PU139

立即咨询

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。

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 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℃, 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。