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, 76:103323
-
Redox Biol, 2024, 70:103072
|
|
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
-
Mol Cell, 2024, 84(16):3115-3127.e11
-
BMC Biol, 2024, 22(1):71
|
|
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
-
Int J Mol Sci, 2024, 25(5)2768
-
Nat Commun, 2023, 14(1):8481
|
|
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
-
Clin Cancer Res, 2023, 29(2):446-457
-
Cancer Cell Int, 2023, 23(1):207
|
|
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. |
-
Nat Commun, 2024, 15(1):9463
-
J Adv Res, 2024, S2090-1232(24)00025-0
-
Cancer Lett, 2024, 604:217258
|
|
S7133 |
P22077
|
P22077 is an inhibitor of ubiquitin-specific protease USP7 with EC50 of 8.6 μM, also inhibits the closely related USP47. |
-
Int J Mol Sci, 2024, 25(5)2768
-
Hepatol Commun, 2024, 8(4)e0405
-
EMBO Rep, 2022, e54391
|
|
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. |
-
Redox Biol, 2024, 76:103318
-
Antioxidants (Basel), 2024, 13(1)114
-
Nat Commun, 2022, 13-1:5644
|
|
S4920 |
b-AP15
|
b-AP15 (NSC687852) is a deubiquitinases inhibitor for 19S proteasomes activity of Ub-AMC cleavage with IC50 of 2.1 μM. |
-
J Transl Med, 2024, 22(1):193
-
Commun Biol, 2024, 7(1):25
-
Science, 2023, 380(6647):eadf2018
|
|
S7529 |
ML323
|
ML323 displays reversible, nanomolar inhibitory activity and excellent selectivity toward USP1/UAF1 with IC50 of 76 nM. |
-
Nucleic Acids Res, 2024, gkae785
-
Mol Med, 2024, 30(1):121
-
Blood Adv, 2023, 7(13):3099-3112
|
|
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. |
-
J Transl Med, 2024, 22(1):478
-
Cells, 2024, 13(9)737
-
Mol Cells, 2023, 46(8):476-485
|
|
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. |
-
BMC Biol, 2024, 22(1):71
-
Cell Rep Med, 2023, 10.1016/j.xcrm.2023.101286
-
Int J Mol Sci, 2023, 25(1)423
|
|
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
-
Int J Biol Sci, 2021, 17(10):2417-2429
|
|
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 is a potent papain-like protease (PLpro) inhibitor with IC50 of 2.6 μM. |
-
PLoS Pathog, 2023, 19(8):e1011592
-
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. |
|
|
E1633New |
BAY-805
|
BAY-805 is a potent, selective, and cell-active inhibitor that non-covalently targets the catalytic activity of USP21, a member of the ubiquitin-specific protease (USP) subfamily of deubiquitinating enzymes (DUBs). |
|
|
E1479 |
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. |
|
|
E0392 |
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. |
-
J Virol, 2024, e0085524.
|
|
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. |
|
|
E1214 |
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. |
-
Cancer Res, 2024, 84(20):3419-3434
-
Sci Adv, 2024, 10(46):eadp6567
|
|
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, 76:103323
- Redox Biol, 2024, 70:103072
|
|
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
- Mol Cell, 2024, 84(16):3115-3127.e11
- BMC Biol, 2024, 22(1):71
|
|
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
- Int J Mol Sci, 2024, 25(5)2768
- Nat Commun, 2023, 14(1):8481
|
|
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
- Clin Cancer Res, 2023, 29(2):446-457
- Cancer Cell Int, 2023, 23(1):207
|
|
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. |
- Nat Commun, 2024, 15(1):9463
- J Adv Res, 2024, S2090-1232(24)00025-0
- Cancer Lett, 2024, 604:217258
|
|
S7133 |
P22077
|
P22077 is an inhibitor of ubiquitin-specific protease USP7 with EC50 of 8.6 μM, also inhibits the closely related USP47. |
- Int J Mol Sci, 2024, 25(5)2768
- Hepatol Commun, 2024, 8(4)e0405
- EMBO Rep, 2022, e54391
|
|
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. |
- Redox Biol, 2024, 76:103318
- Antioxidants (Basel), 2024, 13(1)114
- Nat Commun, 2022, 13-1:5644
|
|
S4920 |
b-AP15
|
b-AP15 (NSC687852) is a deubiquitinases inhibitor for 19S proteasomes activity of Ub-AMC cleavage with IC50 of 2.1 μM. |
- J Transl Med, 2024, 22(1):193
- Commun Biol, 2024, 7(1):25
- Science, 2023, 380(6647):eadf2018
|
|
S7529 |
ML323
|
ML323 displays reversible, nanomolar inhibitory activity and excellent selectivity toward USP1/UAF1 with IC50 of 76 nM. |
- Nucleic Acids Res, 2024, gkae785
- Mol Med, 2024, 30(1):121
- Blood Adv, 2023, 7(13):3099-3112
|
|
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. |
- J Transl Med, 2024, 22(1):478
- Cells, 2024, 13(9)737
- Mol Cells, 2023, 46(8):476-485
|
|
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. |
- BMC Biol, 2024, 22(1):71
- Cell Rep Med, 2023, 10.1016/j.xcrm.2023.101286
- Int J Mol Sci, 2023, 25(1)423
|
|
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
- Int J Biol Sci, 2021, 17(10):2417-2429
|
|
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 is a potent papain-like protease (PLpro) inhibitor with IC50 of 2.6 μM. |
- PLoS Pathog, 2023, 19(8):e1011592
- 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. |
|
|
E1633New |
BAY-805
|
BAY-805 is a potent, selective, and cell-active inhibitor that non-covalently targets the catalytic activity of USP21, a member of the ubiquitin-specific protease (USP) subfamily of deubiquitinating enzymes (DUBs). |
|
|
E1479 |
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. |
|
|
E0392 |
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. |
- J Virol, 2024, e0085524.
|
|
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. |
|
|
E1214 |
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. |
- Cancer Res, 2024, 84(20):3419-3434
- Sci Adv, 2024, 10(46):eadp6567
|
|