USP7 Inhibitor

BAY 11-7082 is an IκBα phosphorylation and NF-κB inhibitor. BAY 11-7082 selectively and irreversibly inhibits the TNF-α-induced phosphorylation of IκB-α, and decreases NF-κB and expression of adhesion molecules. BAY 11-7082 inhibits ubiquitin-specific protease USP7 and USP21 (IC₅₀=0.19, 0.96 μM, respectively). BAY 11-7082 inhibits gasdermin D (GSDMD) pore formation in liposomes and inflammasome-mediated pyroptosis and IL-1β secretion in human and mouse cells.

YCH2823 is an inhibitor of USP7 (IC₅₀ = 49.6 nM; K_d = 0.117 μM). YCH2823 shows significant efficacy in inhibiting TP53 wild-type and mutant tumors, with approximately 5-fold higher potency than FT671. YCH2823 induce apoptosis. YCH2823 synergistic effects with mTOR inhibitors.

HBX 41108 is an inhibitor of ubiquitin-specific protease 7 (USP7) with an IC₅₀ of 424 nM. HBX 41108 inhibits USP7-mediated p53 deubiquitination to stabilize p53 and inhibits cancer cell growth. BX 41108 can be used in cancer and diabetes research.

USP7-797 (USP7-IN-7) is an orally available, selective USP7 inhibitor (IC₅₀=0.5 nmol/L) with antitumor activity. USP7-797 reduces the level of MDM2, thereby increasing the stability and activity of p53, leading to cell cycle arrest and apoptosis. USP7-797 has low nanomolar cytotoxicity against p53 mutant cancer cell lines, p53 wild-type hematological tumors, and neuroblastoma cell lines.

OAT-4828 is an orally active ubiquitin-specific protease 7 (USP7) inhibitor with an IC₅₀ of 32 nM. OAT-4828 induces antileukemic activity in B-cell-derived non-Hodgkin's lymphoma models via inhibition of USP7. OAT-4828 is applicable to research related to chronic lymphocytic leukemia.

LC-U7-44 is a potent USP7 inhibitor with an IC₅₀ of 0.96 μM. LC-U7-44 binds to the hydrophobic catalytic pocket of USP7, forming hydrogen bonds with Gln297, Arg408, Asp295, Val296, and Gln351, and hydrophobic interactions with Leu406. LC-U7-44 exerts anti-proliferative effects on prostate cancer cells. LC-U7-44 can be used for the research of prostate cancer.

P6620 is an orally active USP7 inhibitor. P6620 specifically binds to USP7 and disrupts its interaction with LRRC41. P6620 exhibits anticancer activity against hepatocellular carcinoma. P6620 enhances the antitumor effect of Lenvatinib (HY-10981) in xenograft mouse models. P6620 can be used for the research of hepatocellular carcinoma.

USP7 Ligand-Linker Conjugates 1 is an Target Protein Ligand-Linker Conjugate that incorporates a ligand for USP7 (HY-175359) and a PROTAC linker, which recruits E3 ligases. USP7 Ligand-Linker Conjugates 1 can be used for synthesis of PROTAC USP7 Degrader-1 (HY-175358).

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.

USP7-IN-14 is a Ligand for target protein for pROTAC.

USP7-IN-19 is a USP7 inhibitor. USP7-IN-19 can be used for synthesis of PROTAC USP7 Degrader-1 (HY-175358).

USP7-IN-16 (Compound 61) is a selective USP7 inhibitor with IC₅₀ values of 5.5 nM in the FLINT assay and 2.1 nM in MM.1S cells. USP7-IN-16 exhibits antitumor activity in mice and is a promising candidate for research in the field of oncology.

YCH3124 (compound Z33) is a USP7 inhibitor (IC₅₀=41.9 nM) with antitumor activity. YCH3124 has good in vitro antiproliferative activity against various tumor cells including LNCaP (IC₅₀=3.6 nM) and CHP-212 (IC₅₀=9.9 nM). In addition, YCH3124 disrupts cell cycle progression by restricting G1 phase and induces apoptosis in CHP-212 cells.

USP7-IN-15 (compound J21) is a USP7 inhibitor, with an IC₅₀ of 41.35 nM.

USP7-055 is a USP7 inhibitor. USP7-055 can be used in cancer research.

HBX 28258 is a selective USP7 inhibitor, with an IC₅₀ of 22.6 μM. HBX 28258 can covalently binds to Cys223 located in the catalytic core of USP7, inhibits its deubiquitinating activity, promotes MDM2 protein degradation, and activates p53.

USP7-IN-20 is a highly selective USP7 inhibitor that binds allosterically to the allosteric pocket of USP7 in a non-competitive and reversible manner. USP7-IN-20 downregulates MDM2 protein levels and stabilizes p53, thereby inducing p21 expression and enhancing the ubiquitin-dependent degradation of MDM2. USP7-IN-20 effectively binds endogenous USP7 to inhibit cancer cell proliferation, and also induces apoptosis by promoting the cleavage of PARP and caspase 3. USP7-IN-20 can be widely used in cancer-related basic and translational research.