UC2288

发表于由

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。

UC2288  纯度: 99.92%

UC2288 是一种新型的、具有细胞通透性和口服活性的 p21 衰减试剂 (对 p21 具有相对选择性活性)，基于索拉非尼 (HY-10201) 的结构合成。UC2288 在不依赖 p53 的情况下下调 p21 mRNA 的表达，降低 p21 蛋白水平，对 p21 蛋白的稳定性影响很小。UC2288 对VEGFR2 和 Raf 激酶没有抑制作用，即使在 10 μM。

UC2288

UC2288 Chemical Structure

CAS No. : 1394011-91-6

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
50 mg ￥7300 In-stock
100 mg ￥9230 In-stock
250 mg ￥12000 In-stock
500 mg   询价  
1 g   询价  

* Please select Quantity before adding items.

UC2288 相关产品

•相关化合物库:

  • Covalent Screening Library Plus
  • Bioactive Compound Library Plus
  • Apoptosis Compound Library
  • Kinase Inhibitor Library
  • Anti-Cancer Compound Library
  • Autophagy Compound Library
  • Anti-Aging Compound Library
  • Covalent Screening Library
  • Reprogramming Compound Library
  • Ferroptosis Compound Library
  • Pyroptosis Compound Library
  • Glutamine Metabolism Compound Library
  • Anti-Pancreatic Cancer Compound Library
  • Anti-Blood Cancer Compound Library
  • Transcription Factor Targeted Library

生物活性

UC2288 is a novel, cell-permeable, and orally active p21 attenuator (relatively selective activity for p21), which is synthesized based Sorafenib (HY-10201). UC2288 decreases p21 mRNA expression independently of p53, and attenuates p21 protein levels with minimal effect on p21 protein stability. UC2288 has no inhibition of VEGFR2 and Raf kinases even at 10 μM[1].

体外研究
(In Vitro)

UC2288 (0-10 μM; 24 hours) decreases p21 protein level, but has no effects on other proteins[1].
UC2288 (0-10 μM; 24 hours) decreases p21 mRNA expression transcriptionally or post-transcriptionally but independently of p53[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

Cell Line: HK2 (normal kidney), 786-O (RCC), Caki-1 (RCC), ACHN (RCC) and HEY (ovarian cancer) cells
Concentration: 0 μM; 1 μM; 3 μM; 10 μM
Incubation Time: 24 hours
Result: Decreased p21 protein expression.

RT-PCR[1]

Cell Line: p53-mutant RCC cell line 786-O
Concentration: 10 μM
Incubation Time: 24 hours
Result: Decreased p21 mRNA independent of p53 expression.

体内研究
(In Vivo)

UC2888 (oral gavage; 15 mg/kg; 3 times a week; 4 weeks) co-treatment with imetelstat significantly suppresses tumor growth and does not effect mice weight[2].
UC2288 (intraperitoneal injection; 10 mg/kg; 4 times in 7 days) attenuates MPTP-induced behavioral impairment, prevents activation of MAPK pathway in the MPTP-treated mice brain. MPTP treatment raises TNF-α, IL-6 and IL-1β levels in MPTP treated mice brain, but UC2288 signicantly decreases MPTP-induced TNF-α, IL-6 levels, but IL-1β is not decreased in brain[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Eight-week old, athymic nude (NCr nu/nu) mice injected subcutaneously with HCT116 and ACHN cancer cells(2.5×106)[2]
Dosage: 15 mg/kg
Administration: Oral gavage; 3 times a week; 4 weeks; co-treatment with imetelstat
Result: Combined treatment with imetelstat synergistically inhibited tumor growth in mice.
Animal Model: MPTP-induced C57BL6 Parkinson’s disease mice model[3]
Dosage: 10 mg/kg
Administration: Intraperitoneal injection; 4 times in 7 days
Result: Ameliorated MPTP induced PD progression through inhibition of neuroinammation.

分子量

481.82

Formula

C20H18ClF6N3O2
CAS 号

1394011-91-6
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 50 mg/mL (103.77 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.0755 mL 10.3773 mL 20.7546 mL
5 mM 0.4151 mL 2.0755 mL 4.1509 mL
10 mM 0.2075 mL 1.0377 mL 2.0755 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (4.32 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.32 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Hiromi I Wettersten, et al. A Novel p21 Attenuator Which Is Structurally Related to Sorafenib. Cancer Biol Ther. 2013 Mar;14(3):278-85.

    [2]. Romi Gupta, et al. Synergistic tumor suppression by combined inhibition of telomerase and CDKN1A. Proc Natl Acad Sci U S A. 2014 Jul 29;111(30):E3062-71.

    [3]. Jun Hyung Im, et al. p21 inhibitor UC2288 ameliorates MPTP induced Parkinson’s disease progression through inhibition of oxidative stress and neuroinammation. Translational Medicine.Neurobiology of Disease

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务