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PU139
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
PU139图片
CAS NO:158093-65-3
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议

产品介绍
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 withIC50s of 8.39, 9.74, 2.49 and 5.35 μM, respectively[1][2].

IC50& Target[1]

GCN5

8.39 μM (IC50)

CREBBP

2.49 μM (IC50)

PCAF

9.74 μM (IC50)

p300

5.35 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].

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].

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

性状

Solid

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℃)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM4.0607 mL20.3037 mL40.6075 mL
5 mM0.8121 mL4.0607 mL8.1215 mL
10 mM0.4061 mL2.0304 mL4.0607 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℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。