dubs

MF-094 is a potent and selective inhibitor of USP30 (IC50 of 120 nM).

USP25/28 inhibitor AZ1 (AZ1) (AZ1) is an inhibitor of ubiquitin specific protease (USP) 25/28

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.

P005091 (P5091) is a selective and potent inhibitor of ubiquitin-specific protease 7 (USP7) with EC50 of 4.2 μM.

LDN-57444 is a reversible, competitive proteasome Uch-L1 inhibitor(IC50=0.88 μM) .

PR-619 (2,6-Diamino-3,5-dithiocyanopyridine) is a non-selective, reversible inhibitor of the deubiquitinylating enzymes (DUBs).

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).

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

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

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

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.

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

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

N-Ethylmaleimide (NEM) is a sulfhydryl reagent that is widely used in experimental biochemical studies.

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.

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.

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

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.

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

RA-9 is a potent and selective proteasome-associated inhibitor of deubiquitinating enzymes (DUBs), with favorable toxicity profile and anticancer activity. RA-9 selectively induces 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).

SJB2-043 is an inhibitor of USP1-UAF1 ( IC50 : 544 nM).

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.

Proteasome-IN-3 is an inhibitor of proteasome-associated DUBs.

BC-1471 is a STAM-binding protein (STAMBP) deubiquitinase inhibitor. BC-1471 inhibits inflammasome activity of NALP7 (NACHT, LRR and PYD domains-containing protein 7) [1].

IU1-248 is a derivative of IU1. IU1-248 is a potent and selective USP14 inhibitor with an IC50 of 0.83 μM[1].

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

C527 is a is a pan DUB enzyme inhibitor. Which has a high potency for the USP1/UAF1 complex (IC50=0.88 μM).

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

VLX1570 is a competitive inhibitor of proteasome DUB activity with IC50 ranging from 4.2 uM to 8.6 uM. It has potent inhibition for USP14.

DUB-IN-3 is a potent deubiquitinase (USP) enzyme inhibitor and the IC50 for USP8 is 0.56 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.

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.

TCID (UCH-L3 Inhibitor)(IC50=0.6 μM) is a DUB inhibitor of ubiquitin C-terminal hydrolase L3. It has the 125-fold selectivity to L1.

DUB-IN-7 (compound 43), a deubiquitinating enzyme (DUB) inhibitor, has utility in researching diseases driven by aberrant JAK2 activity, including leukemia [1].

XL177A is a selective irreversible USP7 inhibitor(IC50 : 0.34 nM). XL177A elicits cancer cell killing through a p53-dependent mechanism.

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.

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).

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).

XL-188 is a highly potent and selective inhibitor of USP7. XL188 inhibited USP7 catalytic domain and full-length enzyme with IC50 values of 193 and 90 nM, respectively. XL188 Promotes USP7-Dependent Loss of HDM2 and Increase of p53 and p21. XL188 represents one of only a small set of mammalian DUB inhibitors with low nanomolar potency and a high degree of selectivity relative to other DUBs

GNE-6776 is a selective USP7 inhibitor.