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Home >> Signaling Pathways >> DNA Damage/DNA Repair >> Deubiquitinase

Deubiquitinase

Deubiquitinases (DUBs) 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 thecellular 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. DUBs play several roles in the ubiquitin pathway. One of the best characterised functions of DUBs is the removal of monoubiqutin and polyubiquitin chainsfrom proteins.

Targets for  Deubiquitinase

Products for  Deubiquitinase

  1. Cat.No. Product Name Information
  2. GC39625 6RK73 6RK73 is a covalent irreversible and specific UCHL1 inhibitor with an IC50 of 0.23 ?M. 6RK73 shows almost no inhibition of UCHL3 (IC50=236 ?M). 6RK73 specifically inhibit UCHL1 activity in breast cancer. 6RK73 Chemical Structure
  3. GC13035 Bay 11-7821

    A selective and irreversible NF-κB inhibitor

     Bay 11-7821 Chemical Structure
  4. GC65259 BC-1471 BC-1471 is a STAM-binding protein (STAMBP) deubiquitinase inhibitor. BC-1471 Chemical Structure
  5. GC13892 C527 Inhibitor of USP1/USF1 complex C527 Chemical Structure
  6. GC67886 DC-U4106 DC-U4106 Chemical Structure
  7. GC35906 DUBs-IN-1 DUBs-IN-1 is an active inhibitor of ubiquitin-specific proteases (USPs), with an IC50 of 0.85 μM for USP8. DUBs-IN-1 Chemical Structure
  8. GC17125 DUBs-IN-2 DUBs-IN-2 is a potent deubiquitinase inhibitor with an IC50 of 0.28 μM for USP8. DUBs-IN-2 Chemical Structure
  9. GC10356 DUBs-IN-3 DUBs-IN-3 is a potent deubiquitinase (USP) enzyme inhibitor extracted from reference compound 22c with an IC50 of 0.56 μM for USP8. DUBs-IN-3 Chemical Structure
  10. GC34083 EOAI3402143 EOAI3402143 is a deubiquitinase (DUB) inhibitor, which inhibits dose-dependently inhibits Usp9x/Usp24 and Usp5. EOAI3402143 Chemical Structure
  11. GC62979 FT206 FT206 is an inhibitor of carboxamides as ubiquitin-specific protrase extracted from patent WO 2020033707 A1, example 11-1. FT206 Chemical Structure
  12. GC67915 FT3967385 FT3967385 Chemical Structure
  13. GC32786 FT671 FT671 is a potent, non-covalent and selective USP7 inhibitor with an IC50 of 52 nM and binds to the USP7 catalytic domain with a Kd of 65 nM. FT671 Chemical Structure
  14. GC69134 FT709

    FT709 is an effective selective inhibitor of USP9X with an IC50 value of 82 nM. USP9X is involved in centrosome function, chromosome alignment during mitosis, EGF receptor degradation, chemical sensitization and circadian rhythms.

     FT709 Chemical Structure
  15. GC32917 FT827 FT827 is a selective and covalent ubiquitin-specific protease 7 (USP7) inhibitor (Ki=4.2 ?M). FT827 binds to the USP7 catalytic domain (USP7CD; residues 208-560) with an apparent Kd value of 7.8 ?M. FT827 Chemical Structure
  16. GC32856 GNE-6640 An inhibitor of USP7 GNE-6640 Chemical Structure
  17. GC32727 GNE-6776 GNE-6776 is a selective and orally bioavailable USP7 inhibitor. GNE-6776 Chemical Structure
  18. GC39172 GRL0617 A SARS-CoV and SARS-CoV-2 PLpro inhibitor GRL0617 Chemical Structure
  19. GC34354 GSK2643943A GSK2643943A is a deubiquitinating enzyme (DUB) inhibitor targeting USP20. GSK2643943A has affinity with an IC50 of 160 nM for USP20/Ub-Rho. GSK2643943A has anti-tumor efficacy and can be used for the research of oral squamous cell carcinoma (OSCC) . GSK2643943A Chemical Structure
  20. GC36211 HBX 19818 HBX 19818 is a specific inhibitor of ubiquitin-specific protease 7 (USP7), with an IC50 of 28.1 μM. HBX 19818 Chemical Structure
  21. GC14797 IU1 A deubiquitinating enzyme inhibitor IU1 Chemical Structure
  22. GC63027 IU1-248 IU1-248, a derivative of IU1, is a potent and selective USP14 inhibitor with an IC50 of 0.83?μM. IU1-248 Chemical Structure
  23. GC64956 IU1-47 IU1-47 is a potent and specific USP14 inhibitor with an IC50 of 0.6 μM. IU1-47 Chemical Structure
  24. GC62460 LCAHA LCAHA (LCA hydroxyamide) is a deubiquitinase USP2a inhibitor with IC50s of 9.7 μM and 3.7μM in Ub-AMC Assay and Di-Ub Assay, respectively. LCAHA destabilizes Cyclin D1 and induces G0/G1 arrest by inhibiting deubiquitinase USP2a. LCAHA Chemical Structure
  25. GC10510 LDN 57444 An inhibitor of UCH-L1 LDN 57444 Chemical Structure
  26. GC60981 LDN-91946 LDN-91946 is a potent, selective and uncompetitive ubiquitin C-terminal hydrolase-L1 (UCH-L1) inhibitor with a Ki app of 2.8 μM. LDN-91946 Chemical Structure
  27. GC34670 MF-094 MF-094 is a potent and selective USP30 inhibitor with an IC50 of 120 nM. MF-094 increases protein ubiquitination and accelerates mitophagy. MF-094 Chemical Structure
  28. GC17635 ML-323 USP1-UAF1 inhibitor ML-323 Chemical Structure
  29. GC32720 ML364 An inhibitor of USP2 ML364 Chemical Structure
  30. GC12475 NSC 632839 hydrochloride A deubiquitylase and deSUMOylase inhibitor NSC 632839 hydrochloride Chemical Structure
  31. GC15503 NSC 687852 (b-AP15) An inhibitor of the deubiquitinases USP14 and UCHL5 NSC 687852 (b-AP15) Chemical Structure
  32. GC69637 OTUB1/USP8-IN-1

    OTUB1/USP8-IN-1 is an effective dual inhibitor of OTUB1 and USP8, with IC50 values of 0.17 and 0.28 nM, respectively. It can be used for cancer research.

     OTUB1/USP8-IN-1 Chemical Structure
  33. GC10379 P 22077 P 22077 Chemical Structure
  34. GC12067 P005091 A selective inhibitor of ubiquitin-specific protease 7 P005091 Chemical Structure
  35. GC13208 PR-619 PR-619 is a broad-spectrum DUB (deubiquitinating enzyme) inhibitor. PR-619 has demonstrated robust DUB inhibitory activity (5-20 µM) and growth inhibitory activity with IC50 of 2 µM in HEK 293T cells.. PR-619 Chemical Structure
  36. GC60317 RA-9 RA-9 is a potent and selective proteasome-associated deubiquitinating enzymes (DUBs) inhibitor with favorable toxicity profile and anticancer activity. RA-9 blocks ubiquitin-dependent protein degradation without impacting 20S proteasome proteolytic activity. RA-9 selectively induces onset of apoptosis in ovarian cancer cell lines and primary cultures derived from donors. RA-9 induces endoplasmic reticulum (ER)-stress responses in ovarian cancer cells. RA-9 Chemical Structure
  37. GC17698 SJB2-043 An inhibitor of the USP1-UAF1 complex and SARS-CoV-2 PLpro SJB2-043 Chemical Structure
  38. GC13401 SJB3-019A Usp1 inhibitor SJB3-019A Chemical Structure
  39. GC67712 STAMBP-IN-1 STAMBP-IN-1 Chemical Structure
  40. GC62509 STD1T STD1T is a deubiquitinase USP2a inhibitor with an IC50 of 3.3 μM in Ub-AMC Assay. STD1T Chemical Structure
  41. GC13013 TCID UCHL3 inhibitor, cell-permeable TCID Chemical Structure
  42. GC14366 Thioguanine A thiopurine analog Thioguanine Chemical Structure
  43. GC70098 USP1-IN-2

    USP1-IN-2 (Compound I-193) is an effective inhibitor of USP1 with an IC50 less than 50 nM.

     USP1-IN-2 Chemical Structure
  44. GC67963 USP15-IN-1 USP15-IN-1 Chemical Structure
  45. GC38043 USP25/28 inhibitor AZ1 USP25/28 inhibitor AZ1 (AZ1) is an orally active, selective, noncompetitive, dual ubiquitin specific protease (USP) 25/28 inhibitor with IC50s of 0.7 μM and 0.6 μM, respectively USP25/28 inhibitor AZ1 Chemical Structure
  46. GC70099 USP30 inhibitor 11

    USP30 inhibitor 11 is a selective and effective inhibitor of USP30, with an IC50 value of 0.01 µμ. It is Example 83 derived from patent document WO2017009650A1, used for research on cancer and diseases involving mitochondrial dysfunction.

     USP30 inhibitor 11 Chemical Structure
  47. GC62410 USP30 inhibitor 18 USP30 inhibitor 18 is a selective USP30 inhibitor with an IC50 of 0.02 μM. USP30 inhibitor 18 increases protein ubiquitination and accelerates mitophagy. USP30 inhibitor 18 Chemical Structure
  48. GC66438 USP5-IN-1 USP5-IN-1 (compound 64), a potent deubiquitinase USP5 inhibitor, binds to the USP5 ZnF-UBD with a KD of 2.8 μM. USP5-IN-1 is selective over nine proteins containing structurally similar ZnF-UBD domains. USP5-IN-1 inhibits the USP5 catalytic cleavage of a di-ubiquitin substrate. USP5-IN-1 Chemical Structure
  49. GC37875 USP7-IN-1 USP7-IN-1 is a selective and reversible inhibitor of ubiquitin-specific protease 7 (USP7), with an IC50 of 77 μM, and can be used for the research of cancer. USP7-IN-1 Chemical Structure
  50. GC70100 USP7-IN-11

    USP7-IN-11 is an effective inhibitor of ubiquitin-specific protease 7 (USP7) (Deubiquitinase), with an IC50 of 0.37 nM. USP7-IN-11 has anti-cancer properties (WO2022048498A1; Example 187).

     USP7-IN-11 Chemical Structure
  51. GC65275 USP7-IN-3 USP7-IN-3 (Compound 5) is a potent and selective allosteric ubiquitin-specific protease 7 (USP7) inhibitor. USP7-IN-3 Chemical Structure
  52. GC70101 USP7-IN-7

    USP7-IN-7 (compound 124) is a USP7 inhibitor with an IC50 value of <10 nM. It has low nanomolar cell toxicity against p53 mutant cancer cell lines, p53 wild-type blood tumors, and neuroblastoma cell lines. USP7-IN-7 can be used for tumor research.

     USP7-IN-7 Chemical Structure
  53. GC62377 USP7-IN-8 USP7-IN-8 (example 81) is a selective ubiquitin-specific protease 7 (USP7) inhibitor with an IC50 of 1.4 μM in an Ub-Rho110 assay. USP7-IN-8 shows no activity against USP47 and USP5. USP7-IN-8 has anticancer effects. USP7-IN-8 Chemical Structure
  54. GC70102 USP7-IN-9

    USP7-IN-9 is an efficient inhibitor of USP7 with an IC50 of 40.8 nM. It can induce apoptosis in RS4;11 cells and block the cell cycle at G0/G1 and S phase. USP7-IN-9 reduces the levels of cancer proteins MDM2 and DNMT1, while increasing the levels of tumor suppressor proteins p53 and p21.

     USP7-IN-9 Chemical Structure
  55. GC18160 USP7/USP47 inhibitor

    ?A selective inhibitor of USP7/USP47

     USP7/USP47 inhibitor Chemical Structure
  56. GC64537 USP8-IN-1 USP8-IN-1 is a USP8 inhibitor with an IC50 of 1.9 μM. USP8-IN-1 inhibits H1975 cell growth with a GI50 of 82.04 μM (CN111138358A; U10). USP8-IN-1 Chemical Structure
  57. GC70103 USP8-IN-3

    USP8-IN-3 (Compd U51) is a deubiquitinase USP8 inhibitor with an IC50 value of 4.0 μM. USP8-IN-3 also inhibits the proliferation of GH3 and H1957 cells, with GI50 values of 37.03 μM and 6.01 μM, respectively.

     USP8-IN-3 Chemical Structure
  58. GC19378 VLX1570 VLX1570, an analogue of b-AP15, is a competitive inhibitor of deubiquitinase activity, with an IC50 of appr 10 uM. VLX1570 Chemical Structure
  59. GC10970 WP1130 WP1130 (WP1130) is a cell-permeable deubiquitinase (DUB) inhibitor, directly inhibiting DUB activity of USP9x, USP5, USP14, and UCH37. WP1130 has been shown to downregulate the antiapoptotic proteins Bcr-Abl and JAK2. WP1130 Chemical Structure
  60. GC62517 XL177A XL177A is a highly potent and selective irreversible USP7 inhibitor with an IC50 of 0.34?nM. XL177A elicits cancer cell killing through a p53-dependent mechanism. XL177A Chemical Structure

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