E0389New |
DUBs-IN-2
|
DUBs-IN-2 is a potent inhibitor of USP7 and USP8 deubiquitinating enzymes. |
|
|
E1098New |
MF-094
|
MF-094, a potent and selective USP30 inhibitor (IC50=0.12 μM), accelerates diabetic wound healing by inhibiting the NLRP3 inflammasome. |
|
|
E1118New |
SJB3-019A
|
SJB3-019A, a potent USP1 inhibitor, is 5 times more potent than SJB2-043 in promoting inhibitor of DNA-binding-1 (ID1) degradation and cytoxicity with IC50 of 0.0781 μM in K562 cells. |
|
|
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 Med, 2022, 28(4):752-765
-
Gastroenterology, 2022, 162(6):1716-1731.e17
-
Adv Sci (Weinh), 2022, 10.1002/advs.202104055
|
|
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. |
-
Cell Rep, 2022, 38(12):110538
-
Invest Ophthalmol Vis Sci, 2022, 63(4):11
-
EMBO J, 2021, 40(10):e106632
|
|
S4920 |
b-AP15
|
b-AP15 (NSC687852) is a deubiquitinases inhibitor for 19S proteasomes activity of Ub-AMC cleavage with IC50 of 2.1 μM. |
-
Sci Adv, 2022, 8(3):eabj8357
-
Proc Natl Acad Sci U S A, 2021, 118(29)e2024562118
-
Cell Death Discov, 2021, 7(1):211
|
|
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. |
-
Cell Death Differ, 2022, 10.1038/s41418-022-00983-4
-
Cells, 2022, 11(6)1006
-
Apoptosis, 2022, 10.1007/s10495-021-01706-9
|
|
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. |
-
Sci Adv, 2022, 8(3):eabj8357
-
Nat Commun, 2021, 12(1):5010
-
J Clin Invest, 2021, 146893
|
|
S7133 |
P22077
|
P22077 is an inhibitor of ubiquitin-specific protease USP7 with EC50 of 8.6 μM, also inhibits the closely related USP47. |
-
Cell Biochem Funct, 2022, 10.1002/cbf.3702
-
Nat Commun, 2021, 12(1):51
-
J Cell Sci, 2021, jcs.258922
|
|
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. |
-
Nat Commun, 2022, 13(1):1700
-
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. |
-
Autophagy, 2022, 1-20
-
Atherosclerosis, 2022, 343:10-19
-
J Clin Invest, 2021, 146893
|
|
S8288 |
VLX1570
|
VLX1570 is a competitive inhibitor of proteasome DUB activity, with an IC50 of ~10 μM in vitro. |
-
Front Pharmacol, 2021, 12:778216
-
Cancer Sci, 2021, 112(8):3302-3313
-
Research Square, 2021, 10.21203/rs.3.rs-265240/v1
|
|
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. |
|
|
S8967 |
XL177A
|
XL177A is a potent, selective and irreversible inhibitor of Ubiquitin specific peptidase 7 (USP7) with IC50 of 0.34 nM. |
|
|
E0389New |
DUBs-IN-2
|
DUBs-IN-2 is a potent inhibitor of USP7 and USP8 deubiquitinating enzymes. |
|
|
E1098New |
MF-094
|
MF-094, a potent and selective USP30 inhibitor (IC50=0.12 μM), accelerates diabetic wound healing by inhibiting the NLRP3 inflammasome. |
|
|
E1118New |
SJB3-019A
|
SJB3-019A, a potent USP1 inhibitor, is 5 times more potent than SJB2-043 in promoting inhibitor of DNA-binding-1 (ID1) degradation and cytoxicity with IC50 of 0.0781 μM in K562 cells. |
|
|
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 Med, 2022, 28(4):752-765
- Gastroenterology, 2022, 162(6):1716-1731.e17
- Adv Sci (Weinh), 2022, 10.1002/advs.202104055
|
|
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. |
- Cell Rep, 2022, 38(12):110538
- Invest Ophthalmol Vis Sci, 2022, 63(4):11
- EMBO J, 2021, 40(10):e106632
|
|
S4920 |
b-AP15
|
b-AP15 (NSC687852) is a deubiquitinases inhibitor for 19S proteasomes activity of Ub-AMC cleavage with IC50 of 2.1 μM. |
- Sci Adv, 2022, 8(3):eabj8357
- Proc Natl Acad Sci U S A, 2021, 118(29)e2024562118
- Cell Death Discov, 2021, 7(1):211
|
|
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. |
- Cell Death Differ, 2022, 10.1038/s41418-022-00983-4
- Cells, 2022, 11(6)1006
- Apoptosis, 2022, 10.1007/s10495-021-01706-9
|
|
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. |
- Sci Adv, 2022, 8(3):eabj8357
- Nat Commun, 2021, 12(1):5010
- J Clin Invest, 2021, 146893
|
|
S7133 |
P22077
|
P22077 is an inhibitor of ubiquitin-specific protease USP7 with EC50 of 8.6 μM, also inhibits the closely related USP47. |
- Cell Biochem Funct, 2022, 10.1002/cbf.3702
- Nat Commun, 2021, 12(1):51
- J Cell Sci, 2021, jcs.258922
|
|
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. |
- Nat Commun, 2022, 13(1):1700
- 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. |
- Autophagy, 2022, 1-20
- Atherosclerosis, 2022, 343:10-19
- J Clin Invest, 2021, 146893
|
|
S8288 |
VLX1570
|
VLX1570 is a competitive inhibitor of proteasome DUB activity, with an IC50 of ~10 μM in vitro. |
- Front Pharmacol, 2021, 12:778216
- Cancer Sci, 2021, 112(8):3302-3313
- Research Square, 2021, 10.21203/rs.3.rs-265240/v1
|
|
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. |
|
|
S8967 |
XL177A
|
XL177A is a potent, selective and irreversible inhibitor of Ubiquitin specific peptidase 7 (USP7) with IC50 of 0.34 nM. |
|
|