PU139

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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。

PU139 

PU139 是一种有效的泛组蛋白乙酰转移酶 (HAT) 抑制剂。PU139 阻断 HATs Gcn5、p300/CBP 相关因子 (PCAF)、CBP 和 p300，IC50 分别为 8.39、9.74、2.49 和 5.35 μM。

PU139

PU139 Chemical Structure

CAS No. : 158093-65-3

规格 价格 是否有货 数量
5 mg ￥1500 In-stock
10 mg ￥2600 In-stock
25 mg ￥5600 In-stock
50 mg   询价  
100 mg   询价  

* Please select Quantity before adding items.

PU139 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Epigenetics Compound Library
  • Histone Modification Research Compound Library
  • Anti-Cancer Compound Library
  • Transcription Factor Targeted Library

生物活性

PU139 is a potent pan-histone acetyltransferase (HAT) inhibitor. PU139 blocks the HATs Gcn5, p300/CBP-associated factor (PCAF), CREB (cAMP response element-binding) protein (CBP) and p300 with IC50s of 8.39, 9.74, 2.49 and 5.35 μM, respectively[1][2].

IC50 & Target[1]

GCN5

8.39 μM (IC50)

CBP

2.49 μM (IC50)

p300

5.35 μM (IC50)

PCAF

9.74 μM (IC50)

体外研究
(In Vitro)

PU139 inhibits cell growth with GI50s of <60 μm (a431, a549, a2780, hepg2, sw480, u-87 mg, hct116 and sk-n-sh mcf7 cells)[1].
PU139 (0-100 μM; 24-72 hours) triggers caspase-independent cell death in the neuroblastoma cell line SK-N-SH[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.
体内研究
(In Vivo)

PU139 (25 mg/kg; i.p.) synergizes with Doxorubicin used as a prototypic chemotherapeutic drug in growth inhibition[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.

Animal Model: Male NMRI:nu/nu mice (Neuroblastoma xenografts)[1]
Dosage: 25 mg/kg
Administration: Intraperitoneally (PU139) with Dxorubicin at 8 mg/kg i.v.; Administered on days 14 and 21 as a single dose of each compound or, for combination therapy; both drugs were administered successively within 1 h.
Result: Optimum growth inhibition following a single PU139 therapy was moderate, but significant as compared with the untreated group and confirmed the previous findings.

分子量

246.26

Formula

C12H7FN2OS
CAS 号

158093-65-3
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
溶解性数据
In Vitro: 

DMSO : 12.5 mg/mL (50.76 mM; ultrasonic and warming and heat to 60°C)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 4.0607 mL 20.3037 mL 40.6075 mL
5 mM 0.8121 mL 4.0607 mL 8.1215 mL
10 mM 0.4061 mL 2.0304 mL 4.0607 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 (sealed storage, away from moisture)。-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。
参考文献

  • [1]. Gajer JM, et al. Histone acetyltransferase inhibitors block neuroblastoma cell growth in vivo. Oncogenesis. 2015;4(2):e137. Published 2015 Feb 9.

    [2]. Carneiro VC, et al. Epigenetic changes modulate schistosome egg formation and are a novel target for reducing transmission of schistosomiasis. PLoS Pathog. 2014;10(5):e1004116. Published 2014 May 8.

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