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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.
- IMP-1710T375912383117-96-0In houseIMP-1710 is a selective UCH-L1 inhibitor with an IC50 value of 38 nM in a fluorescence polarization assay.
- $298
SizeQTY
- USP25/28 inhibitor AZ1T76852165322-94-9USP25/28 inhibitor AZ1 (AZ1) (AZ1) is an inhibitor of ubiquitin specific protease (USP) 25/28
- $46
SizeQTY - MF-094T120242241025-68-1MF-094 is a potent and selective inhibitor of USP30 (IC50 of 120 nM).
- $36
SizeQTY - 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.
- $117
SizeQTY
- P22074T2828490680-28-7In houseP22074 is a USP7 inhibitor. It is not an active antagonist like its halogenated related compounds. p22074 has antitumour activity.
- $350
SizeQTY - USP28-IN-3T747932931509-14-5In houseUSP28-IN-3 is a highly selective USP28 inhibitor with an IC50 value of 0.1 μM against USP28.USP28-IN-3 exhibits anticancer activity and inhibits USP2, USP7, USP8, USP9x, UCHL3, and UCHL5.USP28-IN-3 is cytotoxic to human colorectal and lung squamous carcinoma cells, inhibiting c-cells and c-neutralizing c-neutralizing c-neutralizing c-neutralizing c-neutralizing c-neutralizing c-neutralizing c-cells through the ubiquitin-proteasome system. -proteasome system to dose-dependently downregulate cellular levels of c-Myc.
- $293
SizeQTY - $293
- 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.
- $293
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 - OTUB1/USP8-IN-1T727842858800-98-1In houseOTUB1/USP8-IN-1 is a potent OTUB1/USP8 inhibitor with potential anticancer activity, with IC50 values of 0.17 and 0.28 nM for OTUB1 and USP8, respectively.OTUB1/USP8-IN-1 can be used in the study of non-small-cell lung cancer.
- $100
SizeQTY - USP15-IN-1T615752260826-16-0In houseUSP15-IN-1 is a potent USP15 inhibitor (IC50 is 3.76 μM). USP15-IN-1 showed high antiproliferative activity against non-small cell lung cancer and leukemia cells. USP15 is an interacting protein of cGAS, and USP15 can promote cGAS to recognize DNA and activate downstream signaling pathways.
- $128
SizeQTY - 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 - 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 - 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 - 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 - 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 - 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 - 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 - 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 - 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 - Spautin-1T19371262888-28-7Spautin-1 is a novel autophagy inhibitor, IM inhibited the growth of K562 cells with IC50 of 1.03 μM. In contrast, co-treatment with Spautin-1 increased IM-induced inhibition of cell viability with IC50 of 0.45 μM.
- $33
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 - BAY 11-7082T190219542-67-7BAY 11-7082 (BAY 11-7821) is an NF-κB inhibitor that inhibits TNFα-induced IκBα phosphorylation (IC50=10 μM). BAY 11-7082 is also an inhibitor of the ubiquitin-specific proteases USP7 and USP21 (IC50=0.19/0.96 μM).
- $43
SizeQTY Cited - LDN-91946T15729439946-22-2LDN-91946 is an effective and selective inhibitor of ubiquitin C-terminal hydrolase-L1 (UCH-L1) (Ki = 2.8 μM).
- $39
SizeQTY - USP7-IN-1T132681381291-36-6USP7-IN-1 is a selective and reversible ubiquitin-specific protease 7 (USP7) inhibitor (IC50 = 77 μM).
- $163
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 - RA-9T8464919091-63-7RA-9 is a potent and selective proteasome-associated inhibitor of deubiquitinating enzymes (DUBs), with favorable toxicity profile and anticancer activity. RA-9 selectively induces apoptosis in ovarian cancer cell lines.
- $38
SizeQTY - DUB-IN-3T11112924296-17-3DUB-IN-3 is a potent deubiquitinase (USP) enzyme inhibitor and the IC50 for USP8 is 0.56 μM.
- $139
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.
- $64
SizeQTY - LDN-57444T1924668467-91-2LDN-57444 is a reversible, competitive proteasome Uch-L1 inhibitor(IC50=0.88 μM) .
- $34
SizeQTY Cited - PR-619T18622645-32-1PR-619 (2,6-Diamino-3,5-dithiocyanopyridine) is a non-selective, reversible inhibitor of the deubiquitinylating enzymes (DUBs).
- $45
SizeQTY Cited - USP7-IN-8T92172009273-60-1Benzamide, 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.
- $67
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 - FT827T153511959537-86-0FT827 is a covalent inhibitor of selective ubiquitin-specific protease 7 (USP7) (Ki=4.2 µM, Kd=7.8 µM) targeting the catalytic center of the autoinhibitory apolipoprotein form of USP7 for cancer research.
- $397
SizeQTY - USP7-IN-5T132702166599-74-0USP7-IN-5 is a potent inhibitor of ubiquitin-specific protease 7 (USP7, IC50: 49.9 nM).
- $2,570
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 - KSQ-4279T600392446480-97-1KSQ-4279 (USP1-IN-1) is an inhibitor of USP1 and PARP.KSQ-4279 has anticancer activity and is used in the study of non-small cell lung cancer, osteosarcoma, ovarian, breast, glioblastoma, bladder, uterine and pancreatic cancers.
- $158
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 - 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 - N-EthylmaleimideT3088128-53-0N-Ethylmaleimide (NEM) is a sulfhydryl reagent that is widely used in experimental biochemical studies.
- $39
SizeQTY Cited - USP7-IN-6T132712166586-47-4USP7-IN-6 is a potent inhibitor of ubiquitin-specific protease 7 (USP7, IC50: 6.8 nM).
- $2,720
SizeQTY - DUB-IN-1T11110924296-18-4DUB-IN-1, with an IC50 value of 0.24 for USP8, is an active inhibitor of ubiquitin-specific protease (USPs).
- $98
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].
- $87
SizeQTY - 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 - 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 - USP7-IN-3T132692202738-42-7USP7-IN-3 is a potent and selective allosteric inhibitor of ubiquitin-specific protease 7 (USP7).
- $2,120
SizeQTY - FT671T12621L1959551-26-8FT671 is a non-covalent and selective inhibitor of USP7 (IC50: 52 nM) It also binds to the USP7 catalytic domain (Kd: 65 nM).
- $2,120
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.
- $78
SizeQTY
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