usp2

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.

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.

6-Thioguanine (2-Amino-6-purinethiol) is an antineoplastic compound which also has antimetabolite action. The drug is used in the therapy of acute leukemia.

P 22077 (P22077) is an inhibitor of ubiquitin-specific protease USP7 with EC50 of 8.6 μM. It also inhibits the closely related USP47.

ML364 is an inhibitor of ubiquitin specific peptidase 2 (USP2) and can be used for the research of breast cancer.

STD1T is a selective and potent inhibitor of the deubiquitinase USP2a with potential anticancer activity that reduces cell cycle protein D1 protein levels in HCT116 colon and MCF-7 breast cancer cells.

NSC-632839 (Ubiquitin Isopeptidase Inhibitor II) is a nonselective isopeptidase inhibitor, which inhibits USP2 (EC50: 45±4 μM), USP7 (EC50: 37±1 μM), and SENP2 (EC50: 9.8±1.8 μM).

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].

USP25/28-IN-AZ2 is a novel potent, selective, dual usp25/28 inhibitor

USP22-IN-1 is a ubiquitin-specific peptidase 22 (USP22) inhibitor that can be used to treat proliferative diseases or cancer.

USP25/28 inhibitor AZ1 is a selective, orally active and non-competitive dual ubiquitin-specific protease USP25/28 inhibitor with IC50 of 0.7 μM and 0.6 μM, respectively, and exhibits anti-inflammatory and anti-tumor effects.

BAY 11-7082 (BAY 11-7821) is an NF-κB inhibitor that suppresses TNFα-induced IκBα phosphorylation (IC50=10 μM) and also inhibits the ubiquitin-specific proteases USP7 and USP21 (IC50=0.19/0.96 μM).

Lithocholic acid (3α-Hydroxy-5β-cholanic acid) is a toxic secondary bile acid, They were FXR antagonists (IC50=0.7, 1.4 μM), EphA2 antagonists (IC50=48, 66 μM) and EphB4 antagonists (IC50=141 μM). Lithocholic acid can promote intrahepatic cholestasis and promote tumorigenesis. Lithocholic acid is a cleanser that dissolves fat for absorption and is itself absorbed.

F1063-0967 is a Dual-specificity phosphatase 26 (DUSP26) inhibitor with an IC50 of 11.62 μM.

EOAI3402143 inhibits Usp9x and Usp24 activity, increases tumor cell apoptosis. EOAI3402143 phenocopies the FAS induction and apoptotic sensitization of Usp5 knockdown and fully blocks melanoma tumor growth.

GSK2643943A is a deubiquitylating enzyme (DUB) inhibitor, with an IC 50 of 160 nM for USP20/Ub-Rho. GSK2643943A has anti-tumor efficacy.

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.

XH161-180 is an effective and orally active inhibitor of ubiquitin carboxyl-terminal hydrolase 2 (USP2). It reduces the protein levels of cyclin D and ACE2, exhibiting antiproliferative activity. XH161-180 also has potential for research in cancers and viral infections that depend on ACE2.

MS1172 (XH161-172; Example 54) is an orally active inhibitor of USP2 and plays a crucial role in the treatment of cancer and viral infections.

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].