XL177A 是一种高效选择性的不可逆 USP7 抑制剂，IC50 为 0.34 nM。XL177A 通过 p53 依赖性机制引发癌杀伤细胞作用。
货号:ajcx33878
CAS:2417089-74-6
分子式:C48H57ClN8O5
分子量：861.47
溶解度:DMSO : 50 mg/mL (58.04 mM; Need ultrasonic)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

XL177A is a highly potent and selective irreversible USP7 inhibitor with an IC50 of 0.34 nM. XL177A elicits cancer cell killing through a p53-dependent mechanism[1].

XL177A is a potent USP7 inhibitor and p53 stabilizer in cyto. XL177A suppresses cancer cell growth predominantly through a p53-dependent mechanism. XL177A labels the catalytic cysteine, C223, of USP7 with exquisite selectivity for USP7 across the DUBome and human proteome[1]. XL177A (1 μM) induces complete G1 arrest in MCF7 cells after 24 hours[1].Treatment of MCF7 cells, which express WT TP53, with XL177A (0.001- 10 μM) induces rapid degradation of HDM2 within 2 hours, followed by increases in p53 and downstream p21 protein levels[1].

[1]. Nathan J Schauer, et al. Selective USP7 inhibition elicits cancer cell killing through a p53-dependent mechanism. Sci Rep.2020 Mar 24;10(1):5324.