DUB

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DUB Signaling Pathways
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Catalog No. Product Name Information Product Use Citations Product Validations
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
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.
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.
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.
Br J Cancer, 2021, 10.1038/s41416-021-01421-x
Cell Chem Biol, 2021, S2451-9456(21)00213-0
Transl Lung Cancer Res, 2021, 10(10):3995-4011
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 Cell Biol, 2021, 23(4):355-365
Nat Commun, 2021, 12(1):1394
EMBO Rep, 2021, 22(9):e52576
S3692 N-Ethylmaleimide (NEM) N-Ethylmaleimide (NEM) 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.
EMBO J, 2021, 40(10):e106632
Cell Death Dis, 2021, 12(11):1050
J Hematol Oncol, 2020, 1;13(1):40
S4920 b-AP15 b-AP15 (NSC687852) is a deubiquitinases inhibitor for 19S proteasomes activity of Ub-AMC cleavage with IC50 of 2.1 μM.
Proc Natl Acad Sci U S A, 2021, 118(29)e2024562118
Cell Death Discov, 2021, 7(1):211
Cell Chem Biol, 2021, S2451-9456(21)00213-0
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.
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.
J Virol, 2020, JVI.01857-20
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.
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.
Int J Biol Sci, 2021, 17(10):2417-2429
Transl Lung Cancer Res, 2021, 10(10):3995-4011
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
S6883New 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.
S6943New 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).
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.
Mol Cell, 2021, S1097-2765(21)00800-5
Nat Commun, 2021, 12(1):2970
Nat Commun, 2021, 12(1):5263
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.
Nat Commun, 2021, 12(1):5010
J Clin Invest, 2021, 146893
Cell Death Dis, 2021, 12(5):456
S7133 P22077 P22077 is an inhibitor of ubiquitin-specific protease USP7 with EC50 of 8.6 μM, also inhibits the closely related USP47.
Nat Commun, 2021, 12(1):51
J Cell Sci, 2021, jcs.258922
J Cell Mol Med, 2021, 25(19):9228-9240
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.
Cell Death Dis, 2021, 12(9):803
FASEB J, 2021, 35(9):e21870
Cell Chem Biol, 2021, S2451-9456(21)00213-0
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.
Cell Biol Int, 2021, 10.1002/cbin.11662
J Int Med Res, 2021, 49(6):3000605211020641
Theranostics, 2020, 15;10(13):6048-6060
S7140 TCID TCID is a DUB inhibitor for ubiquitin C-terminal hydrolase L3 with IC50 of 0.6 μM, 125-fold selective to L1.
Cell Chem Biol, 2021, S2451-9456(21)00213-0
S7529 ML323 ML323 displays reversible, nanomolar inhibitory activity and excellent selectivity toward USP1/UAF1 with IC50 of 76 nM.
Oncogene, 2021, 40(25):4291-4306
J Exp Clin Cancer Res, 2021, 40(1):201
Front Pharmacol, 2021, 12:695009
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 Clin Invest, 2021, 146893
Protein Cell, 2021, 10.1007/s13238-021-00858-3
Autophagy, 2021, 1-19
S8288 VLX1570 VLX1570 is a competitive inhibitor of proteasome DUB activity, with an IC50 of ~10 μM in vitro.
Cancer Sci, 2021, 112(8):3302-3313
Research Square, 2021, 10.21203/rs.3.rs-265240/v1
J Med Chem, 2020, 9;63(7):3756-3762
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.
S8967New XL177A XL177A is a potent, selective and irreversible inhibitor of Ubiquitin specific peptidase 7 (USP7) with IC50 of 0.34 nM.
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
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.
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.
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.
Br J Cancer, 2021, 10.1038/s41416-021-01421-x
Cell Chem Biol, 2021, S2451-9456(21)00213-0
Transl Lung Cancer Res, 2021, 10(10):3995-4011
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 Cell Biol, 2021, 23(4):355-365
Nat Commun, 2021, 12(1):1394
EMBO Rep, 2021, 22(9):e52576
S3692 N-Ethylmaleimide (NEM) N-Ethylmaleimide (NEM) 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.
EMBO J, 2021, 40(10):e106632
Cell Death Dis, 2021, 12(11):1050
J Hematol Oncol, 2020, 1;13(1):40
S4920 b-AP15 b-AP15 (NSC687852) is a deubiquitinases inhibitor for 19S proteasomes activity of Ub-AMC cleavage with IC50 of 2.1 μM.
Proc Natl Acad Sci U S A, 2021, 118(29)e2024562118
Cell Death Discov, 2021, 7(1):211
Cell Chem Biol, 2021, S2451-9456(21)00213-0
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.
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.
J Virol, 2020, JVI.01857-20
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.
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.
Int J Biol Sci, 2021, 17(10):2417-2429
Transl Lung Cancer Res, 2021, 10(10):3995-4011
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
S6883New 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.
S6943New 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).
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.
Mol Cell, 2021, S1097-2765(21)00800-5
Nat Commun, 2021, 12(1):2970
Nat Commun, 2021, 12(1):5263
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.
Nat Commun, 2021, 12(1):5010
J Clin Invest, 2021, 146893
Cell Death Dis, 2021, 12(5):456
S7133 P22077 P22077 is an inhibitor of ubiquitin-specific protease USP7 with EC50 of 8.6 μM, also inhibits the closely related USP47.
Nat Commun, 2021, 12(1):51
J Cell Sci, 2021, jcs.258922
J Cell Mol Med, 2021, 25(19):9228-9240
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.
Cell Death Dis, 2021, 12(9):803
FASEB J, 2021, 35(9):e21870
Cell Chem Biol, 2021, S2451-9456(21)00213-0
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.
Cell Biol Int, 2021, 10.1002/cbin.11662
J Int Med Res, 2021, 49(6):3000605211020641
Theranostics, 2020, 15;10(13):6048-6060
S7140 TCID TCID is a DUB inhibitor for ubiquitin C-terminal hydrolase L3 with IC50 of 0.6 μM, 125-fold selective to L1.
Cell Chem Biol, 2021, S2451-9456(21)00213-0
S7529 ML323 ML323 displays reversible, nanomolar inhibitory activity and excellent selectivity toward USP1/UAF1 with IC50 of 76 nM.
Oncogene, 2021, 40(25):4291-4306
J Exp Clin Cancer Res, 2021, 40(1):201
Front Pharmacol, 2021, 12:695009
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 Clin Invest, 2021, 146893
Protein Cell, 2021, 10.1007/s13238-021-00858-3
Autophagy, 2021, 1-19
S8288 VLX1570 VLX1570 is a competitive inhibitor of proteasome DUB activity, with an IC50 of ~10 μM in vitro.
Cancer Sci, 2021, 112(8):3302-3313
Research Square, 2021, 10.21203/rs.3.rs-265240/v1
J Med Chem, 2020, 9;63(7):3756-3762
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.
S8967New XL177A XL177A is a potent, selective and irreversible inhibitor of Ubiquitin specific peptidase 7 (USP7) with IC50 of 0.34 nM.
S6883New HBX 19818 HBX19818 is a specific inhibitor of USP7 with an IC 50 of 28.1 μM.
S6943New 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).
S8967New XL177A XL177A is a potent, selective and irreversible inhibitor of Ubiquitin specific peptidase 7 (USP7) with IC50 of 0.34 nM.