DUB

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DUB製品

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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.
MedComm (2020), 2025, 6(1):e70037
Int J Biol Sci, 2025, 21(1):346-362
Cell Rep, 2025, S2211-1247(25)00057-9
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.
J Orthop Surg Res, 2025, 20(1):220
Nat Commun, 2024, 15(1):1642
Mol Cell, 2024, 84(16):3115-3127.e11
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.
Mol Metab, 2025, 94:102111
J Exp Clin Cancer Res, 2024, 43(1):28
Int J Mol Sci, 2024, 25(5)2768
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.
Nat Commun, 2025, 16(1):628
Nat Commun, 2025, 16(1):1313
Mol Metab, 2025, 94:102111
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
Cell Death Discov, 2024, 10(1):295
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 Control Release, 2025, 380:417-432
J Transl Med, 2024, 22(1):193
Commun Biol, 2024, 7(1):25
S7529 ML323 ML323 displays reversible, nanomolar inhibitory activity and excellent selectivity toward USP1/UAF1 with IC50 of 76 nM.
Oncol Res, 2025, 33(1):213-224
Nucleic Acids Res, 2024, gkae785
Mol Med, 2024, 30(1):121
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.
Toxicol Lett, 2025, 406:31-37
J Exp Clin Cancer Res, 2024, 43(1):330
BMC Biol, 2024, 22(1):71
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
F3038New USP10 Rabbit mAb
F0629New HAUSP Rabbit mAb HAUSP Rabbit mAb detects endogenous levels of total HAUSP protein.
F1361New USP15 Rabbit mAb USP15 Rabbit mAb recognizes endogenous levels of total USP15 protein.
F1387New USP9X Rabbit mAb
F0865New USP14 Rabbit mAb
F2044New USP22 Rabbit mAb
F1344New OTUD5 Rabbit mAb
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.
J Biol Chem, 2025, 301(3):108190
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

DUB阻害剤の選択性比較

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