FT827 is a selective and covalent ubiquitin-specific protease 7 (USP7) inhibitor with an IC50 of 52 nM.
STD1T (USP2a inhibitor STD1T) is a hit-to-lead, small-molecule inhibitor of USP2a with IC50 of 3.3 uM in Ub-AMC assays, displays no activity against USP7 at 10 uM.
EOAI3402143 is a deubiquitinase (DUB) inhibitor, which inhibits dose-dependently inhibits Usp9x/Usp24 and Usp5.
LDN-57444 is a reversible, competitive and site-directed inhibitor of ubiquitin C-terminal hydrolase L1 (UCH-L1), with an IC50 of 0.88 μM and a Ki of 0.40 μM; LDN-57444 also suppresses UCH-L3 activity, with an IC50 of 25 μM.
FT671 is a potent and selective USP7 inhibitor with an IC50 of 52 nM and binds to the USP7 catalytic domain with a Kd of 65 nM.
USP7-IN-12 (compound 1) is a potent and orally active Usp7 inhibitor with an IC50 value of 3.67 nM. USP7-IN-12 shows antiproliferative activity[1].
HBX 19818 is a specific inhibitor of ubiquitin-specific protease 7 (USP7), with an IC50 of 28.1 μM.
LDN 91946 is a selective, uncompetitive ubiquitin C-terminal hydrolase-L1 (UCH-L1) inhibitor with Ki of 2.8 uM, exhibits no activity against other cysteine hydrolase (UCH-L3, TGase 2, papain and caspase-3).
6-Thioguanine is an anti-leukemia and immunosuppressant agent, acts as an inhibitor of SARS and MERS coronavirus papain-like proteases (PLpros) and also potently inhibits USP2 activity, with IC50s of 25 μM and 40 μM for Plpros and recombinant human USP2, respectively.
USP1-IN-4 (compound 10) is an effective USP1 inhibitor with an IC50 value of 2.44 nM. USP1-IN-4 has anticancer activity and synergistic activity with various anticancer drugs[1].
USP1-IN-6 (compound 11) is a USP1 inhibitor (IC50<50 nM). USP1-IN-5 also inhibits MDA-MB-436 cells with IC50 <50 nM[1].
STAMBP-IN-1 is a small-molecule inhibitor of STAMBP deubiquitinase, and interrupts STAMBP-Ub-NALP7 interaction. STAMBP-IN-1 decreases protein level of its inflammasome substrate NALP7 and suppresses IL-1b release after Toll-like receptor (TLR) agonism. STAMBP-IN-1 inhibits the activity of STAMBP to cleave recombinant di-Ub with an IC50 value of 0.33 mM[1].
IU1-47 is a potent USP14 inhibitor with an IC50 of 0.6 μM. IU1-47 induces tau elimination in cultured neurons[1].
USP8-IN-2 (Compd U52) is a deubiquitinase USP8 inhibitor with an IC50 value of 6.0 μM. USP8-IN-2 also inhibits the proliferation of H1957 cells with an GI50 value of 24.93 μM, respectively[1].
b-AP15 is a specific inhibitor of the deubiquitinating enzymes UCHL5 and Usp14.
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[1].
GNE-6640 is a selective and non-covalent inhibitor of ubiquitin epecific peptidase 7 (USP7), with IC50 values of 0.75 μM, 0.43 μM, 20.3 μM and 0.23 μM for full length USP7, USP7 catalytic domain, full length USP43 and Ub-MDM2, respectively.
USP7-IN-10 (compound 1) is a potent ubiquitin-specific protease 7 (USP7) inhibitor, with an IC50 of 13.39 nM[1].
USP8-IN-3 (Compd U51) is a deubiquitinase USP8 inhibitor with an IC50 value of 4.0 μM. USP8-IN-3 also inhibits the proliferation of GH3 and H1957 cells with GI50s of 37.03 μM and 6.01 μM, respectively[1].
BAY 11-7082 is a NF-κB inhibitor which decreases NF-κB by inhibiting TNF-α-induced phosphorylation of IκB-α. BAY 11-7082 inhibits ubiquitin-specific protease USP7 and USP21 with IC50s of 0.19 μM and 0.96 μM, respectively.
USP7-IN-3 (Compound 5) is a potent and selective allosteric ubiquitin-specific protease 7 (USP7) inhibitor[1].
PR-619 is a broad-range DUB inhibitor with EC50 of 3.93, 4.9, 6.86, 7.2, and 8.61 μM for USP4, USP8, USP7, USP2, and USP5, respectively.
ML364 is an inhibitor of ubiquitin specific peptidase 2 (USP2), and can be used for the research of breast cancer, extracted from patent WO 2016134026 A1, compound Figure 10G.
IU1 is a special Usp14 inhibitor with IC50 of 4-5 μM.
USP15-IN-1 is a potent USP15 inhibitor with an IC50 value of 3.76 μM. USP15-IN-1 can be used for researching anticancer[1].
FT206 is an inhibitor of carboxamides as ubiquitin-specific protrase extracted from patent WO 2020033707 A1, example 11-1[1].
USP7-IN-11 is a potent ubiquitin-specific protease 7 (USP7) (Deubiquitinase) inhibitor with an IC50 of 0.37 nM. USP7-IN-11 has anticancer effects (WO2022048498A1; Example 187)[1].
SJB2-043 is an inhibitor of the native USP1/UAF1 complex with IC50 of 544 nM.
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[1].
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[1].