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).

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.

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.

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.

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

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).

USP7/USP47 inhibitor (USP7/47 inhibitor-1) is a selective ubiquitin-specific protease 7/47 (USP7/USP47) inhibitor, with EC50s of 0.42 μM and 1.0 μM, respectively.

GNE-6776 is a selective USP7 inhibitor.

GNE-6640 is a non-covalent inhibitor targeting ubiquitin specific peptidase 7 (USP7), exhibiting IC50 values of 0.75 μM for full-length USP7, 0.43 μM for the USP7 catalytic domain, 20.3 μM for full-length USP43, and 0.23 μM for Ub-MDM2, respectively.

KSQ-4279 (USP1-IN-1) is an inhibitor of USP1 and PARP, exhibiting anticancer activity. It is utilized in the study of non-small cell lung cancer, osteosarcoma, ovarian, breast, glioblastoma, bladder, uterine, and pancreatic cancers.

IU1(IC50=4.7 μ M), a reversible, specific human USP14 proteasome inhibitor, can penetrate the cell.

Degrasyn (WP1130) (WP1130), a specific deubiquitinase (DUB: USP5, UCH-L1, USP9x, USP14, and UCH37) inhibitor, also inhibits Bcr/Abl, which is a JAK2 transducer (without affecting 20S proteasome) and activator of transcription (STAT).