USP/UBP Selective Inhibitors

Catalog No. Product Name Information Selective / Pan IC50 / Ki
S8967 XL177A

XL177A is a potent, selective and irreversible inhibitor of Ubiquitin specific peptidase 7 (USP7) with IC50 of 0.34 nM.

Selective USP7, IC50: 0.34 nM
S6878 GSK2643943A

GSK2643943A is an inhibitor of deubiquitylating enzyme (DUB) with IC50 of 160 nM for USP20/Ub-Rho.

Selective USP20/Ub-Rho, IC50: 160 nM
S2913 BAY 11-7082

BAY 11-7082 (BAY 11-7821) is a NF-κB inhibitor, inhibits TNFα-induced IκBα phosphorylation with IC50 of 10 μM in tumor cells. BAY 11-7082 inhibits ubiquitin-specific protease USP7 and USP21 with IC50 of 0.19 μM and 0.96 μM, respectively. BAY 11-7082 induces apoptosis and S phase arrest in gastric cancer cells.

Selective USP6, IC50: 1.7 μM; USP21, IC50: 0.96 μM; USP7, IC50: 0.19 μM
S7888 Spautin-1

Spautin-1 is a potent and specific autophagy inhibitor, and inhibits the deubiquitinating activity of USP10 and USP13 with IC50 of ∼0.6-0.7 μM. Spautin-1 enhances apoptosis.

Selective USP10, IC50: 0.5779 μM; USP13, IC50: 0.6916 μM
S6933 GEN-6776

GNE-6776 is a potent, non-covalent, selective and orally bioavailable inhibitor of USP7 with IC50 of 1.34 μM and 0.61 μM for full length USP7 and USP7 catalytic domain, respectively.

Selective USP7 catalytic domain, IC50: 0.61 μM; full length USP7, IC50: 1.34 μM
S8904 USP25/28 inhibitor AZ1

AZ1 is a potent and noncompetitive dual Inhibitors of the ubiquitin-specific protease (USP) 25/28 with IC50s of 0.62 μM and 0.7 μM in Ub-RH110 assay,respectively.

Selective USP28, IC50: 0.7 μM; USP25, IC50: 0.62 μM
S6748 ML364

ML364 is a small molecule inhibitor of the deubiquitinase USP2 with an IC50 of 1.1 μM in a biochemical assay using an internally quenched fluorescent di-ubiquitin substrate.

Selective USP8, IC50: 0.95 μM; USP2, IC50: 1.1 μM
S7132 P5091 (P005091)

P5091(P005091) is a selective and potent inhibitor of ubiquitin-specific protease 7 (USP7) with EC50 of 4.2 μM and the closely related USP47.

Selective USP47, IC50: 4.3 μM; USP7, EC50: 4.2 μM
S7134 IU1

IU1 is a cell-permeable, reversible and selective proteasome inhibitor of human USP14 with IC50 of 4.7 μ M, 25-fold selective to IsoT. IU1 induces autophagy.

Selective USP14, IC50: 4.7 μM
S7133 P22077

P22077 is an inhibitor of ubiquitin-specific protease USP7 with EC50 of 8.6 μM, also inhibits the closely related USP47.

Selective USP47, EC50: 8.74 μM; USP7, IC50: 8.6 μM
S4922 NSC 632839

NSC 632839 is not only a DUB inhibitor, but also a deSUMOylase inhibitor, it inhibits USP2, USP7, and SENP2 with EC50 of 45 μM, 37 μM, and 9.8 μM, respectively.

Selective USP7, EC50: 37 μM; USP2, EC50: 45 μM
S6877 EOAI3402143

EOAI3402143 is a dose-dependent inhibitor of Usp9x, Usp24 and Usp5 that increases tumor cell apoptosis, and fully blocks or regresses myeloma tumors in mice.

Selective
S7130 PR-619

PR-619 is a non-selective, reversible inhibitor of the deubiquitinylating enzymes (DUBs) with EC50 of 1-20 μM in a cell-free assay. PR-619 activates autophagy.

Pan USP47, EC50: 8.87 μM; USP28, EC50: 6.24 μM; USP20, EC50: 5.10 μM; USP15, EC50: 8.23 μM; USP8, EC50: 4.90 μM; USP7, EC50: 6.86 μM; USP5, EC50: 8.61 μM; USP4, EC50: 3.93 μM; USP2 core, EC50: 7.20 μM
S4920 b-AP15

b-AP15 (NSC687852) is a deubiquitinases inhibitor for 19S proteasomes activity of Ub-AMC cleavage with IC50 of 2.1 μM.

Pan