| 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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