PU139
目录号: PL15148 纯度: ≥99%
CAS No. :158093-65-3
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中文名称
PU139
英文名称
PU139
英文别名
PU139;2-(4-Fluorophenyl)isothiazolo[5,4-b]pyridin-3(2H)-one;BDBM50346554;2-(4-fluorophenyl)-[1,2]thiazolo[5,4-b]pyridin-3-one
Cas No.
158093-65-3
分子式
C12H7FN2Os
分子量
246.26
包装储存
4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
产品详情
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。
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 IC 50 s of 8.39, 9.74, 2.49 and 5.35 μM, respectively.
性状
Solid
IC50 & Target[1][2]
GCN5 8.39 μM (IC50) CREBBP 2.49 μM (IC
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 and MCF7 cells).
PU139 (0-100 μM; 24-72 hours) triggers caspase-independent cell death in the neuroblastoma cell line SK-N-SH. 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. has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male NMRI:nu/nu mic
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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.
溶解度数据
In Vitro: DMSO : 12.5 mg/mL (50.76 mM; ultrasonic and warming and heat to 60°C)配制储备液
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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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