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Cell Cycle/Checkpoint Filter
Cell Cycle/Checkpoint DNA Damage/DNA Repair UbiquitinationDUB
Deubiquitinating enzymes (DUBs), also known as deubiquitinating peptidases, deubiquitinating isopeptidases, deubiquitinases, ubiquitin proteases, ubiquitin hydrolases, ubiquitin isopeptidases, are a large group of proteases that cleave ubiquitin from proteins and other molecules. Ubiquitin is attached to proteins in order to regulate the degradation of proteins via the proteasome and lysosome; coordinate the cellular localisation of proteins; activate and inactivate proteins; and modulate protein-protein interactions.DUBs can reverse these effects by cleaving the peptide or isopeptide bond between ubiquitin and its substrate protein. In humans there are nearly 100 DUB genes, which can be classified into two main classes: cysteine proteases and metalloproteases. The cysteine proteases comprise ubiquitin-specific proteases (USPs), ubiquitin C-terminal hydrolases (UCHs), Machado-Josephin domain proteases (MJDs) and ovarian tumour proteases (OTU). The metalloprotease group contains only the Jab1/Mov34/Mpr1 Pad1 N-terminal+ (MPN+) (JAMM) domain proteases.
KSQ-4279
T600392446480-97-1
KSQ-4279 (USP1-IN-1) is an inhibitor of USP1 and PARP, exhibiting anticancer activity. It is utilized in the study of non-small cell lung cancer, osteosarcoma, ovarian, breast, glioblastoma, bladder, uterine, and pancreatic cancers.
- $158
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IMP-1710
T375912383117-96-0In house
IMP-1710 is a selective UCH-L1 inhibitor with an IC50 value of 38 nM in a fluorescence polarization assay.IMP-1710 has antifibrotic activity. [1]
- $156
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Vialinin A
T22168858134-23-3In house
Vialinin A (Terrestrin A), a p-terphenyl compound, exhibits antioxidant properties and acts as a potent inhibitor of TNF-α, USP4, USP5, and sentrin SUMO-specific protease 1 (SENP1). Its efficacy in autoimmune diseases and cancer research is noteworthy, highlighting its potential therapeutic applications.
- $213
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USP1-IN-2
T635182098212-05-4In house
USP1-IN-2 is a potent USP1 inhibitor with potential anti-tumor activity for the study of cancer.
- $293
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Degrasyn
Cited
T6300856243-80-6
Degrasyn (WP1130) (WP1130), a specific deubiquitinase (DUB: USP5, UCH-L1, USP9x, USP14, and UCH37) inhibitor, also inhibits Bcr Abl, which is a JAK2 transducer (without affecting 20S proteasome) and activator of transcription (STAT).
- $58
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CitedN-Ethylmaleimide Cited
T3088128-53-0
N-Ethylmaleimide (NEM) is a reagent for alkylation of free sulfhydryl groups, a cysteine protease inhibitor used in experimental biochemistry. N-Ethylmaleimide is also a deubiquitinating enzyme inhibitor that specifically inhibits phosphate transport in mitochondria.
- $39
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CitedBAY 11-7082 Cited
T190219542-67-7
BAY 11-7082 (BAY 11-7821) is an NF-κB inhibitor that suppresses TNFα-induced IκBα phosphorylation (IC50=10 μM) and also inhibits the ubiquitin-specific proteases USP7 and USP21 (IC50=0.19 0.96 μM).
- $43
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CitedI-138
T735602098211-50-6
I-138 is an orally active and potent reversible inhibitor of USP1-UAF1.I-138 induces mono-ubiquitination of FANCD2 and PCNA and inhibits USP1 auto-cleavage in cells.
- $198
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Wu-5
T777632630378-05-9
Wu-5 is a potent USP10 inhibitor that inhibits FLT3 and AMPK pathways, promoting the breakdown of FLT3-ITD and inducing apoptosis.
- $76
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USP30 inhibitor 18
T366822242582-40-5In house
USP30 inhibitor 18 is a selective USP30 inhibitor with an IC50 of 0.02 μM. USP30 inhibitor 18 increases protein ubiquitination and accelerates mitophagy[1]. [1]. Arthur F Kluge, et al. Novel highly selective inhibitors of ubiquitin specific protease 30 (USP30) accelerate mitophagy. Bioorg Med Chem Lett. 2018 Aug 15;28(15):2655-2659.
- $147
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OTUB1/USP8-IN-1
T727842858800-98-1In house
OTUB1 USP8-IN-1 is a potent OTUB1 USP8 inhibitor with potential anticancer activity, demonstrating IC50 values of 0.17 nM for OTUB1 and 0.28 nM for USP8. OTUB1 USP8-IN-1 can be used in the study of non-small-cell lung cancer.
- $100
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USP15-IN-1
T615752260826-16-0In house
USP15-IN-1 is a potent USP15 inhibitor (IC50 is 3.76 μM) with high antiproliferative activity against non-small cell lung cancer and leukemia cells. As an interacting protein of cGAS, USP15 promotes cGAS to recognize DNA and activate downstream signaling pathways.
- $128
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XL177A
T91222417089-74-6
XL177A is a selective irreversible USP7 inhibitor(IC50 : 0.34 nM). XL177A elicits cancer cell killing through a p53-dependent mechanism.
- $97
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DUB-IN-3
T11112924296-17-3
DUB-IN-3 is a potent deubiquitinase (USP) enzyme inhibitor with an IC50 of 0.56 μM for USP8.
- $139
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P005091 Cited
T6925882257-11-6
P005091 (P5091) is a selective and potent inhibitor of ubiquitin-specific protease 7 (USP7) with EC50 of 4.2 μM.
- $39
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CitedML364 Cited
T35551991986-30-1
ML364 is an inhibitor of ubiquitin specific peptidase 2 (USP2) and can be used for the research of breast cancer.
- $66
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CitedMF-094
T120242241025-68-1
MF-094 is a selective USP30 inhibitor with IC50 of 0.12 μM. MF-094 can increase protein ubiquitination and accelerate mitophagy.
- $36
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USP5-IN-1
T60130
USP5-IN-1 (compound 64) is a potent deubiquitinase USP5 inhibitor that binds to the USP5 ZnF-UBD with a KD of 2.8 μM and is selective over nine proteins containing structurally similar ZnF-UBD domains. Additionally, USP5-IN-1 inhibits the USP5 catalytic cleavage of a di-ubiquitin substrate [1].
- $80
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PR-619
Cited
T18622645-32-1
PR-619 (2,6-Diamino-3,5-dithiocyanopyridine) is a DUB inhibitor that inhibits USP2 4 5 7 8 (EC50=7.2 3.93 8.61 6.86 4.9 μM). PR-619 induces endoplasmic reticulum stress and activates autophagy.
- $45
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CitedB-AP15 Cited
T19321009817-63-3
B-AP15 (NSC-687852)(NSC-687852) is a selective inhibitor of the deubiquitinating enzymes Usp14 and UCHL5 of the 26S proteasome. It blocks the deubiquitinating activity of the 26S proteasome.
- $32
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CitedUSP8-IN-1
T601462477650-96-5
USP8-IN-1 is an inhibitor of USP8 with an IC 50 of 1.9 μM. USP8-IN-1 inhibits H1975 cell growth with a GI 50 of 82.04 μM [1].
- $81
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GRL0617 Cited
T114641093070-16-6
GRL0617 is a selective and competitive noncovalent inhibitor of SARS-CoVPLpro and deubiquitinase (IC50: 0.6 μM, Ki: 0.49 μM).
- $31
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CitedEOAI3402143
T112091699750-95-2
EOAI3402143 inhibits Usp9x and Usp24 activity, increases tumor cell apoptosis. EOAI3402143 phenocopies the FAS induction and apoptotic sensitization of Usp5 knockdown and fully blocks melanoma tumor growth.
- $61
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NSC632839
T3951157654-67-6
NSC-632839 (Ubiquitin Isopeptidase Inhibitor II) is a nonselective isopeptidase inhibitor, which inhibits USP2 (EC50: 45±4 μM), USP7 (EC50: 37±1 μM), and SENP2 (EC50: 9.8±1.8 μM).
- $47
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USP7-797
T732342413944-70-2In house
USP7-797 is a selective non-covalent active site USP7 inhibitor, inhibiting USP7 and ubiquitin binding, with anti-tumor, oral and high efficiency (IC50=0.44 nmol), it is effective on both wild-type and mutant p53 tumor cells, and can significantly inhibit the growth of tumor cells and induce apoptosis.
- $545
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IU1 Cited
T6107314245-33-5
IU1(IC50=4.7 μ M), a reversible, specific human USP14 proteasome inhibitor, can penetrate the cell.
- $54
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CitedGSK2643943A
T114852449301-27-1
GSK2643943A is a deubiquitylating enzyme (DUB) inhibitor, with an IC 50 of 160 nM for USP20 Ub-Rho. GSK2643943A has anti-tumor efficacy.
- $38
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LDN-57444 Cited
T1924668467-91-2
LDN-57444 is a reversible, competitive inhibitor of the proteasome Uch-L1 with an IC50 of 0.88 μM.
- $34
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CitedUSP22-IN-1
T73151309735-96-4
USP22-IN-1 is a ubiquitin-specific peptidase 22 (USP22) inhibitor that can be used to treat proliferative diseases or cancer.
- $40
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Spautin-1 Cited
T19371262888-28-7
Spautin-1 is an autophagy inhibitor that suppresses the deubiquitination activity of ubiquitin-specific peptidase USP10 and USP13. Spautin-1 inhibits UPR and exhibits preferential cytotoxicity in glucose-starved cancer cells.
- $33
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CitedVLX1570
T40671431280-51-1
VLX1570 is a competitive inhibitor of proteasome DUB activity, with an IC50 ranging from 4.2 μM to 8.6 μM, and exhibits potent inhibition of USP14.
- $97
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USP25/28 inhibitor AZ1
T76852165322-94-9
USP25 28 inhibitor AZ1 is a selective, orally active and non-competitive dual ubiquitin-specific protease USP25 28 inhibitor with IC50 of 0.7 μM and 0.6 μM, respectively, and exhibits anti-inflammatory and anti-tumor effects.
- $30
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DUB-IN-1
T11110924296-18-4
DUB-IN-1, with an IC50 value of 0.24 for USP8, is an active inhibitor of ubiquitin-specific protease (USPs).
- $59
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HBX 41108
T21527924296-39-9
HBX 41108 (HBX-41108) is a non-competitive, reversible inhibitor of USP7 with an IC50 of 424nM. HBX 41108 inhibited deubiquitination of p53 mediated by USP7 in a dose-dependent manner with an IC50 of 0.8μM.
- $47
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DUB-IN-2
T11111924296-19-5
Dub-in-2, with an IC50 value of 0.28 for USP8, is an effective deubiquitinase inhibitor.
- $72
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USP7-IN-1
T132681381291-36-6
USP7-IN-1 is a selective and reversible inhibitor of ubiquitin-specific protease 7 (USP7) with an IC50 of 77 μM.
- $98
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USP7/USP47 inhibitor
T43381247825-37-1
USP7 USP47 inhibitor (USP7 47 inhibitor-1) is a selective ubiquitin-specific protease 7 47 (USP7 USP47) inhibitor, with EC50s of 0.42 μM and 1.0 μM, respectively.
- $36
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USP8-IN-2
T678762477651-11-7
USP8-IN-2 is a potent inhibitor of the deubiquitinating enzymes USP7 and USP8, with an IC50 of 4.0 μM against USP8D. USP8-IN-2 is a potential compound for the treatment of cancer and viral infections.
- $90
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TCID
T669730675-13-9
TCID (UCH-L3 Inhibitor)(IC50=0.6 μM) is a DUB inhibitor of ubiquitin C-terminal hydrolase L3. It has the 125-fold selectivity to L1.
- $33
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ML-323 Cited
T17571572414-83-5
ML323 is a reversible and effective USP1-UAF1 inhibitor in a Ub-Rho assay (IC50: 76 nM) and in orthogonal gel-based assays using K63-linked diubiquitin (di-Ub) (IC50: 174 nM 820 nM)and monoubiquitinated PCNA (Ub-PCNA) (IC50: 820 nM) as substrates, respectively.
- $91
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CitedUSP8-IN-3
T678732477651-10-6
USP8-IN-3 is a potent inhibitor of the deubiquitinating enzymes USP7 and USP8, with IC50 of 4.0 μM against USP8D. USP8-IN-3 inhibited the proliferation of GH3 and H1957 cells with GI50 values of 37.03 μM and 6.01 μM, respectively. USP8-IN-3 is a potential compound for the treatment of cancer and viral infections.
- $30
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USP30 inhibitor 11
T132672067332-64-1In house
USP30 inhibitor 11 (USP30-IN-11) is a selective USP30 inhibitor (IC50: 0.01 µΜ) that inhibits SVA and can be used in studies of cancer, mitochondrial dysfunction and Parkinson's.
- $215
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STD1T
T36970893075-58-6
STD1T is a selective and potent inhibitor of the deubiquitinase USP2a with potential anticancer activity that reduces cell cycle protein D1 protein levels in HCT116 colon and MCF-7 breast cancer cells.
- $225
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IU1-248
T93752307472-03-1
IU1-248 is a derivative of IU1. IU1-248 is a potent and selective USP14 inhibitor with an IC50 of 0.83 μM[1].
- $45
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USP7-IN-8
T92172009273-60-1
Benzamide, 4-[6-amino-4-ethyl-5-(4-hydroxyphenyl)-3-pyridinyl]-N-methyl- is a selective ubiquitin-specific protease 7 (USP7) inhibitor with an IC50 of 1.4 μM. USP7-IN-8 (GNE-6776) has anticancer effects.
- $40
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P 22077 Cited
T24241247819-59-5
P 22077 (P22077) is an inhibitor of ubiquitin-specific protease USP7 with EC50 of 8.6 μM. It also inhibits the closely related USP47.
- $32
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CitedGNE-6640
T54612009273-67-8
GNE-6640 is a non-covalent inhibitor targeting ubiquitin specific peptidase 7 (USP7), exhibiting IC50 values of 0.75 μM for full-length USP7, 0.43 μM for the USP7 catalytic domain, 20.3 μM for full-length USP43, and 0.23 μM for Ub-MDM2, respectively.
- $64
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