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DUB

DUB

Deubiquitinases (DUBs) are a family of proteases whose job it is to separate proproteins or ubiquitin(s) conjugated with target substrate from ubiquitin (Ub) or ubiquitin-like proteins. According to their enzymatic cleavage mechanism, DUBs can be classified into two main 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 modification known as ubiquitination is essential for many crucial cellular 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 pathologies, including cancer. DUBs are fresh candidates for the development of drugs that are target-directed.

DUB related products

Structure Cat No. Product Name CAS No. Product Description
AZ1 V8466 AZ1 2165322-94-9 AZ1 is a novel and potent dual inhibitor of the USP25/28 deubiquitinating enzyme subfamily with potential anticancer activity.
b-AP15 (NSC 687852) V1329 b-AP15 (NSC 687852) 1009817-63-3 b-AP15 (formerly known as NSC687852; b-AP15; USP14 Inhibitor III; b-AP-15;NSC-687852)is a novel, potent and specific deubiquitinase (DUB) inhibitor of 19S proteasomes activity of Ub-AMC cleavage with potential antineoplastic activity.
EOAI3402143 V25341 EOAI3402143 1699750-95-2 EOAI3402143 (EOAI 3402143; EOAI-3402143) is a novel and potent inhibitor of Usp9x, Usp24 and deubiquitinase(DUB) with potential anticancer activity.
GNE-6776 V3028 GNE-6776 2009273-71-4 GNE-6776 (GNE6776) is anovel, highly potent, specific, non-covalent, and orally bioavailable USP7 (Ubiquitin specific proteases7) inhibitor with anticancer activity.
GSK2643943A V3964 GSK2643943A GSK2643943A is a novel and potent inhibitor of deubiquitylating enzyme(DUB)with anIC50of 160 nM for USP20/Ub-Rho.
IU1 V1324 IU1 314245-33-5 IU1 (IU-1; IU 1) is a cell-permeable, reversible and selective proteasome inhibitor of human USP14 with the potential to be used for treatingneurodegenerative disease.
IU1-47 V22779 IU1-47 670270-31-2 IU1-47 is a potent and specific USP14 inhibitor (antagonist) with IC50 of 0.6 μM.
LDN-57444 V1326 LDN-57444 668467-91-2 LDN-57444 (LDN57444; LDN 57444) is a potent, reversible, and competitive proteasome inhibitor for Uch-L1 (ubiquitin C-terminal hydrolase-L1) with the potential to treat PD-Parkinsons disease.
ML323 V1330 ML323 1572414-83-5 ML323 (ML-323; ML 323) is a novel, potent and highly selective USP1-UAF1 inhibitor with potential antitumor activity.
ML364 V2858 ML364 1991986-30-1 ML364 is asmall molecule inhibitor of ubiquitin specific peptidase 2 (USP2, a deubiquitinase) with an IC50of 1.1 μm in a biochemical assay.
NSC632839 V3231 NSC632839 157654-67-6 NSC632839 is a nonselective isopeptidase inhibitor that inhibitsUSP2,USP7, andSENP2withEC50values of 45±4 μM, 37±1 μM, and 9.8±1.8 μM, respectively.
NSC632839 HCl V3232 NSC632839 HCl 157654-67-6 NSC632839 is a nonselective isopeptidase inhibitor that inhibitsUSP2,USP7, andSENP2withEC50values of 45±4 μM, 37±1 μM, and 9.8±1.8 μM, respectively.
P22077 V1328 P22077 1247819-59-5 P22077 (P-22077; P 22077) isa potent,cell-permeable and selectiveinhibitor of ubiquitin-specific protease USP7 (ubiquitin-specific protease 7) with potential antitumor activity.
P5091 (P005091) V1323 P5091 (P005091) 882257-11-6 P5091 (also called P5091;P-005091;P-5091; P005091) is a novel, potent,specific and selective inhibitor of ubiquitin-specific protease 7 (USP7) with potential anticancer activity.
PLpro inhibitor V33931 PLpro inhibitor 1093070-14-4 PLpro inhibitor is a papin-like protease (PLpro) inhibitor (antagonist) with IC50 of 2.6 µM.
PR-619 V1322 PR-619 2645-32-1 PR-619 (PR619; PR 619) is a novel, cell-permeable, non-selective and reversible inhibitor of the deubiquitinylating enzymes (DUBs) with potential antineoplastic activity.
RA-9 UPS inhibitor V2165 RA-9 UPS inhibitor 919091-63-7 RA-9 is a cell permeable and potent inhibitor of the ubiquitin-proteasome system (UPS).
SJB2-043 V14847 SJB2-043 63388-44-3 SJB2-043, a C527 analog, is a novel and potent inhibitor of USP1/UAF1(ubiquitin-specific protease 1/Usp1-associated Factor 1)complex with IC50 of 544 nM.
TCID V1325 TCID 30675-13-9 TCID (4,5,6,7-tetrachloro-1H-indene-1,3(2H)-dione) is a novel and potent DUB (deubiquitinylating enzymes) inhibitor that inhibits ubiquitin C-terminal hydrolase L3 with an IC50 of 0.6 μM.
VLX1570 V2787 VLX1570 1431280-51-1 VLX1570 is a competitive inhibitor of the 19S proteasome-specific DUB (deubiquitylating enzymes) activity with IC50 ranging from 4.2 uM to 8.6 uM.
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