USP7-IN-9

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

USP7-IN-9 

USP7-IN-9 是一种高效的 USP7 抑制剂，IC50 为 40.8 nM。USP7-IN-9 能诱导 RS4; 11 细胞凋亡 (apoptosis)，将细胞周期阻滞在 G0/G1 和 S 期。USP7-IN-9 降低癌蛋白 MDM2 和 DNMT1 的水平，升高抑癌蛋白 p53 和 p21 的水平。

USP7-IN-9

USP7-IN-9 Chemical Structure

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生物活性

USP7-IN-9 is a highly potent ubiquitin-specific protease 7 (USP7) inhibitor with an IC50 value of 40.8 nM. USP7-IN-9 can induce apoptosis and arrest cell progression at G0/G1 and S phases in RS4; 11 cells. USP7-IN-9 reduces the protein levels of oncoproteins MDM2 and DNMT1 and increases the protein levels of tumor suppressors p53 and p21[1].

IC50 & Target

IC50: 40.8 nM (USP7)[1]
体外研究
(In Vitro)

USP7-IN-9 (compound L55) (0-50 μM; 3 or 6 days) exhibits inhibitory activity against cancer cells[1].
USP7-IN-9 (1 μM; 0-72 hours) reduces the proportions of G2/M cells, and does not change the proportions of G0/G1 and S cells[1].
USP7-IN-9 (0.1-1 μM; 24 hours) reduces the protein levels of MDM2 and DNMT1 in a dose-dependent manner, and increases the protein levels of p53 and p21[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay

Cell Line: LNCaP, RS4; 11, HCT 116, NB4, K562 and HuH-7 cells[1]
Concentration: 0-50 μM
Incubation Time: LNCaP, 6 days; RS4; 11, HCT 116, HuH-7, K562 and NB4, 3 days
Result: Exhibited high inhibitory activity against LNCaP and RS4; 11 cells, with IC50s of 29.6 nM and 41.6 nM, respectively, and weak inhibitory activity on HCT 116, NB4, K562 and HuH-7 cells.

Cell Cycle Analysis

Cell Line: RS4; 11 cells[1]
Concentration: 1 μM
Incubation Time: 0, 24, 48 and 72 hours
Result: Reduced the proportions of G2/M cells, while the proportions of G0/G1 and S cells were not apparently altered.

Western Blot Analysis

Cell Line: RS4; 11 cells[1]
Concentration: 0.1, 0.3 and 1 μM
Incubation Time: 24 hours
Result: Reduced the protein levels of MDM2 and DNMT1 in a dose-dependent manner, and increased the protein levels of p53 and p21.

分子量

779.08

Formula

C32H33ClF6N6O8
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Li M, Liu S, Chen H, et al. N-benzylpiperidinol derivatives as novel USP7 inhibitors: Structure-activity relationships and X-ray crystallographic studies. Eur J Med Chem. 2020;199:112279.

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