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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-4279T600392446480-97-1KSQ-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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- Spautin-1T19371262888-28-7Spautin-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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Cited - MF-094T120242241025-68-1MF-094 is a selective USP30 inhibitor with IC50 of 0.12 μM. MF-094 can increase protein ubiquitination and accelerate mitophagy.
- $36
SizeQTY - Vialinin AT22168858134-23-3In houseVialinin 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
SizeQTY - USP1-IN-2T635182098212-05-4In houseUSP1-IN-2 is a potent USP1 inhibitor with potential anti-tumor activity for the study of cancer.
- $293
SizeQTY - I-138T735602098211-50-6I-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
SizeQTY - Wu-5T777632630378-05-9Wu-5 is a potent USP10 inhibitor that inhibits FLT3 and AMPK pathways, promoting the breakdown of FLT3-ITD and inducing apoptosis.
- $76
SizeQTY - VLX1570T40671431280-51-1VLX1570 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
SizeQTY - P005091T6925882257-11-6P005091 (P5091) is a selective and potent inhibitor of ubiquitin-specific protease 7 (USP7) with EC50 of 4.2 μM.
- $39
SizeQTY Cited - N-EthylmaleimideT3088128-53-0N-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
SizeQTY Cited - USP30 inhibitor 18T366822242582-40-5In houseUSP30 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
SizeQTY - ML364T35551991986-30-1ML364 is an inhibitor of ubiquitin specific peptidase 2 (USP2) and can be used for the research of breast cancer.
- $66
SizeQTY Cited - XL177AT91222417089-74-6XL177A is a selective irreversible USP7 inhibitor(IC50 : 0.34 nM). XL177A elicits cancer cell killing through a p53-dependent mechanism.
- $97
SizeQTY - DegrasynT6300856243-80-6Degrasyn (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
SizeQTY Cited - OTUB1/USP8-IN-1T727842858800-98-1In houseOTUB1 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
SizeQTY - BAY 11-7082T190219542-67-7BAY 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
SizeQTY Cited - IMP-1710T375912383117-96-0In houseIMP-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]
- $298
SizeQTY - ML-323T17571572414-83-5ML323 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.
- $218
SizeQTY Cited - USP25/28 inhibitor AZ1T76852165322-94-9USP25 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
SizeQTY - USP15-IN-1T615752260826-16-0In houseUSP15-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
SizeQTY - USP5-IN-1T60130USP5-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
SizeQTY - USP7/USP47 inhibitorT43381247825-37-1USP7 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.
- $40
SizeQTY
- GRL0617T114641093070-16-6GRL0617 is a selective and competitive noncovalent inhibitor of SARS-CoVPLpro and deubiquitinase (IC50: 0.6 μM, Ki: 0.49 μM).
- $31
SizeQTY Cited - USP30 inhibitor 11T132672067332-64-1In houseUSP30 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
SizeQTY - USP8-IN-1T601462477650-96-5USP8-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
SizeQTY - SJB3-019AT129262070015-29-9In houseSJB3-019A is a potent, potent and novel ubiquitin-specific protease 1 (USP1) inhibitor, which promotes ID1 degradation and cytotoxicity in K562 cells 5 times more than SJB2-043, with IC50 of 0.0781 μM. SJB3-019A inhibits cell proliferation and causes cell apoptosis.
- $95
SizeQTY - USP22-IN-1T73151309735-96-4USP22-IN-1 is a ubiquitin-specific peptidase 22 (USP22) inhibitor that can be used to treat proliferative diseases or cancer.
- $40
SizeQTY - PR-619T18622645-32-1PR-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
SizeQTY Cited - P 22077T24241247819-59-5P 22077 (P22077) is an inhibitor of ubiquitin-specific protease USP7 with EC50 of 8.6 μM. It also inhibits the closely related USP47.
- $32
SizeQTY Cited - LDN-57444T1924668467-91-2LDN-57444 is a reversible, competitive inhibitor of the proteasome Uch-L1 with an IC50 of 0.88 μM.
- $34
SizeQTY Cited - EOAI3402143T112091699750-95-2EOAI3402143 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
SizeQTY - OTUB1/USP8-IN-1 HClT72784L In houseOTUB1 USP8-IN-1 HCL is a potent dual inhibitor of OTUB1 and USP8 with potential antitumour activity, inhibiting both OTUB1 and USP8. OTUB1 USP8-IN-1 may be used in the study of leukaemia.
- $162
SizeQTY - HBX 41108T21527924296-39-9HBX 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
SizeQTY - DUB-IN-3T11112924296-17-3DUB-IN-3 is a potent deubiquitinase (USP) enzyme inhibitor with an IC50 of 0.56 μM for USP8.
- $139
SizeQTY - IU1T6107314245-33-5IU1(IC50=4.7 μ M), a reversible, specific human USP14 proteasome inhibitor, can penetrate the cell.
- $54
SizeQTY Cited - NSC632839T3951157654-67-6NSC-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
SizeQTY - B-AP15T19321009817-63-3B-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
SizeQTY Cited - 6-ThioguanineT3089154-42-76-Thioguanine (2-Amino-6-purinethiol) is an antineoplastic compound which also has antimetabolite action. The drug is used in the therapy of acute leukemia.
- $40
SizeQTY Cited - USP8-IN-2T678762477651-11-7USP8-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
SizeQTY - STD1TT36970893075-58-6STD1T 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
SizeQTY - TCIDT669730675-13-9TCID (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
SizeQTY - USP8-IN-3T678732477651-10-6USP8-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
SizeQTY - GNE-6640T54612009273-67-8GNE-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.
- $38
SizeQTY - DUB-IN-2T11111924296-19-5Dub-in-2, with an IC50 value of 0.28 for USP8, is an effective deubiquitinase inhibitor.
- $83
SizeQTY - IU1-47T15604670270-31-2IU1-47 is an effective and specific USP14 inhibitor (IC50: 0.6 μM). IU1-47 causes tau elimination in cultured neurons. IU1-47 inhibits IsoT/USP5 (IC50: 20 μM).
- $29
SizeQTY - GSK2643943AT114852449301-27-1GSK2643943A is a deubiquitylating enzyme (DUB) inhibitor, with an IC 50 of 160 nM for USP20/Ub-Rho. GSK2643943A has anti-tumor efficacy.
- $38
SizeQTY - IU1-248T93752307472-03-1IU1-248 is a derivative of IU1. IU1-248 is a potent and selective USP14 inhibitor with an IC50 of 0.83 μM[1].
- $42
SizeQTY - SJB2-043T767863388-44-3SJB2-043, an inhibitor of USP1-UAF1, has an IC50 of 544 nM.
- $47
SizeQTY - USP28-IN-4T747942931509-15-6USP28-IN-4 is a potent USP28 inhibitor with an IC50 value of 0.04 μM against USP28. USP28-IN-4 exhibits anticancer activity and inhibits USP2, USP7, USP8, USP9x, UCHL3 and UCHL5. USP28-IN-4 is cytotoxic to human colorectal and lung squamous carcinoma cells and dose-dependently downregulates c-Myc cellular levels through the ubiquitin-proteasome system. -proteasome system to dose-dependently downregulate cellular levels of c-Myc.
- $56
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