Deubiquitinases (DUBs) are a family of proteases whose function is to cleave ubiquitin (Ub) or ubiquitin-like proteins from proproteins or ubiquitin(s) conjugated with target substrate.According to their enzymatic cleavage method, DUBs can be classified into two primary classes: zinc metalloproteases and cysteine proteases. These include Jab1/Mov34/Mpr1 (JAMM) metalloproteases, ovarian tumor proteases, Machado-Joseph disease proteases, ubiquitin-specific proteases (USPs), ubiquitin C-terminal hydrolases (UCHs), and novel DUB family, (MINDY) proteases that contain MIU.
A significant post-translational alteration known as ubiquitination is essential for several crucial biological processes. A coordinated action of the E1, E2, and E3 enzymes results in the attachment of ubiquitin to a substrate protein in this process, and DUBs remove it. DUBs are crucial Ub system regulators because they control a wide range of cellular functions, such as protein sorting, trafficking, and turnover. Alterations in DUB activity have been linked to a wide range of diseases, including cancer. DUBs are fresh options for the creation of drugs that are target-directed.
| Structure | Cat No. | Product Name | CAS No. | Product Description |
|---|---|---|---|---|
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V54456 | IMP-1710 | 2383117-96-0 | IMP-1710 is a potent and specific inhibitor of the deubiquitinating enzyme UCHL1 with IC50 of 38 nM. |
|
V51255 | IU1-248 | 2307472-03-1 | IU1-248 is an analogue of IU1 and a potent and specific USP14 inhibitor (antagonist) with IC50 of 0.83 μM. |
|
V93539 | JMS-175-2 | 3042887-70-4 | JMS-175-2 is a potent inhibitor of BRCC36 isopeptidase complex (BRISC) with IC50 of 3.8 μM. |
|
V103307 | KSQ-4279 (gentisate) | 2938991-80-9 | KSQ-4279 (gentisate) (Compound Formula I) is a potent USP1 inhibitor and a selective PARP1 inhibitor. |
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V93015 | MS1172 | 3058588-43-2 | MS1172 (XH161-172; Example 54) is an orally available USP2 inhibitor that plays an important role in cancer and viral infections. |
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V56174 | N-Ethylmaleimide-d5 (NEM-d5) | 360768-37-2 | N-Ethylmaleimide-d5 is the deuterated form of N-Ethylmaleimide. |
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V41058 | OTUB1/USP8-IN-1 | 2858800-98-1 | OTUB1/USP8-IN-1 is a potent dual OTUB1/USP8 inhibitor (antagonist) with IC50s of 0.17 and 0.28 nM for OTUB1 and USP8 inhibition, respectively. |
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V88632 | OTUB1/USP8-IN-1 TFA | OTUB1/USP8-IN-1 TFA is the TFA salt form of OTUB1/USP8-IN-1. | |
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V88631 | OTUB2-IN-1 | OTUB2-IN-1 is a specific inhibitor of OTUB2 (KD approximately 12 μM), which can reduce the expression of PD-L1 protein in tumor cells and inhibit tumors by promoting strong intratumoral infiltration of cytotoxic T lymphocytes (CTL). | |
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V102564 | rac-MF-094 | 2758431-95-5 | rac-MF-094 is the racemate of MF-094. |
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V35255 | STAMBP-IN-1 | 896683-78-6 | STAMBP-IN-1 is a small molecule inhibitor of STAMBP deubiquitinase that can interrupt the STAMBP-Ub-NALP7 interaction. |
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V106257 | T20-M | T20-M is a leader peptide with good binding affinity to UBE2C. | |
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V88630 | TNG348 | 2839740-79-1 | TNG348 is an orally active inhibitor of the deubiquitinase USP1 for investigation in BRCA1/2 mutant or HRD+ cancers. |
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V88640 | UCHL1-IN-1 | UCHL1-IN-1 (Compound 46) is a ubiquitin C-terminal hydrolase L1 (UCHL1) inhibitor with IC50 of 5.1 μM. | |
|
V101173 | USP1-IN-10 | 2857051-98-8 | USP1-IN-10 (Compound 2) is a potent tricyclic USP1 inhibitor with IC50 of 7.6 nM. |
|
V51243 | USP1-IN-3 | 2821749-58-8 | USP1 inhibitor |
|
V35154 | USP1-IN-4 | 2878441-72-4 | USP1-IN-4 (compound 10) is a USP1 inhibitor (antagonist) with IC50 of 2.44 nM. |
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V54457 | USP1-IN-5 | 2925547-94-8 | USP1-IN-5 (compound 10) is a USP1 inhibitor (IC50<50 nM). |
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V54458 | USP1-IN-6 | 2925547-95-9 | USP1-IN-6 (compound 11) is a USP1 inhibitor (IC50<50 nM). |
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V88636 | USP1-IN-7 | 3033480-42-8 | USP1-IN-7 (Compound 3) is an inhibitor of ubiquitin-specific peptidase 1 (USP1) and its cofactor UAF1 with IC50≤50 nM. |
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