usp7 in 3

USP7-IN-3 is a potent and selective allosteric inhibitor of ubiquitin-specific protease 7 (USP7).

USP28-IN-3 is a highly selective USP28 inhibitor with an IC50 value of 0.1 μM against USP28.USP28-IN-3 exhibits anticancer activity and inhibits USP2, USP7, USP8, USP9x, UCHL3, and UCHL5.USP28-IN-3 is cytotoxic to human colorectal and lung squamous carcinoma cells, inhibiting c-cells and c-neutralizing c-neutralizing c-neutralizing c-neutralizing c-neutralizing c-neutralizing c-neutralizing c-cells through the ubiquitin-proteasome system. -proteasome system to dose-dependently downregulate cellular levels of c-Myc.

USP7-IN-18 (Compound X21) serves as a novel USP7 inhibitor by directly suppressing enzyme activity and modulating downstream pathways, including the newly identified PCLAF target. At concentrations of 0.25-1 μM for 24 hours, it exhibits inhibitory effects. USP7-IN-18 effectively reduces proliferation in leukemia (RS4;11) and colon cancer (MC38/CT26.WT) cells at 0.01-100 μM over 72 hours. It demonstrates high selectivity for USP7 at 2.5 μM within 0.5 hours, surpassing eight other deubiquitinating enzymes. SPR analysis shows that at 1.95-2000 nM for 3 minutes, the compound binds the catalytic domain of USP7 with a KD value of 4.9 μM.

USP8-IN-3 is a potent inhibitor of the deubiquitinating enzymes USP7 and USP8, with IC50 of 4.0 μM against USP8D. USP8-IN-3 inhibited the proliferation of GH3 and H1957 cells with GI50 values of 37.03 μM and 6.01 μM, respectively. USP8-IN-3 is a potential compound for the treatment of cancer and viral infections.

Benzamide, 4-[6-amino-4-ethyl-5-(4-hydroxyphenyl)-3-pyridinyl]-N-methyl- is a selective ubiquitin-specific protease 7 (USP7) inhibitor with an IC50 of 1.4 μM. USP7-IN-8 (GNE-6776) has anticancer effects.