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You are here:Home-Inhibitors & Agonists-Proteasome/Ubiquitin-Deubiquitinase (DUB)

Request The Product List ofDeubiquitinase (DUB) Deubiquitinase (DUB)

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.

Cat. No. Product Name CAS No. Information
GY02966

ML364

1991986-30-1

A potent, selective, reversible deubiquitinase USP2 inhibitor with IC50 of 1.1 uM in biochemical assay; also inhibits USP8 (IC50=0.95 uM), shows no against caspase 6/7, MMP1, MMP9 and USP15 and a panel of 102 kinase; increases cellular cyclin D1 degradation and causes cell cycle arrest and shows antiproliferative in cancer cell lines; also decreases homologous recombination-mediated DNA repair.

GY02670

NSC632839

157654-67-6

A small molecule inhibitor of ubiquitin-proteasome system by inhibiting the ubiquitin isopeptidases; induce a unique apoptotic pathway, which includes a Bcl-2-dependent but apoptosome-independent mitochondrial pathway with up-regulation of the BH3-only protein Noxa, stabilization of the IAP antagonist Smac, but also the involvement of the death receptor pathway.

GY02554

VLX1570

1431280-51-1

VLX1570 is a small molecule b-AP15 analog that fucttion as proteasome deubiquitinase inhibitor with IC50 of 10 uM, interacts at the active sites of the proteasome DUBs USP14 and UCHL5; demonstrates cytotoxicity in survival assays in HCT116 colon cancer cells with IC50 of 0.58 uM, shows no inhibitory activity on a panel of recombinant non-proteasome DUBs, recombinant kinases, or caspase-3; decreases cell viability in chemotherapy resistant endometrial cancer cells consistent with cell cycle arrest and caspase-3 mediated apoptosis; decreases tumor burden and prolongs survival in WM-xenografted mice.

GY02540

HBX 19818

1426944-49-1

HBX-19818 is a potent, selective USP7 inhibitor with IC50 of 28.1 uM; exhibits high selectivity over other USP members, such as USP8, USP5, USP2, and USP20 (IC50 >200 uM), and no activity against UCH-L1, UCH-L3 and SENP1; reduces HCT116 cell proliferation, induces caspase activity and PARP cleavage, and arrests HCT116 cancer cells in G1.

GY02469

USP7-IN-1

1381291-36-6

A novel selective and reversible inhibitor of USP7 with IC50 of 33 uM; shows less or no inhibition on USP5, USP8, Uch-L1, Uch-L3 and Caspase (IC50>200 uM); HCT116 cell viability GI50 is 67 uM.

GY07087

GNE-6776

2009273-71-4

GNE-6776 is a novel potent, specific, non-covalent, orally bioavailable USP7 inhibitor with IC50 of 1.34 uM ; dislpalys selectivity over USP47 and USP5 (>200 uM); promotes endogenous MDM2 ubiquitination, stabilized p53 and upregulated p21, induces tumour cell death and enhances cytotoxicity with chemotherapeutic agents; promotes on-target pathway modulation in human xenografts.

GY07086

FT-671

1959551-26-8

FT-671 is a novel potent, specific, non-covalent USP7 inhibitor with Kd of 65 nM (USP7 catalytic domain); inhibits USP7 with IC50 values of 52 nM (USP7 CD) and 69 nM (USP7C-term), display good USP7 selectivity in a panel of 38 deubiquitinases (DUBs); destabilizes USP7 substrates including MDM2, increases levels of p53, and results in the transcription of p53 target genes and induces tumour suppressor p21; blocks the proliferation of MM.1S cells (IC50=33 nM), suppresses tumour growth in mice; orally available.

GY07085

FT-827

1959537-86-0

FT-827 is a novel potent, specific, covalent USP7 inhibitor with Kd of 7.8 uM (USP7 catalytic domain); modifies the catalytic Cys223 of USP7 and inhibits the enzyme with kinact/Ki of 66 M-1s-1, display good USP7 selectivity in a panel of 38 deubiquitinases (DUBs)

GY07075

GNE-6640

2009273-67-8

GNE-6640 (GNE6640) is a potent, selective USP7 inhibitor with IC50 of 0.75 uM; dislpalys selectivity over USP47 and USP5 (IC50>200 uM); promotes endogenous MDM2 ubiquitination, stabilized p53 and upregulated p21, induces tumour cell death and enhances cytotoxicity with chemotherapeutic agents and targeted compounds, including PIM kinase inhibitors; decreased viability of 108 cell lines with IC50 <10 uM.

GY10098

IU1-248

IU1-248 (USP14 inhibitor IU1-248) is a potent, selective USP14 inhibitor with IC50 of 0.83 uM, IU1-248 is an IU1 derivative that is 10-fold more potent than IU1; exhibits 25-fold selectivity over USP5 (IsoT).

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