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 cancer.
性状
Solid
IC50 & Target[1][2]
Kd: 4.7 μM (USP8), IC50: 1.2 μM (USP8).
体外研究(In Vitro)
DC-U4106 (1.2-45.2 μM) inhibits USP8 and USP2 with the IC50 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. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
DC-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. has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, sealed storage, away from moisture and light In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
参考文献
[1]. Yucheng Tian, et al. Discovery of Potent Small-Molecule USP8 Inhibitors for the Treatment of Breast Cancer through Regulating ERα Expression. J Med Chem. 2022 Jul 5.
溶解度数据
In Vitro: THF : 10 mg/mL (19.03 mM; Need ultrasonic)配制储备液