DUB

Isoform-selective Products

Signaling Pathway

DUB Signaling Pathway

DUB Products

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  • DUB Inhibitors (33)
  • New DUB Products
Catalog No. Product Name Information Product Use Citations Product Validations
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.
Nat Cancer, 2024, 10.1038/s43018-023-00712-x
Redox Biol, 2024, 70:103072
Cell Death Dis, 2024, 15(1):70
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.
Nat Commun, 2024, 15(1):1642
J Nanobiotechnology, 2023, 21(1):117
Ecotoxicol Environ Saf, 2023, 263:115197
S7132 P5091 P5091 is a selective and potent inhibitor of ubiquitin-specific protease 7 (USP7) with EC50 of 4.2 μM and the closely related USP47.
J Exp Clin Cancer Res, 2024, 43(1):28
Adv Sci (Weinh), 2023, 10(8):e2206212
Oncogene, 2023, 42(22):1843-1856
S2243 Degrasyn (WP1130) Degrasyn (WP1130) is a selective deubiquitinase (DUB: USP5, UCH-L1, USP9x, USP14, and UCH37) inhibitor and also suppresses Bcr/Abl, also a JAK2 transducer (without affecting 20S proteasome) and activator of transcription (STAT). Degrasyn (WP1130) induces apoptosis and blocks autophagy.
Clin Cancer Res, 2023, 29(2):446-457
Cancer Cell Int, 2023, 23(1):207
Biomedicines, 2023, 10.3390/biomedicines11030759
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.
J Adv Res, 2024, S2090-1232(24)00025-0
Nat Commun, 2023, 14(1):2691
Acta Neuropathol Commun, 2023, 11(1):110
S7133 P22077 P22077 is an inhibitor of ubiquitin-specific protease USP7 with EC50 of 8.6 μM, also inhibits the closely related USP47.
EMBO Rep, 2022, e54391
Front Pharmacol, 2022, 13:1021361
Front Pharmacol, 2022, 13:1021361
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.
Antioxidants (Basel), 2024, 13(1)114
Nat Commun, 2022, 13-1:5644
Cell Death Dis, 2021, 12(9):803
S4920 b-AP15 b-AP15 (NSC687852) is a deubiquitinases inhibitor for 19S proteasomes activity of Ub-AMC cleavage with IC50 of 2.1 μM.
Commun Biol, 2024, 7(1):25
Cell Death Differ, 2022, 10.1038/s41418-022-01054-4
Clin Transl Med, 2022, 12(9):e1038
S7529 ML323 ML323 displays reversible, nanomolar inhibitory activity and excellent selectivity toward USP1/UAF1 with IC50 of 76 nM.
Blood Adv, 2023, 7(13):3099-3112
PLoS One, 2023, 18(5):e0285337
J Exp Clin Cancer Res, 2021, 40(1):201
S7135 LDN-57444 LDN-57444 is a reversible, competitive proteasome inhibitor for Uch-L1 with IC50 of 0.88 μM, 28-fold selectivity over isoform Uch-L3.
Mol Cells, 2023, 46(8):476-485
Mol Cells, 2023, 46(8):476-485
Cell Biol Int, 2021, 10.1002/cbin.11662
S3692 NEM (N-Ethylmaleimide) NEM (N-Ethylmaleimide) is an organic compound that is derived from maleic acid. It is an irreversible inhibitor of all cysteine peptidases, with alkylation occurring at the active site thiol group. N-Ethylmaleimide (NEM) inactivates endogenous deubiquitinating enzymes (DUBs). N-Ethylmaleimide (NEM) specifically inhibits phosphate transport in mitochondria.
Cell Rep Med, 2023, 10.1016/j.xcrm.2023.101286
Int J Mol Sci, 2023, 25(1)423
Breast Cancer Res Treat, 2023, 200(1):151-162
S8288 VLX1570 VLX1570 is a competitive inhibitor of proteasome DUB activity, with an IC50 of ~10 μM in vitro.
Commun Biol, 2024, 7(1):25
PLoS One, 2022, 17(7):e0271245
Cancer Sci, 2021, 112(8):3302-3313
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.
Cell Rep Med, 2023, 4(4):101007
Int J Biol Sci, 2021, 17(10):2417-2429
Transl Lung Cancer Res, 2021, 10(10):3995-4011
S7140 TCID TCID is a DUB inhibitor for ubiquitin C-terminal hydrolase L3 with IC50 of 0.6 μM, 125-fold selective to L1.
Nat Commun, 2022, 13(1):1700
Cell Chem Biol, 2021, S2451-9456(21)00213-0
S0515 PLpro inhibitor  PLpro inhibitor (compound 6) is a potent papain-like protease (PLpro)/deubiquitinase (DUBs) inhibitor with IC50 of 2.6 μM and EC50 of 13.1 μM that blocks SARS virus replication.
PLoS Pathog, 2023, 19(8):e1011592
bioRxiv, 2022, 2022.08.06.503039
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.
Mol Oncol, 2022, 10.1002/1878-0261.13217
Cancer Sci, 2022, 113-10:3463-3475
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.
Cell Insight, 2022, 1(4):100047
J Virol, 2020, JVI.01857-20
S0399 SJB2-043 SJB2-043 is a potent USP1 inhibitor that inhibits the activity of native USP1/UAF1 with IC50 of 544 nM.
Front Pharmacol, 2021, 12:695009
S6878 GSK2643943A GSK2643943A is an inhibitor of deubiquitylating enzyme (DUB) with IC50 of 160 nM for USP20/Ub-Rho.
Nature, 2020, 10.1038/s41586-020-2928-y
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.
E1479New I-138 I-138 is an orally active, potent reversible inhibitor of USP1-UAF1 with IC50 0f 4.1 nM. I-138 is structurally related to ML323 and induces the monoubiquitination of FANCD2 and PCNA in MDA-MB-436 cells and increases PCNA and FANCD2 monoubiquitination in HAP-1 USP1 WT cells.
S8967 XL177A XL177A is a potent, selective and irreversible inhibitor of Ubiquitin specific peptidase 7 (USP7) with IC50 of 0.34 nM.
E1098 MF-094 MF-094, a potent and selective USP30 inhibitor (IC50=0.12 μM), accelerates diabetic wound healing by inhibiting the NLRP3 inflammasome.
E0392New Dubs-IN-1 Dubs-IN-1 is an active inhibitor of ubiquitin-specific proteases (USPs), with an IC50 of 0.85 μM for USP8.
E0389 DUBs-IN-2 DUBs-IN-2 is a potent inhibitor of USP7 and USP8 deubiquitinating enzymes. 
E1330 Usp22i-S02 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.
S6845 GRL0617 GRL0617 is a potent, selective and competitive noncovalent inhibitor of severe acute respiratory syndrome (SARS-CoV) papain-like protease (PLPro)/deubiquitinase with IC50 of 0.6 μM and Ki of 0.49 μM. GRL0617 inhibits SARS-CoV viral replication in Vero E6 cells with EC50 of 15 microM and has no associated cytotoxicity.
S6883 HBX 19818 HBX19818 is a specific inhibitor of USP7 with an IC 50 of 28.1 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.
E0947 Iu1-248 Iu1-248, a derivative of IU1, is a potent and selective ubiquitin specific peptidase 14 (USP14) inhibitor with an IC50 of 0.83 μM.
S6943 IU1-47 IU1-47 is a potent and specific inhibitor of USP14 with an IC50 of 0.6 μM. IU1-47 shows ∼33-fold selectivity for USP14 over USP5 (IsoT).
S0884 RA-9 RA-9 is a cell-permeable, potent and selective inhibitor of proteasome-associated deubiquitinating enzymes (DUBs) with favorable toxicity profile and anticancer activity. RA-9 selectively induces apoptosis in ovarian cancer cell lines.
E1214New KSQ-4279 KSQ-4279 (USP1-IN-1) is an orally bioavailable selective inhibitor of the ubiquitin specific protease 1 (USP1) with anti-proliferative activity. KSQ-4279 also exhibits synergistic activity in combination with PARP inhibitors.
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.
Nat Cancer, 2024, 10.1038/s43018-023-00712-x
Redox Biol, 2024, 70:103072
Cell Death Dis, 2024, 15(1):70
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.
Nat Commun, 2024, 15(1):1642
J Nanobiotechnology, 2023, 21(1):117
Ecotoxicol Environ Saf, 2023, 263:115197
S7132 P5091 P5091 is a selective and potent inhibitor of ubiquitin-specific protease 7 (USP7) with EC50 of 4.2 μM and the closely related USP47.
J Exp Clin Cancer Res, 2024, 43(1):28
Adv Sci (Weinh), 2023, 10(8):e2206212
Oncogene, 2023, 42(22):1843-1856
S2243 Degrasyn (WP1130) Degrasyn (WP1130) is a selective deubiquitinase (DUB: USP5, UCH-L1, USP9x, USP14, and UCH37) inhibitor and also suppresses Bcr/Abl, also a JAK2 transducer (without affecting 20S proteasome) and activator of transcription (STAT). Degrasyn (WP1130) induces apoptosis and blocks autophagy.
Clin Cancer Res, 2023, 29(2):446-457
Cancer Cell Int, 2023, 23(1):207
Biomedicines, 2023, 10.3390/biomedicines11030759
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.
J Adv Res, 2024, S2090-1232(24)00025-0
Nat Commun, 2023, 14(1):2691
Acta Neuropathol Commun, 2023, 11(1):110
S7133 P22077 P22077 is an inhibitor of ubiquitin-specific protease USP7 with EC50 of 8.6 μM, also inhibits the closely related USP47.
EMBO Rep, 2022, e54391
Front Pharmacol, 2022, 13:1021361
Front Pharmacol, 2022, 13:1021361
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.
Antioxidants (Basel), 2024, 13(1)114
Nat Commun, 2022, 13-1:5644
Cell Death Dis, 2021, 12(9):803
S4920 b-AP15 b-AP15 (NSC687852) is a deubiquitinases inhibitor for 19S proteasomes activity of Ub-AMC cleavage with IC50 of 2.1 μM.
Commun Biol, 2024, 7(1):25
Cell Death Differ, 2022, 10.1038/s41418-022-01054-4
Clin Transl Med, 2022, 12(9):e1038
S7529 ML323 ML323 displays reversible, nanomolar inhibitory activity and excellent selectivity toward USP1/UAF1 with IC50 of 76 nM.
Blood Adv, 2023, 7(13):3099-3112
PLoS One, 2023, 18(5):e0285337
J Exp Clin Cancer Res, 2021, 40(1):201
S7135 LDN-57444 LDN-57444 is a reversible, competitive proteasome inhibitor for Uch-L1 with IC50 of 0.88 μM, 28-fold selectivity over isoform Uch-L3.
Mol Cells, 2023, 46(8):476-485
Mol Cells, 2023, 46(8):476-485
Cell Biol Int, 2021, 10.1002/cbin.11662
S3692 NEM (N-Ethylmaleimide) NEM (N-Ethylmaleimide) is an organic compound that is derived from maleic acid. It is an irreversible inhibitor of all cysteine peptidases, with alkylation occurring at the active site thiol group. N-Ethylmaleimide (NEM) inactivates endogenous deubiquitinating enzymes (DUBs). N-Ethylmaleimide (NEM) specifically inhibits phosphate transport in mitochondria.
Cell Rep Med, 2023, 10.1016/j.xcrm.2023.101286
Int J Mol Sci, 2023, 25(1)423
Breast Cancer Res Treat, 2023, 200(1):151-162
S8288 VLX1570 VLX1570 is a competitive inhibitor of proteasome DUB activity, with an IC50 of ~10 μM in vitro.
Commun Biol, 2024, 7(1):25
PLoS One, 2022, 17(7):e0271245
Cancer Sci, 2021, 112(8):3302-3313
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.
Cell Rep Med, 2023, 4(4):101007
Int J Biol Sci, 2021, 17(10):2417-2429
Transl Lung Cancer Res, 2021, 10(10):3995-4011
S7140 TCID TCID is a DUB inhibitor for ubiquitin C-terminal hydrolase L3 with IC50 of 0.6 μM, 125-fold selective to L1.
Nat Commun, 2022, 13(1):1700
Cell Chem Biol, 2021, S2451-9456(21)00213-0
S0515 PLpro inhibitor  PLpro inhibitor (compound 6) is a potent papain-like protease (PLpro)/deubiquitinase (DUBs) inhibitor with IC50 of 2.6 μM and EC50 of 13.1 μM that blocks SARS virus replication.
PLoS Pathog, 2023, 19(8):e1011592
bioRxiv, 2022, 2022.08.06.503039
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.
Mol Oncol, 2022, 10.1002/1878-0261.13217
Cancer Sci, 2022, 113-10:3463-3475
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.
Cell Insight, 2022, 1(4):100047
J Virol, 2020, JVI.01857-20
S0399 SJB2-043 SJB2-043 is a potent USP1 inhibitor that inhibits the activity of native USP1/UAF1 with IC50 of 544 nM.
Front Pharmacol, 2021, 12:695009
S6878 GSK2643943A GSK2643943A is an inhibitor of deubiquitylating enzyme (DUB) with IC50 of 160 nM for USP20/Ub-Rho.
Nature, 2020, 10.1038/s41586-020-2928-y
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.
E1479New I-138 I-138 is an orally active, potent reversible inhibitor of USP1-UAF1 with IC50 0f 4.1 nM. I-138 is structurally related to ML323 and induces the monoubiquitination of FANCD2 and PCNA in MDA-MB-436 cells and increases PCNA and FANCD2 monoubiquitination in HAP-1 USP1 WT cells.
S8967 XL177A XL177A is a potent, selective and irreversible inhibitor of Ubiquitin specific peptidase 7 (USP7) with IC50 of 0.34 nM.
E1098 MF-094 MF-094, a potent and selective USP30 inhibitor (IC50=0.12 μM), accelerates diabetic wound healing by inhibiting the NLRP3 inflammasome.
E0392New Dubs-IN-1 Dubs-IN-1 is an active inhibitor of ubiquitin-specific proteases (USPs), with an IC50 of 0.85 μM for USP8.
E0389 DUBs-IN-2 DUBs-IN-2 is a potent inhibitor of USP7 and USP8 deubiquitinating enzymes. 
E1330 Usp22i-S02 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.
S6845 GRL0617 GRL0617 is a potent, selective and competitive noncovalent inhibitor of severe acute respiratory syndrome (SARS-CoV) papain-like protease (PLPro)/deubiquitinase with IC50 of 0.6 μM and Ki of 0.49 μM. GRL0617 inhibits SARS-CoV viral replication in Vero E6 cells with EC50 of 15 microM and has no associated cytotoxicity.
S6883 HBX 19818 HBX19818 is a specific inhibitor of USP7 with an IC 50 of 28.1 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.
E0947 Iu1-248 Iu1-248, a derivative of IU1, is a potent and selective ubiquitin specific peptidase 14 (USP14) inhibitor with an IC50 of 0.83 μM.
S6943 IU1-47 IU1-47 is a potent and specific inhibitor of USP14 with an IC50 of 0.6 μM. IU1-47 shows ∼33-fold selectivity for USP14 over USP5 (IsoT).
S0884 RA-9 RA-9 is a cell-permeable, potent and selective inhibitor of proteasome-associated deubiquitinating enzymes (DUBs) with favorable toxicity profile and anticancer activity. RA-9 selectively induces apoptosis in ovarian cancer cell lines.
E1214New KSQ-4279 KSQ-4279 (USP1-IN-1) is an orally bioavailable selective inhibitor of the ubiquitin specific protease 1 (USP1) with anti-proliferative activity. KSQ-4279 also exhibits synergistic activity in combination with PARP inhibitors.
E1479New I-138 I-138 is an orally active, potent reversible inhibitor of USP1-UAF1 with IC50 0f 4.1 nM. I-138 is structurally related to ML323 and induces the monoubiquitination of FANCD2 and PCNA in MDA-MB-436 cells and increases PCNA and FANCD2 monoubiquitination in HAP-1 USP1 WT cells.
E0392New Dubs-IN-1 Dubs-IN-1 is an active inhibitor of ubiquitin-specific proteases (USPs), with an IC50 of 0.85 μM for USP8.
E1214New KSQ-4279 KSQ-4279 (USP1-IN-1) is an orally bioavailable selective inhibitor of the ubiquitin specific protease 1 (USP1) with anti-proliferative activity. KSQ-4279 also exhibits synergistic activity in combination with PARP inhibitors.

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Tags: DUB inhibitor|DUB agonist|DUB activator|DUB inducer|DUB antagonist|DUB signaling pathway|DUB assay kit