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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

    BAY 11-7082

     Bay 11-7821(BAY 11-7082) is an inhibitor of IκBα phosphorylation and NF-κB, selectively and irreversibly inhibits TNF-α-induced IκB-α phosphorylation (IC50 value is approximately 10μM), and reduces the expression of NF-κB and adhesion molecules. Bay 11-7821 inhibits ubiquitin-specific proteases USP7 and USP21 with IC50 values of 0.19 and 0.96μM, respectively . Bay 11-7821 Chemical Structure
  4. GC68740 BAY-728

    BAY-728 can be used as a negative control for BAY-805. BAY-805 is an effective selective inhibitor of USP21.

     BAY-728 Chemical Structure
  5. GC68742 BAY-805

    BAY-805 is a selective inhibitor of the ubiquitin-specific protease USP21. BAY-805 has high selectivity for deubiquitinating enzyme (DUB) targets, kinases, proteases, and other common off-target enzymes.

     BAY-805 Chemical Structure
  6. GC65259 BC-1471 BC-1471 is a STAM-binding protein (STAMBP) deubiquitinase inhibitor. BC-1471 Chemical Structure
  7. GC13892 C527 Inhibitor of USP1/USF1 complex C527 Chemical Structure
  8. GC67886 DC-U4106 DC-U4106 Chemical Structure
  9. 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
  10. 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
  11. 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
  12. GC34083 EOAI3402143 EOAI3402143 is a deubiquitinase (DUB) inhibitor, which inhibits dose-dependently inhibits Usp9x/Usp24 and Usp5. EOAI3402143 Chemical Structure
  13. GC62979 FT206 FT206 is an inhibitor of carboxamides as ubiquitin-specific protrase extracted from patent WO 2020033707 A1, example 11-1. FT206 Chemical Structure
  14. GC67915 FT3967385

    FT385

     FT3967385 Chemical Structure
  15. GC32786 FT671 FT671 is a potent and selective inhibitor of ubiquitin-specific protease 7 (USP7) with an IC50 value of 52nM. FT671 Chemical Structure
  16. 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
  17. 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
  18. GC73465 GK13S G13KS is a deubiquitinase UCHL1 ligand and inhibitor. GK13S Chemical Structure
  19. GC71305 GK16S GK16S is a UCHL1 chemogenomic probe. GK16S Chemical Structure
  20. GC32856 GNE-6640 An inhibitor of USP7 GNE-6640 Chemical Structure
  21. GC32727 GNE-6776 GNE-6776 is a selective and orally bioavailable USP7 inhibitor. GNE-6776 Chemical Structure
  22. GC39172 GRL0617 A SARS-CoV and SARS-CoV-2 PLpro inhibitor GRL0617 Chemical Structure
  23. 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
  24. 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
  25. GC69249 I-138

    I-138 is an orally effective compound structurally related to ML323. I-138 and ML323 are potent USP1-UAF1 reversible inhibitors. I-138 displays synergistic binding with ubiquitin and mutually exclusive binding with ML323. I-138 induces mono-ubiquitination of FANCD2 and PCNA in MDA-MB-436 cells, increasing mono-ubiquitination of PCNA and FANCD2 in HAP-1 USP1 WT cells. I-138 eliminates self-cleavage of USP1 in cells.

     I-138 Chemical Structure
  26. GC14797 IU1

    Usp14 inhibitor

     IU1 is a cytopermeable, reversible selective inhibitor of proteasome with an IC50 of 4.7μM for USP14. IU1 Chemical Structure
  27. 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
  28. GC64956 IU1-47 IU1-47 is a potent and specific USP14 inhibitor with an IC50 of 0.6 μM. IU1-47 Chemical Structure
  29. GC62460 LCAHA

    LCA hydroxyamide

     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
  30. GC10510 LDN 57444

    Ubiquitin C-terminal Hydrolase L1 Inhibitor, UCHL1 Inhibitor

     An inhibitor of UCH-L1 LDN 57444 Chemical Structure
  31. 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
  32. 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
  33. GC17635 ML-323 USP1-UAF1 inhibitor ML-323 Chemical Structure
  34. GC32720 ML364 An inhibitor of USP2 ML364 Chemical Structure
  35. GC12475 NSC 632839 hydrochloride

    F6, Ubiquitin Isopeptidase Inhibitor II

     A deubiquitylase and deSUMOylase inhibitor NSC 632839 hydrochloride Chemical Structure
  36. GC15503 NSC 687852 (b-AP15)

    b-AP15

     An inhibitor of the deubiquitinases USP14 and UCHL5 NSC 687852 (b-AP15) Chemical Structure
  37. 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
  38. GC73354 OTUB1/USP8-IN-1 TFA OTUB1/USP8-IN-1 TFA is the TFA salt form of OTUB1/USP8-IN-1. OTUB1/USP8-IN-1 TFA Chemical Structure
  39. GC71471 OTUB2-IN-1 OTUB2-IN-1, a specific inhibitor of OTUB2 (KD: ~12 μM), reduces PD-L1 protein expression in tumor cells and inhibits tumor growth by promoting robust intra-tumor infiltration of cytotoxic T lymphocytes (CTL) . OTUB2-IN-1 Chemical Structure
  40. GC10379 P 22077 P 22077 Chemical Structure
  41. GC12067 P005091

    P005091,P5091

     P005091 is a potent and selective ubiquitin-specific proteinase 7 (USP7) inhibitor with an EC50 value of 4.2 μM. P005091 Chemical Structure
  42. 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
  43. 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
  44. GC17698 SJB2-043 An inhibitor of the USP1-UAF1 complex and SARS-CoV-2 PLpro SJB2-043 Chemical Structure
  45. GC13401 SJB3-019A Usp1 inhibitor SJB3-019A Chemical Structure
  46. GC67712 STAMBP-IN-1 STAMBP-IN-1 Chemical Structure
  47. GC62509 STD1T STD1T is a deubiquitinase USP2a inhibitor with an IC50 of 3.3 μM in Ub-AMC Assay. STD1T Chemical Structure
  48. GC13013 TCID

    UCH-L3 Inhibitor

     UCHL3 inhibitor, cell-permeable TCID Chemical Structure
  49. GC14366 Thioguanine

    NSC 752, NSC 76504, 6TG

     A thiopurine analog Thioguanine Chemical Structure
  50. GC73166 U7D-1 U7D-1 is a first-in-class potent and selective USP7 (ubiquitin-specific protease 7) PROTAC degrader, with a DC50 of 33 nM in RS4;11 cells. U7D-1 Chemical Structure
  51. GC73948 UCHL1-IN-1 UCHL1-IN-1 (Compound 46) is an inhibitor for Ubiquitin C-terminal drolase L1 (UCHL1), with an IC50 of 5.1 μM. UCHL1-IN-1 Chemical Structure
  52. 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
  53. GC73156 USP1-IN-3 USP1-IN-3 is a selective USPI inhibitor. USP1-IN-3 Chemical Structure
  54. GC67963 USP15-IN-1 USP15-IN-1 Chemical Structure
  55. GC38043 USP25/28 inhibitor AZ1

    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
  56. GC73221 USP28-IN-3 USP28-IN-3 is a USP28 inhibitor (IC50=0.1 μM) with high selectivity over USP2, USP7, USP8, USP9x, UCHL3 and UCHL5. USP28-IN-3 Chemical Structure
  57. GC73222 USP28-IN-4 USP28-IN-4 is a USP28 inhibitor (IC50=0.04 μM) with high selectivity over USP2, USP7, USP8, USP9x, UCHL3 and UCHL5. USP28-IN-4 Chemical Structure
  58. 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
  59. 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
  60. 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
  61. 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
  62. GC73177 USP7-IN-10 hydrochloride USP7-IN-10 drochloride (compound 1) is a potent ubiquitin-specific protease 7 (USP7) inhibitor, with an IC50 of 13.39 nM. USP7-IN-10 hydrochloride Chemical Structure
  63. 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
  64. GC73882 USP7-IN-13 USP7-IN-13 (Compound 101) is a USP7 inhibitor with an IC50 value of 0.2-1 μM, which can be used for the study of multiple myeloma. USP7-IN-13 Chemical Structure
  65. 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
  66. 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
  67. 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
  68. 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
  69. GC18160 USP7/USP47 inhibitor

    ?A selective inhibitor of USP7/USP47

     USP7/USP47 inhibitor Chemical Structure
  70. 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
  71. GC73283 USP8-IN-2 USP8-IN-2 (Compd U52) is a deubiquitinase USP8 inhibitor with an IC50 value of 6.0 μM. USP8-IN-2 Chemical Structure
  72. 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
  73. 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
  74. GC10970 WP1130

    WP 1130; WP-1130

     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
  75. GC72934 XL 188 XL 188 is a potent and selective USP7 inhibitor with IC50 values of 90 nM and 193 nM for USP7 full-length and catalytic domain enzyme, respectively. XL 188 Chemical Structure
  76. 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
  77. GC73774 YCH2823 YCH2823 is an inhibitor of USP7 (IC50 = 49.6 nM; Kd = 0.117 μM). YCH2823 Chemical Structure

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