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.
体外研究
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.
XL177A (1 μM) induces complete G1 arrest in MCF7 cells after 24 hours.
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.
Western Blot Analysis
Cell Line:
MCF7 cells
Concentration:
0.001, 0.01, 0.1, 1, 10 μM
Incubation Time:
18-24 hours
Result:
The p53 and p21 protein levels remained high, but MDM2 protein levels matched DMSO control.
分子式
C48H57ClN8O5
分子量
861.47
CAS号
2417089-74-6
运输条件
Room temperature in continental US; may vary elsewhere.