deubiquitinase

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).

Vialinin A (Terrestrin A), a p-terphenyl compound, exhibits antioxidant properties and acts as a potent inhibitor of TNF-α, USP4, USP5, and sentrin/SUMO-specific protease 1 (SENP1). Its efficacy in autoimmune diseases and cancer research is noteworthy, highlighting its potential therapeutic applications.

USP30 inhibitor 18 is a selective USP30 inhibitor with an IC50 of 0.02 μM. USP30 inhibitor 18 increases protein ubiquitination and accelerates mitophagy[1]. [1]. Arthur F Kluge, et al. Novel highly selective inhibitors of ubiquitin specific protease 30 (USP30) accelerate mitophagy. Bioorg Med Chem Lett. 2018 Aug 15;28(15):2655-2659.

N-Ethylmaleimide (NEM) is a reagent for alkylation of free sulfhydryl groups, a cysteine protease inhibitor used in experimental biochemistry. N-Ethylmaleimide is also a deubiquitinating enzyme inhibitor that specifically inhibits phosphate transport in mitochondria.

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.

RA-9 is a potent and selective proteasome-associated inhibitor of deubiquitinating enzymes (DUBs) with a favorable toxicity profile and anticancer activity, particularly effective in inducing apoptosis in ovarian cancer cell lines.

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.

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.

GRL0617 is a selective and competitive noncovalent inhibitor of SARS-CoVPLpro and deubiquitinase (IC50: 0.6 μM, Ki: 0.49 μM).

MF-094 is a selective USP30 inhibitor with IC50 of 0.12 μM. MF-094 can increase protein ubiquitination and accelerate mitophagy.

USP7-IN-1 is a selective and reversible inhibitor of ubiquitin-specific protease 7 (USP7) with an IC50 of 77 μM.

C527 is a potent pan DUB enzyme inhibitor with a high affinity for the USP1/UAF1 complex (IC50=0.88 μM).

HBX 19818 is a specific ubiquitin-specific protease 7 (USP7) inhibitor (IC50: 28.1 μM).

IU1-47 is an effective and specific USP14 inhibitor (IC50: 0.6 μM). IU1-47 causes tau elimination in cultured neurons. IU1-47 inhibits IsoT/USP5 (IC50: 20 μM).

LDN-91946 is an effective and selective inhibitor of ubiquitin C-terminal hydrolase-L1 (UCH-L1) (Ki = 2.8 μM).

ML323 is a reversible and effective USP1-UAF1 inhibitor in a Ub-Rho assay (IC50: 76 nM) and in orthogonal gel-based assays using K63-linked diubiquitin (di-Ub) (IC50: 174 nM 820 nM)and monoubiquitinated PCNA (Ub-PCNA) (IC50: 820 nM) as substrates, respectively.

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.

LDN-57444 is a reversible, competitive inhibitor of the proteasome Uch-L1 with an IC50 of 0.88 μM.

B-AP15 (NSC-687852)(NSC-687852) is a selective inhibitor of the deubiquitinating enzymes Usp14 and UCHL5 of the 26S proteasome. It blocks the deubiquitinating activity of the 26S proteasome.

HBX 41108 (HBX-41108) is a non-competitive, reversible inhibitor of USP7 with an IC50 of 424nM. HBX 41108 inhibited deubiquitination of p53 mediated by USP7 in a dose-dependent manner with an IC50 of 0.8μM.

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.