usp8

OTUB1/USP8-IN-1 is a potent OTUB1/USP8 inhibitor with potential anticancer activity, demonstrating IC50 values of 0.17 nM for OTUB1 and 0.28 nM for USP8. OTUB1/USP8-IN-1 can be used in the study of non-small-cell lung cancer.

USP8-IN-1 is an inhibitor of USP8 with an IC 50 of 1.9 μM. USP8-IN-1 inhibits H1975 cell growth with a GI 50 of 82.04 μM [1].

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.

USP8-IN-2 is a potent inhibitor of the deubiquitinating enzymes USP7 and USP8, with an IC50 of 4.0 μM against USP8D. USP8-IN-2 is a potential compound for the treatment of cancer and viral infections.

OTUB1/USP8-IN-1 HCL is a potent dual inhibitor of OTUB1 and USP8 with potential antitumour activity, inhibiting both OTUB1 and USP8. OTUB1/USP8-IN-1 may be used in the study of leukaemia.

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.

DUB-IN-1, with an IC50 value of 0.24 for USP8, is an active inhibitor of ubiquitin-specific protease (USPs).

Dub-in-2, with an IC50 value of 0.28 for USP8, is an effective deubiquitinase inhibitor.

DUB-IN-3 is a potent deubiquitinase (USP) enzyme inhibitor with an IC50 of 0.56 μM for USP8.

PR-619 (2,6-Diamino-3,5-dithiocyanopyridine) is a DUB inhibitor that inhibits USP2/4/5/7/8 (EC50=7.2/3.93/8.61/6.86/4.9 μM). PR-619 induces endoplasmic reticulum stress and activates autophagy.

USP28-IN-4 is a potent USP28 inhibitor with an IC50 value of 0.04 μM against USP28. USP28-IN-4 exhibits anticancer activity and inhibits USP2, USP7, USP8, USP9x, UCHL3 and UCHL5. USP28-IN-4 is cytotoxic to human colorectal and lung squamous carcinoma cells and dose-dependently downregulates c-Myc cellular levels through the ubiquitin-proteasome system. -proteasome system to dose-dependently downregulate cellular levels of c-Myc.

Cysteine protease inhibitor 2 is a cysteine protease inhibitor. Cysteine protease inhibitor 2 inhibited DCT116 and PC3 cells with GI50 values of 6.5 μM and 4.4 μM, respectively.

Huib32 is a potent small-molecule USP32 inhibitor with an IC₅₀ of 21.2 nM and high selectivity over closely related deubiquitinases (DUBs) including USP8/10/16, UCHL1, and OTUB2. It inhibits USP32 via reversible covalent binding to the active site Cys743, thereby increasing substrate ubiquitination, altering endosomal morphology, and producing biological phenotypes similar to USP32 knockout. It can be used in research on breast cancer, ovarian cancer, lung cancer, Alzheimer’s disease, Parkinson’s disease, and other diseases.

DC-U4106 is a USP8-targeted inhibitor (Kd: 4.7 μM, IC50: 1.2 μM). DC-U4106 can use the ubiquitination pathway to promote the degradation of Erα. DC-U4106 inhibits the growth of tumor cells with low toxicity and can be used to study breast cancer.

USP28-IN-2 is a selective USP28 inhibitor (IC50 = 0.3 μM), demonstrating high specificity compared to USP2, USP7, USP8, USP9x, UCHL3, and UCHL5. This compound exhibits cytotoxic effects on cancer cells and induces the degradation of c-Myc via the ubiquitin-proteasome pathway. Additionally, USP28-IN-2 reduces ankyrin-1/2 levels in vitro and potentiates the responsiveness of colorectal cancer cells to Regorafenib [1].

LLK203 is a potent dual-target inhibitor of USP2/USP8 with IC50 values of 0.89 μM and 0.52 μM, respectively. It promotes ERα degradation and induces apoptosis in breast cancer MCF-7 cells, demonstrating antitumor activity in the 4T1 tumor mice model [1].