产品
编 号:F752185
分子式:C29H27N5O5
分子量:525.56
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1mg
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5mg
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生物活性:
DC-U4106 is a USP8 targeting inhibitor with the Kdvalue of 4.7 μM and the IC50 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.

体内研究:
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.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.

体外研究:
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.
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