DC-U4106 (C09-1125-958)

DC-U4106 is a USP8 targeting inhibitor with the K d value of 4.7 μM and the IC 50 value of 1.2 μM. DC-U4106 can target the ubiquitin pathway and facilitate the degradation of Erα . DC-U4106 inhibits tumor growth with minimal toxicity and has the potential for the research of breast cancerIn VitroDC-U4106 (1.2-45.2 μM) inhibits USP8 and USP2 with the IC 50 values of 1.2 μM and 58.4 μM, respectively, and no activity in USP7. DC-U4106 (0-7 μM, 24 hours) reduces mRNA levels of ERα and PR. DC-U4106 (0-5 μM, 24 hours) can regulate the RTK pathway related proteins and the expression of ERα and PR proteins. DC-U4106 (0-5 μM, 12 hours) can induce apoptosis and inhibit cell proliferation. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Western Blot AnalysisCell Line: USP8-positive cell line MCF-7 Concentration: 0-5 μM Incubation Time: 24 hours Result: Reduced the expression of EGFR, ErbB2, and ErbB3 proteins with increasing concentrations and caused degradation of ERα and PR proteins. RT-PCRCell Line: USP8-positive cell line MCF-7 Concentration: 0-7 μM Incubation Time: 24 hours Result: Reduced mRNA levels of ERα and PR. Cell Proliferation AssayCell Line: USP8-positive cell line MCF-7 Concentration: 0-5 μM Incubation Time: Result: Inhibited cell growth in a dose-dependent manner. Apoptosis AnalysisCell Line: USP8-positive cell line MCF-7 Concentration: 0-5 μM Incubation Time: 12 hours Result: Resulted in increasing in the proportion of apoptotic cells with increasing concentrations.In VivoDC-U4106 (intraperitoneal injection, 5 mg/kg or 20 mg/kg, every 2 days, 14 days) inhibits the proliferation of tumors and no significantly effects on body weight, organ morphology and structure in BALB/c nude mice . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: BALB/c nude mice Dosage: 5 mg/kg , 20 mg/kg Administration: Intraperitoneal injection, Every 2 days, 14 days Result: Inhibited tumor growth significantly at a concentration of 20 mg/kg.Form:SolidIC50& Target:Kd: 4.7 μM (USP8), IC50: 1.2 μM (USP8). Specification: 0.99 Molecular Formula: C29H27N5O5 Molecular Weight: 525.56