(R)-USP-IN-4 is a highly potent, selective, allosteric USP7 inhibitor with IC50 of 6 nM in FP assays.

A novel potent, specific, covalent USP7 inhibitor with Kd of 7.8 uM (USP7 catalytic domain).

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

FT-671 is a novel potent, specific, non-covalent USP7 inhibitor with Kd of 65 nM (USP7 catalytic domain).

GNE-6640 is a potent, selective USP7 inhibitor with IC50 of 0.75 uM; dislpalys selectivity over USP47 and USP5 (IC50>200 uM).

GNE-6776 is a novel potent, specific, non-covalent, orally bioavailable USP7 inhibitor with IC50 of 1.34 uM .

GSK2643943A is a potent USP20 inhibitor with IC50 = 160 nM.

HBX 19818 is a selective USP7 inhibitor with IC50 of 28.1 uM .

LDN-57444 is a reversible, competitive proteasome inhibitor for Uch-L1 with IC50 of 0.88 μM, 28-fold selectivity over isoform Uch-L3.

MF-094 (MF094) is a potent, highly selective inhibitor of ubiquitin specific protease 30 (USP30) with IC50 of 0.12 uM, demonstrates <30% inhibitory activity for a panel of 22 USPs assays at 10 uM.

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

ML364 is an USP2 inhibitor.xtracted from patent WO 2016134026 A1, compound example 10G.

NSC632839 is a nonselective isopeptidase inhibitor, which inhibits USP2, USP7, and SENP2 with EC50s of 45±4 μM, 37±1 μM, and 9.8±1.8 μM, respectively.

Spautin 1 is an inhibitor of autophagy; inhibits USP10 and USP13 activity (IC50 values are 0.6 and 0.7 μM respectively) and promotes degradation of Vps34 (class III PI 3-kinase) complexes.

Ubiquitin Isopeptidase Inhibitor I, G5 (NSC 144303) is an apoptosome-independent caspase and apoptosis activator with IC50 values of 1.76 and 1.6 μM in E1A and E1A/C9DN cells, respectively.

USP25 and 28 inhibitor AZ-2 is a potent, selective, dual USP25/28 inhibitor with IC50 of 0.9/0.9 uM, respectively.

USP7/USP47 inhibitor is a potent and dual inhibitor of USP7/USP47 with IC50s of 0.42 uM(USP7) and 1.0 uM(USP47).

VLX1570 is a competitive inhibitor of proteasome DUB activity, with an IC50 of ~10 μM in vitro.

XL188 (XL-188) is a potent, selective, non-covalent active-site inhibitor of USP7 with IC50 of 90 nM and 193 nM for USP7 full length enzyme and catalytic domain, respectively.

USP25 and 28 inhibitor AZ-1 (AZ1) is a potent, selective, dual USP25/28 inhibitor with IC50 of 0.7/0.6 uM, respectively; shows a high degree of selectivity over other deubiquitinases (USP4,7 etc.); demonstrates target engagement against both USP25 and USP28 in cells, elicits modulation of both the total levels and the half-life of the c-Myc oncoprotein in cells, and also induces apoptosis and inhibits cell viability in a range of cancer cell lines.

USP7-IN-5 is a potent ubiquitin specific protease 7 (USP7) inhibitor extracted from patent WO2017212012A1, example 40, has an IC50 of 49.9 nM.

USP7-IN-6 is a potent ubiquitin specific protease 7 (USP7) inhibitor, extracted from patent WO2017212010A1, example 25, has an IC50 of 6.8 nM.

6RK73 is a covalent irreversible and specific UCHL1 inhibitor with an IC50 of 0.23 µM. 6RK73 shows almost no inhibition of UCHL3 (IC50=236 µM). 6RK73 specifically inhibit UCHL1 activity in breast cancer.

A novel potent ubiquitin-specific protease USP1 inhibitor with IC50 of 78.1 nM, 5 times more potent than SJB2-043 in promoting ID1 degradation and cytoxicity in K562 cells.

BC-1471 is a selective, small-molecule deubiquitinase STAM-binding protein (STAMBP) inhibitor (IC50=0.33 uM) that interrupts STAMBP-Ub-NALP7 interaction.

P 217564 is a potent, selective, irreversible second generation inhibitor of USP7 with IC50 of 0.48 uM, with similar potency against USP47 and no significant activity aginst other DUBs.

LCAHA (LCA hydroxyamide) is a deubiquitinase USP2a inhibitor with IC50s of 9.7 μM and 3.7μM in Ub-AMC Assay and Di-Ub Assay, respectively. LCAHA destabilizes Cyclin D1 and induces G0/G1 arrest by inhibiting deubiquitinase USP2a.

USP30 inhibitor 11 is a selective and potent ubiquitin specific peptidase 30 (USP30) inhibitor with an IC50 of 0.01 µΜ, the example 83 extracted from patent WO2017009650A1. USP30 inhibitor 11 is used for the study of cancer and conditions involving mitochondrial dysfunction.

USP30 inhibitor 18 is a selective USP30 inhibitor with an IC50 of 0.02 μM. USP30 inhibitor 18 increases protein ubiquitination and accelerates mitophagy.

Vialinin A (Terrestrin A) is a p-terphenyl compound with antioxidant properties. Vialinin A is a potent inhibitor of TNF-α, USP4, USP5, and sentrin/SUMO-specific protease 1 (SENP1). Vialinin A (Terrestrin A) can be used for autoimmune diseases and cancer research.

FT3967385 is a novel USP30 inhibitor that recapitulates genetic loss of USP30 and sets the trigger for PINK1-PARKIN amplification of mitochondrial ubiquitylation.

USP5-IN-1 (compound 64), a potent deubiquitinase USP5 inhibitor, binds to the USP5 ZnF-UBD with a KD of 2.8 μM. USP5-IN-1 is selective over nine proteins containing structurally similar ZnF-UBD domains. USP5-IN-1 inhibits the USP5 catalytic cleavage of a di-ubiquitin substrate.

USP7i-1 is a potent, selective USP7 inhibitor..

EN523 (EN-523) is a small molecule covalent ligand EN523 that targets a non-catalytic allosteric cysteine C23 in the K48-ubiquitin-specific deubiquitinase OTUB1, OTUB1 recruiter component of DUBTAC NJH-2-057.Deubiquitinase-targeting chimeras (DUBTACs), heterobifunctional small molecules consisting of a deubiquitinase recruiter linked to a protein-targeting ligand, to stabilize the levels of specific proteins degraded in a ubiquitin-dependent manner.

iBAP-II (BAP1 inhibitor II) is a next-generation, specific small molecule inhibitor of BAP1 histone H2A deubiquitinase activity with IC50 of <0.1 ug/mL.iBAP-II displays higher affinity for BAP1 than the closest UCH family member, UCHL5, and other deubiquitinases, such as USP5, USP7, USP8, TNFAIP3-catalytic domain, USP2-catalytic domain, Otubain-1, and Ataxin3.Inhibition of BAP1 via iBAP-II reduces ASXL3 protein stability in small cell lung cancer cells, without significant changes to ASXL1 and ASXL2 protein levels.iBAP-II suppresses ASCL1 expression in NCI-H1963 cells, along with the mRNA levels involving a handful of known ASCL1 transcriptional targeted genes, such as GRP, DMPK, RNF183, SCN3A, MYCL, and CACNA1A.iBAP-II exhibited more potent cell viability inhibition activity on four different BAP1-WT SCLC cell lines than iBAP.iBAP-II (50 mg/kg/d) significantly delayed the disease progression in SCLC xenograft model.

IMP-1710 (IMP1710) is a potent, selective, covalent UCHL1 inhibitor with IC50 of 38 nM.IMP-1710 demonstrated exquisite selectivity in a cross-screening against 20 DUBs.IMP-1710 can profile activity of endogenous UCHL1 with excellent selectivity in cell types including endothelial cells (EA.hy926) and adenocarcinoma human alveolar basal epithelial cells (A549).IMP-1710 demonstrated >50% fibroblast–myofibroblast transition (FMT) inhibition (IC50=740 nM) in idiopathic pulmonary fibrosis (IPF), as well as αSMA inhibition.IMP-1710 is a powerful and selective probe to explore UCHL1 activity with potential application to substrate identification, mode of action studies, and cellular target profiling.

MT16-001 is a selective, covalent inhibitor of deubiquitinating enzyme UCHL1 with IC50 of 580 nM, no inhibitory effect against UCHL3 (IC50>30 uM).MT16-001 inhibits structurally unrelated DUB USP30 with similar potency.MT16-001 showed cytotoxicity in human embryonic kidney cells (HEK293) with EC50 of 730 nM, effectively engaged UCHL1 in cells with EC50 of 550 nM.MT16-001 showed excellent selectivity for UCHL1 across the UCH family: UCHL1, UCHL3, UCHL5 and BAP1.

MT16-205 (MT 16-205) is a potent, selective, covalent UCHL1 inhibitor with IC50 of 600 nM, no inhibition agianst UCHL3 (IC50>10 uM).MT16-205 inhibited both UCHL1 and the structurally unrelated DUB USP30 with similar potency.MT16-205 displayed cell proliferation cytotoxicity in human embryonic kidney cells (HEK293) with IC50 of 350 nM, MT16-205 effectively engaged UCHL1 in cells with IC50 of 830 nM.

NJH-2-075 is an alkyne-functionalized probe of EN523, retains binding to OTUB1 in vitro.

UCHL1 inhibitor 27 is a potent, selective, covalent UCHL1 inhibitor with IC50 of 90 nM.UCHL1 inhibitor 27 demonstrated exquisite selectivity in a cross-screening against 20 DUBs.UCHL1 inhibitor 27 demonstrated >50% fibroblast–myofibroblast transition (FMT) inhibition (IC50=100 nM) in idiopathic pulmonary fibrosis (IPF), as well as αSMA inhibition.UCHL1 inhibitor 27 is a powerful and selective probe to explore UCHL1 activity with potential application to substrate identification, mode of action studies, and cellular target profiling.

USP inhibitor 1 is an irreversible USP inhibitor with submicromolar IC50 of USP4 and its phylogenetic relative USP11, also functionally inhibits USP33, leading to CP110 instability and synergy with ATR inhibition in U2OS cells.

USP inhibitor 2 is a broad DUB inhibitor with IC50 of 0.04 and 0.21 uM for USP4 and USP11, also inhibits USP10/16/15/19 with submicromolar potency, forms a covalent adduct with USP11. USP inhibitor 2 does not inhibit USP5 (IC50>100 uM).

USP10 inhibitor Wu-5 (Wu-5) is a novel small molecule USP10 inhibitor inducing the degradation of FLT3-mutated protein, directly interacts and inactivates USP10, the deubiquitinase for FLT3-ITD in vitro (IC50=8.3 uM) and in FLT3-ITD-positive AML cells.Wu-5 selectively inhibited the viability of FLT3 inhibitor-sensitive (MV4-11, Molm13) and -resistant (MV4-11R) FLT3-ITD-positive AML cells with IC50 of 3.794, 5.056, and 8.386 uM, respectively.Wu-5 (1-10 μM) dose-dependently induced apoptosis of MV4-11, Molm13, and MV4-11R cells through the proteasome-mediated degradation of FLT3-ITD.Combined treatment of Wu-5 and crenolanib produced synergistic cell death in FLT3-ITD-positive cells via the reduction of both FLT3 and AMPKα proteins.

USP30 inhibitor Q14 peptide is a peptide derived from the transmembrane (TM) domain of USP30 that can target mitochondrial-anchored USP30 directly and increase mitophagy.

USP30Inh-1 is a potent, selective small molecule USP30 inhibitor with IC50 of 15-30 nM (inhibition of USP30-mediated cleavage of Ub-Rho110).USP30Inh-1 is anticipated to form a covalent linkage with the catalytic cysteine within the USP30 active site.USP30Inh-1 demonstrated good selectivity against >40 known DUB enzymes at 1 uM. USP30Inh-1 (1-10 uM) enhances mitoKeima signal in SHSY5Y cell, increases p-Ser65-Ub in dopaminergic neurones and astrocytes, as well as in Parkin heterozygote fibroblasts.

USP5 inhibitor 64 is a selective chemical probe (inhibitor) against USP5 deubiquitinase, binds to the USP5 ZnF-UBD (zinc-finger ubiquitin binding domain) with KD of 2.8 uM.USP5 inhibitor 64 is selective over nine proteins containing structurally similar ZnF-UBD domains.USP5 inhibitor 64 inhibits the USP5 catalytic cleavage of a di-ubiquitin substrate in an in vitro assay.

USP7-866 is a novel potent selective inhibitor of USP7 with IC50 of 0.18 nM; USP7-866 inhibited the growth of p53-mutant small cell lung cancer cell line H526 at a CC50 of 42 nM.

FT709 is a potent and selective USP9X inhibitor, an IC50 of 82 nM. USP9X has been linked with centrosome function, chromosome alignment during mitosis, EGF receptor degradation, chemo-sensitization, and circadian rhythms.

Iu1-248, a derivative of IU1, is a potent and selective ubiquitin specific peptidase 14 (USP14) inhibitor with an IC50 of 0.83 μM.

8RK64 is a covalent UCHL1 inhibitor (IC50: 0.32 μM).

Usp22i-S02(USP22-IN-1, compound S02) is a potent inhibitor of ubiquitin specific peptidase 22 (USP22). It showed anticancer activity by suppressing Foxp3 expression in T-regulatory cells.

BAY-728 (NAY728) is a less potent enantiomer and negative control compound of BAY-805.

BK50118-C is a potent small molecule inhibitor of ubiquitin-specific protease-13 (USP13) with IC50 of 0.42 nM.

BML-260 (BML260) is a potent inhibitor of dual-specific phosphatase JSP-1 (JNK Stimulatory Phosphatase-1, DUSP22) and stimulator of uncoupling protein 1 (UCP-1) expression in adipocytes.

C598-0556 is a selective, small molecule inhibitor of USP10, inhibits USP10 comparably to HBX19818 (IC50=10 uM), with no inhibition against USP7 (IC50>100 uM).

C673-0105 is a selective, small molecule inhibitor of USP10, inhibits USP10 comparably to HBX19818 (IC50=10 uM), with no inhibition against USP7 (IC50>100 uM.

CAS-12290-201 is a potent and selective inhibitor of deubiquitinating enzyme (DUB) VCPIP1 with IC50 of 70 nM, covalently and specificly targets the catalytic cysteine of VCPIP1 with little to no activity toward other cellular DUBs.

DC-U4106 is a potent, selective small molecule inhibitor of Ubiquitin-specific protease 8 (USP8) with binding KD value of 4.7 uM, DC-U4106 is selective over USP2 and USP7.

FT206 (FT-206, FT3951206, CRT0511973) is a potent, selectivel inhibitor of USP28 with a remarkable USP28/25 selectivity.

FT385 (FT3967385) is a potent, selective USP30 inhibitor with biochemical IC50 of 1.5 nM.

GK13S is a highly potent, specific and covalent inhibitor of deubiquitinase UCHL1 with IC50 of 87 nM, displays exquisite specificity for UCHL1 over the other UCH family members (IC50>10 uM).

HY041004 is the first small molecule inhibitor of deubiquitinase Josephin Domain-containing protein 2 (JOSD2) with IC50 of 0.26 uM for JOSD2 catalytic activity inhibition.

I-138 (I 138) is a potent, specific small molecule USP1-UAF1 inhibitor with IC50 of 4.1 nM, binds to USP1-UAF1 at an allosteric pocket synergistically with ubiquitin.

IMP-2373 is a highly targeted cyanopyrrolidine (CNPy) probe for pan-DUB to monitor DUB activity in physiologically relevant live cells.

IU1-206 is a IU1 derivative with more potent activity against USP14, 10-fold more potent than IU1 and is comparable to the IU1-47.

IU2-6 is a small molecule USP14 inhibitor, shows 74% inhibition at 8 uM.

LN5P45 is a selective, covalent, irreversible inhibitor of ubiquitin thioesterase OTUB2 with IC50 of 2.3 uM, strongly induces monoubiquitination of OTUB2 on Lys31.

MS102 is a small molecule, orally available USP2 inhibitor with IC50 of 5.46 uM, induces transient degradation of ACE2 protein and inhibits ACE2-dependent coronavirus infection.

MTX115325 is a potent, selective, brain-penetrant USP30 inhibitor with IC50 of 12 nM in biochemical fluorescence polarization assays.

NCI677397 is a specific small molecule inhibitor of USP24, inhibits chemotherapy-induced drug resistance in vitro and in vivo.

OTUDin3 (OTUD3 inhibitor) is a specific, small molecule inhibitor of deubiquitylase OTUD3, binds to OTUD3 (KD=0.32 uM) and inhibits the deubiquitinating activity of OTUD3 by interfering with Ub binding to OTUD3.

SB1-F-70 is a potent, selective inhibitor of the deubiquitinase (DUB) JOSD1/USP30/UCHL1 with IC50 of 324/400/400 nM, respectively.

TG2-179-1 is a potent, selective and covalently inhibitor of deubiquitinase (DUB) BRCA1-associated protein-1 (BAP1), covalently binds to the active site of BAP1 (Cys91), exhibits potent cytotoxic activity against colon cancer cells.

USP7-797 is a novel potent selective inhibitor of USP7 with IC50 of 0.44 nM.

XL-9872-106C (XL-106C) is a potent, selective inhibitor of the deubiquitinase (DUB) JOSD1/USP30/UCHL1 with IC50 of 134/390/166 nM, respectively.

YCH2823 is a potent, selective USP7 inhibitor with IC50 of 49.6 nM, ITC Kd of 117 nM.