DC-U4106
目录号: PL04335 纯度: ≥99%
CAS No. :2410534-62-0
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中文名称
DC-U4106
英文名称
DC-U4106
英文别名
4H-1-Benzopyran-4-one, 8-[(3,5-dimethyl-1H-pyrazol-4-yl)oxy]-5,7-dihydroxy-2-[4-[4-(2-pyridinyl)-1-piperazinyl]phenyl]-;DC-U4106
Cas No.
2410534-62-0
分子式
C29H27N5O5
分子量
525.56
包装储存
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)
产品详情
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。
生物活性
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
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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