| Cat. No. |
Product Name |
CAS No. |
Information |
| H9642 |
FT-385
|
|
FT385 (FT3967385) is a potent, selective USP30 inhibitor with biochemical IC50 of 1.5 nM;FT385 (FT3967385) displays high selectivity against a broad panel of USP enzymes, with one exception of plasma membrane-associated USP6.FT385 engages USP30 in cells at low nanomolar concentrations.Inhibition of USP30 via FT385 phenocopies USP30 KO in enhancing basal mitophagy and promoting ubiquitylation of TOM20 upon depolarisation, enhances phospho-Ser65 ubiquitin (pUb) levels on mitochondria of SHSY5Y cells. |
| H9626 |
EN-523
|
2094893-05-5 |
EN-523 is a small molecule covalent ligand EN523 that targets a non-catalytic allosteric cysteine C23 in the K48-ubiquitin-specific deubiquitinase OTUB1, OTUB1 recruiter component of DUBTAC NJH-2-057;Deubiquitinase-targeting chimeras (DUBTACs), heterobifunctional small molecules consisting of a deubiquitinase recruiter linked to a protein-targeting ligand, to stabilize the levels of specific proteins degraded in a ubiquitin-dependent manner. |
| H9402 |
XL177A
|
2417089-74-6 |
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. |
| H9393 |
LCAHA
|
117094-40-3 |
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。 |
| H8688 |
HBX 41108
|
924296-39-9 |
HBX 41108 is a inhibitor of ubiquitin-specific protease (USP) 7 activity (IC50 = 424 nM). Displays uncompetitive inhibition. Also inhibits USP7-mediated p53 deubiquitination (IC50 = 0.8 μM); Stabilizes p53 and inhibits cancer cell growth; induces p53-dependent apoptosis in p53 wild type and null isogenic cancer cell lines. |
| H7152 |
XL 188
|
2305045-76-3 |
XL188 (XL-188) is a potent, selective, non-covalent active-site inhibitor of USP7 with IC50 of 90 nM and 193 nM for USP7 full length enzyme and catalytic domain, respectively; exhibits little to no inhibition against a panel of 41 DUBs; promotes USP7-dependent loss of HDM2 and increases p53 and p21, significantly blocks labeling of USP7 by HA-Ub-Vs with an IC50 of 0.9 uM; a probe suitable for in vivo studies, highly valuable for pharmacological validation of USP7 in animal disease models. |
| H7151 |
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. |
| H7150 |
USP8-IN-22e
|
924296-19-5 |
A potent, selective ubiquitin-specific protease USP8 inhibitor with IC50 of 0.28 uM; shows no inhibitory activity for USP7 (IC50>100 uM). |
| H7149 |
USP8-IN-22d
|
924296-18-4 |
A potent, selective ubiquitin-specific protease USP8 inhibitor with IC50 of 0.85 uM; shows no inhibitory activity for USP7 (IC50>100 uM). |
| H7148 |
USP8-IN-22c
|
924296-17-3 |
A potent, selective ubiquitin-specific protease USP8 inhibitor with IC50 of 0.56 uM; shows no inhibitory activity for USP7, USP5, SENP1, Uch-L3, and caspase 3 (IC50>100 uM), and displays partial activity against Uch-L3; inhibits the viability of HCT116 colon and PC-3 prostate cancer cell lines with IC50 values in the 0.5-1.5 uM range. |
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