390-401.

[2]Yap JL, Wang H, et al. Pharmacophore identification of c-Myc inhibitor 10074-G5. Bioorg Med Chem Lett. 2013 Jan 1;23(1):370-4.

[3]Yin X, Giap C, et al. Low molecular weight inhibitors of Myc-Max interaction and function. Oncogene. 2003 Sep 18;22(40):6151-9.

[4]Clausen DM, Guo J, et al. In vitro cytotoxicity and in vivo efficacy, pharmacokinetics, and metabolism of 10074-G5, a novel small-molecule inhibitor of c-Myc/Max dimerization. J Pharmacol Exp Ther. 2010 Dec;335(3):715-27.

[5]Follis AV, Hammoudeh DI, et al. Structural rationale for the coupled binding and unfolding of the c-Myc oncoprotein by small molecules. Chem Biol. 2008 Nov 24;15(11):1149-55.