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DUB

Deubiquitinating enzymes (DUBs), belonging to the superfamily of proteases, are a group of enzymes that catalyze the cleavage of ubiquitin from ubiquitin-linked molecules after the terminal carbonyl of the last residue of ubiquitin (Gly76). Based on the mechanism of catalysis, DUBs is divided into two classes, cysteine proteases, which interact with substrates through the thiol group of a cysteine in the active site, and metalloproteases, which form a noncovalent intermediate with the substrate through a Zn2+ bound polarized water molecule. The cysteine protease DUBs have different Ub-protease domains and hence are further divided into four subclasses, ubiquitin-specific protease (USP), ubiquitin C-terminal hydrolase (UCH), Otubain protease (OTU) and Machado-Joseph disease protease (MJD); while all metalloprotease DUBs have one Ub protease domain called JAMM (JAB1/MPN/Mov34 metalloenzyme).

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  1. Cat.No. Product Name Information
  2. A8693 C527 C527, also named heterocyclic tricyclic 1,4-dihydro-1,4-dioxo-1H-naphthalene, is an inhibitor of USP1 (deubiquitinating enzyme 1) / USF1 (USP1-associated factor 1) complex with IC50 value of 0.88 ± 0.03 μM in vivo.
  3. B4861 TZ9
  4. B5550 HBX 41108 New Product
  5. B3516 DUBs-IN-3
  6. B3515 DUBs-IN-2
  7. B3514 DUBs-IN-1
  8. B1307 SJB3-019A

    SJB3-019A is a potent and novel usp1 inhibitor. SJB3-019A (IC50 = 0.0781 uM) was 5 times more potent than SJB2-043 in promoting ID1 degradation and cytoxicity in K562 cells.

  9. B1317 ML-323 ML323 is a reversible, potent USP1-UAF1 inhibitor with IC50 of 76 nM in a Ub-Rho assay and 174 nM and 820 nM in orthogonal gel-based assays using K63-linked diubiquitin (di-Ub) and monoubiquitinated PCNA (Ub-PCNA) as substrates, respectively.
  10. B1096 USP7-USP47 inhibitor USP7/USP47 Inhibitor(P 22077)is a selective and dual inhibitor of human ubiquitin-specific proteases 7 (USP7) and 47(USP47) with EC50 values of 4.2±0.9μM and 4.3±0.8μM, respectively .
  11. A8323 WP1130 WP1130, also known as degrasyn, is a second-generation tyrphostin derivative initially identified as a Janus-activated kinase (JAK)-signal transducer and activator of transcription (STAT) pathway inhibitor that reduces STAT activation stimulated by cytokines (such as IL-6 and IL-3) through the rapid down-regulation of upstream JAK kinases. WP1130 has also been identified as a selective deubiquitinating enzyme (DUB) inhibitor that directly inhibits DUB activity of USP9x, USP5, USP14 and UCH37 leading to rapid accumulation of polyubiquitinated proteins into juxtanuclear aggresomes and tumor cell apoptosis. WP1130-induced apoptosis and anti-proliferation in tumor cells have been implicated in the treatment of chronic myelogenous leukemia (CML), melanoma, glioblastoma and myeloproliferative disorders.

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