PU139
目录号 : KM10933 CAS No. : 158093-65-3 纯度 : 98%

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。

规格 价格 是否有货 数量
5mg
In-stock
10mg
In-stock
25mg
In-stock

Other Forms of Rapamycin:

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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.

IC50&Target

GCN5

8.39 μM (IC50)

CBP

2.49 μM (IC50)

p300

5.35 μM (IC50)

PCAF

9.74 μM (IC50)

体外研究

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.

体内研究

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

Animal Model: Male NMRI:nu/nu mice (Neuroblastoma xenografts)
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.
分子式
C12H7FN2Os
分子量
246.26
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)

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