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.


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USP7-IN-11

USP7-IN-11 is a potent ubiquitin-specific protease 7 (USP7) (Deubiquitinase) inhibitor with an IC50 of 0.37 nM. USP7-IN-11 has anticancer effects (WO2022048498A1; Example 187)[1].

  • CAS Number: 2763872-32-6
  • MF: C29H27ClN6O2S
  • MW: 559.08
  • Catalog: Deubiquitinase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

SJB2-043

SJB2-043 is an inhibitor of the native USP1/UAF1 complex with IC50 of 544 nM.

  • CAS Number: 63388-44-3
  • MF: C17H9NO3
  • MW: 275.258
  • Catalog: Deubiquitinase
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: 495.0±48.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 253.2±29.6 °C

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[1].

  • CAS Number: 117094-40-3
  • MF: C24H41NO3
  • MW: 391.59
  • Catalog: Deubiquitinase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

USP30 inhibitor 11

USP30 inhibitor 11 is a selective and potent ubiquitin specific peptidase 30 (USP30) inhibitor with an IC50 of 0.01 µΜ, the example 83 extracted from patent WO2017009650A1. USP30 inhibitor 11 is used for the study of cancer and conditions involving mitochondrial dysfunction[1].

  • CAS Number: 2067332-64-1
  • MF: C17H16N6O2S
  • MW: 368.41
  • Catalog: Deubiquitinase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

USP1-IN-5

USP1-IN-5 (compound 10) is a USP1 inhibitor (IC50<50 nM). USP1-IN-5 also inhibits MDA-MB-436 cells with IC50 <50 nM[1].

  • CAS Number: 2925547-94-8
  • MF: C27H23F3N8O
  • MW: 532.52
  • Catalog: Deubiquitinase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

USP1-IN-2

USP1-IN-2 (Compound I-193) is a potent ubiquitin-specific protease 1 (USP1) inhibitor with an IC50 of less than about 50 nM[1].

  • CAS Number: 2098212-05-4
  • MF: C26H22F4N6O
  • MW: 510.49
  • Catalog: Deubiquitinase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

IU1-248

IU1-248, a derivative of IU1, is a potent and selective USP14 inhibitor with an IC50 of 0.83 μM.

  • CAS Number: 2307472-03-1
  • MF: C20H23N3O2
  • MW: 337.42
  • Catalog: Deubiquitinase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

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[1].

  • CAS Number: 2242582-40-5
  • MF: C26H28FN3O4S
  • MW: 497.58
  • Catalog: Deubiquitinase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

GNE-6776

GNE-6776 is a selective USP7 inhibitor.

  • CAS Number: 2009273-71-4
  • MF: C20H20N4O2
  • MW: 348.4
  • Catalog: Deubiquitinase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

TCID

TCID (4,5,6,7-Tetrachloroindan-1,3-dione) is a potent and selective neuronal ubiquitin C-terminal hydrolase (UCH-L3) inhibitor with an IC50 of 0.6 μM[1]. TCID diminishes glycine transporter GlyT2 ubiquitination in brainstem and spinal cord primary neurons[2].

  • CAS Number: 30675-13-9
  • MF: C9H2Cl4O2
  • MW: 283.923
  • Catalog: Deubiquitinase
  • Density: 1.8±0.1 g/cm3
  • Boiling Point: 448.1±45.0 °C at 760 mmHg
  • Melting Point: 218-220ºC
  • Flash Point: 188.8±29.3 °C

Vialinin A

Vialinin A (Terrestrin A) is a p-terphenyl compound with antioxidant properties[1]. Vialinin A is a potent inhibitor of TNF-α, USP4, USP5, and sentrin/SUMO-specific protease 1 (SENP1). Vialinin A (Terrestrin A) can be used for autoimmune diseases and cancer research[2][3].

  • CAS Number: 858134-23-3
  • MF: C34H26O8
  • MW: 562.57
  • Catalog: Deubiquitinase
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: 846.9±65.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 277.1±27.8 °C

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.

  • CAS Number: 1381291-36-6
  • MF: C23H24ClN3O3
  • MW: 425.90800
  • Catalog: Deubiquitinase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

P 22077

P 22077 is a cell-permeable ubiquitin-specific protease 7 (USP7) inhibitor with an EC50 of 8.01 μM. It also inhibits USP47 with an EC50 of 8.74 μM.

  • CAS Number: 1247819-59-5
  • MF: C12H7F2NO3S2
  • MW: 315.31600
  • Catalog: Deubiquitinase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

DUB-IN-7

DUB-IN-7 (compound 43) is a Deubiquitinating enzymes (DUBs) inhibitor. DUB-IN-7 can be used in the study of diseases mediated by dysregulated JAK2 activity, such as leukemia[1].

  • CAS Number: 2894064-79-8
  • MF: C17H19N5O
  • MW: 309.37
  • Catalog: Deubiquitinase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

USP25 and 28 inhibitor AZ-1

USP25/28 inhibitor AZ1 (AZ1) is a potent, 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 reduces cell viability across a range of cancer cell lines[1].

  • CAS Number: 2165322-94-9
  • MF: C17H16BrF4NO2
  • MW: 422.21
  • Catalog: Deubiquitinase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

C527

C527 is a is a pan DUB enzyme inhibitor, with a high potency for the USP1/UAF1 complex (IC50=0.88 μM).

  • CAS Number: 192718-06-2
  • MF: C17H8FNO3
  • MW: 293.249
  • Catalog: Deubiquitinase
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: 488.6±47.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 249.3±29.3 °C

IMP-1710

IMP-1710 (IMP1710) is a potent, selective, covalent UCHL1 inhibitor with IC50 of 38 nM.IMP-1710 demonstrated exquisite selectivity in a cross-screening against 20 DUBs.IMP-1710 can profile activity of endogenous UCHL1 with excellent selectivity in cell types including endothelial cells (EA.hy926) and adenocarcinoma human alveolar basal epithelial cells (A549).IMP-1710 demonstrated >50% fibroblast–myofibroblast transition (FMT) inhibition (IC50=740 nM) in idiopathic pulmonary fibrosis (IPF), as well as αSMA inhibition.IMP-1710 is a powerful and selective probe to explore UCHL1 activity with potential application to substrate identification, mode of action studies, and cellular target profiling.

  • CAS Number: 2383117-96-0
  • MF: C23H19N5O
  • MW: 381.439
  • Catalog: Deubiquitinase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

NSC-632839

NSC632839 is a nonselective isopeptidase inhibitor, which inhibits USP2, USP7, and SENP2 with EC50s of 45±4 μM, 37±1 μM, and 9.8±1.8 μM, respectively.

  • CAS Number: 157654-67-6
  • MF: C21H22ClNO
  • MW: 339.858
  • Catalog: Deubiquitinase
  • Density: N/A
  • Boiling Point: 522.7ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 184ºC

P5091

P005091 is a selective and potent inhibitor of ubiquitin-specific protease 7 (USP7) with an EC50 of 4.2 μM.

  • CAS Number: 882257-11-6
  • MF: C12H7Cl2NO3S2
  • MW: 348.225
  • Catalog: Deubiquitinase
  • Density: 1.6±0.1 g/cm3
  • Boiling Point: 452.4±45.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 227.4±28.7 °C

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)[1].

  • CAS Number: 2477650-96-5
  • MF: C18H21N5O3S
  • MW: 387.46
  • Catalog: Deubiquitinase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

USP7/USP47 inhibitor

USP7/USP47 inhibitor is a selective ubiquitin-specific protease 7/47 (USP7/USP47) inhibitor, with EC50s of 0.42 μM and 1.0 μM, respectively.

  • CAS Number: 1247825-37-1
  • MF: C18H11Cl2N3O3S3
  • MW: 484.39900
  • Catalog: Deubiquitinase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

FT709

FT709 is a potent and selective USP9X inhibitor, an IC50 of 82 nM. USP9X has been linked with centrosome function, chromosome alignment during mitosis, EGF receptor degradation, chemo-sensitization, and circadian rhythms[1].

  • CAS Number: 2413991-74-7
  • MF: C23H22N4O7S
  • MW: 498.51
  • Catalog: Deubiquitinase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Acetamide, 2-[[3,4-dihydro-6-(4-morpholinyl)-4-oxo-3-(2-phenylethyl)-2-quinazolinyl]thio]-N-[(tetrahydro-2-furanyl)methyl]-

BC-1471 is a STAM-binding protein (STAMBP) deubiquitinase inhibitor. BC-1471 inhibits NALP7 (NACHT, LRR and PYD domains-containing protein 7) inflammasome activity[1].

  • CAS Number: 896683-84-4
  • MF: C27H32N4O4S
  • MW: 508.63
  • Catalog: Deubiquitinase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

STD1T

STD1T (USP2a inhibitor STD1T) is a hit-to-lead, small-molecule inhibitor of USP2a with IC50 of 3.3 uM in Ub-AMC assays, displays no activity against USP7 at 10 uM.

  • CAS Number: 893075-58-6
  • MF: C19H19N3O4S2
  • MW: 417.498
  • Catalog: Deubiquitinase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

LDN-57444

LDN-57444 is a reversible, competitive and site-directed inhibitor of ubiquitin C-terminal hydrolase L1 (UCH-L1), with an IC50 of 0.88 μM and a Ki of 0.40 μM; LDN-57444 also suppresses UCH-L3 activity, with an IC50 of 25 μM.

  • CAS Number: 668467-91-2
  • MF: C17H11Cl3N2O3
  • MW: 397.640
  • Catalog: Deubiquitinase
  • Density: 1.5±0.1 g/cm3
  • Boiling Point: 534.4±60.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 277.0±32.9 °C

USP7-IN-12

USP7-IN-12 (compound 1) is a potent and orally active Usp7 inhibitor with an IC50 value of 3.67 nM. USP7-IN-12 shows antiproliferative activity[1].

  • CAS Number: 2763698-01-5
  • MF: C29H28ClFN4O2S
  • MW: 551.07
  • Catalog: Deubiquitinase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

HBX 19818

HBX 19818 is a specific inhibitor of ubiquitin-specific protease 7 (USP7), with an IC50 of 28.1 μM.

  • CAS Number: 1426944-49-1
  • MF: C25H28ClN3O
  • MW: 421.962
  • Catalog: Deubiquitinase
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 631.2±55.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 335.6±31.5 °C

LDN 91946

LDN 91946 is a selective, uncompetitive ubiquitin C-terminal hydrolase-L1 (UCH-L1) inhibitor with Ki of 2.8 uM, exhibits no activity against other cysteine hydrolase (UCH-L3, TGase 2, papain and caspase-3).

  • CAS Number: 439946-22-2
  • MF: C17H12N6O
  • MW: 314.316
  • Catalog: Deubiquitinase
  • Density: 1.6±0.1 g/cm3
  • Boiling Point: 714.0±60.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 385.6±32.9 °C

GNE-6640

GNE-6640 is a selective and non-covalent inhibitor of ubiquitin epecific peptidase 7 (USP7), with IC50 values of 0.75 μM, 0.43 μM, 20.3 μM and 0.23 μM for full length USP7, USP7 catalytic domain, full length USP43 and Ub-MDM2, respectively.

  • CAS Number: 2009273-67-8
  • MF: C20H18N4O
  • MW: 330.38
  • Catalog: Deubiquitinase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

USP7-IN-10

USP7-IN-10 (compound 1) is a potent ubiquitin-specific protease 7 (USP7) inhibitor, with an IC50 of 13.39 nM[1].

  • CAS Number: 2755995-01-6
  • MF: C26H29ClN4O3S
  • MW: 513.05
  • Catalog: Deubiquitinase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A