DC-U4106

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

DC-U4106 

DC-U4106 是一种 USP8 靶向抑制剂,其 Kd 值为 4.7 μM,IC50 值为 1.2 μM。DC-U4106 可作用于泛素化途径,促进 Erα 的降解。DC-U4106 可以抑制剂肿瘤细胞的生长,具有较小毒性,可用于乳腺癌研究。

DC-U4106

DC-U4106 Chemical Structure

CAS No. : 2410534-62-0

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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[1].

IC50 & Target

Kd: 4.7 μM (USP8), IC50: 1.2 μM (USP8)[1].

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[1].
DC-U4106 (0-7 μM, 24 hours) reduces mRNA levels of ERα and PR[1].
DC-U4106 (0-5 μM, 24 hours) can regulate the RTK pathway related proteins and the expression of ERα and PR proteins[1].
DC-U4106 (0-5 μM, 12 hours) can induce apoptosis and inhibit cell proliferation[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

Cell 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-PCR[1]

Cell 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 Assay[1]

Cell Line: USP8-positive cell line MCF-7
Concentration: 0-5 μM
Incubation Time:
Result: Inhibited cell growth in a dose-dependent manner.

Apoptosis Analysis[1]

Cell 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.

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[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: BALB/c nude mice[1]
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.

分子量

525.56

Formula

C29H27N5O5

CAS 号

2410534-62-0

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

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.

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