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  2. Epigenetics
  3. Histone Acetyltransferase
  4. PU139

PU139 是一種有效的泛組蛋白乙酰轉(zhuǎn)移酶 (HAT) 抑制劑。PU139 阻斷 HATs Gcn5、p300/CBP 相關(guān)因子 (PCAF)、CBP 和 p300，IC50 分別為 8.39、9.74、2.49 和 5.35 μM。

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PU139 Chemical Structure

PU139 Chemical Structure

CAS No. : 158093-65-3

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規(guī)格 價格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥1547
In-stock
1 mg ￥571
In-stock
5 mg ￥1500
In-stock
10 mg ￥2600
In-stock
25 mg ￥5600
In-stock
50 mg   詢價  
100 mg   詢價  

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Customer Review

查看 Histone Acetyltransferase 亞型特異性產(chǎn)品:

  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻

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)

CREBBP

2.49 μM (IC50)

PCAF

9.74 μM (IC50)

p300

5.35 μM (IC50)

細胞效力
(Cellular Effect)
Cell Line Type Value Description References
HL-60 GI50
3.42 μM
Compound: 1, PU139
Cytotoxicity against human HL60 cells assessed as growth inhibition after 72 hrs by MTS assay
Cytotoxicity against human HL60 cells assessed as growth inhibition after 72 hrs by MTS assay
10.1039/C4MD00245H
HL-60 GI50
3.42 μM
Compound: 67
Antiproliferative activity against human HL-60 cells incubated for 72 hrs by CellTiter 96 Aqueous non-radioactive cell proliferation assay
Antiproliferative activity against human HL-60 cells incubated for 72 hrs by CellTiter 96 Aqueous non-radioactive cell proliferation assay
[PMID: 33045661]
LNCaP GI50
36.2 μM
Compound: 1, PU139
Cytotoxicity against human LNCAP cells assessed as growth inhibition after 72 hrs by MTS assay
Cytotoxicity against human LNCAP cells assessed as growth inhibition after 72 hrs by MTS assay
10.1039/C4MD00245H
MCF7 GI50
37.2 μM
Compound: 4d
Growth inhibition of human MCF7 cells by CellTiter-96 Aqueous Non-radioactive cell proliferation assay
Growth inhibition of human MCF7 cells by CellTiter-96 Aqueous Non-radioactive cell proliferation assay
[PMID: 21353783]
Sf9 IC50
10 μM
Compound: PU139
Inhibition of recombinant human N-terminal His-GST-tagged p300 (965 to 1810 residues) expressed in baculovirus infected Sf9 insect cells preincubated for 10 mins in presence of biotinylated-histone H3/H4 followed by acetyl-CoA addition and measured after
Inhibition of recombinant human N-terminal His-GST-tagged p300 (965 to 1810 residues) expressed in baculovirus infected Sf9 insect cells preincubated for 10 mins in presence of biotinylated-histone H3/H4 followed by acetyl-CoA addition and measured after
[PMID: 31910017]
SK-N-SH GI50
10.3 μM
Compound: 4d
Growth inhibition of human SK-N-SH cells by CellTiter-96 Aqueous Non-radioactive cell proliferation assay
Growth inhibition of human SK-N-SH cells by CellTiter-96 Aqueous Non-radioactive cell proliferation assay
[PMID: 21353783]
體外研究
(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)[1].
? PU139 (0-100 μM; 24-72 hours) triggers caspase-independent cell death in the neuroblastoma cell line SK-N-SH[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
體內(nèi)研究
(In Vivo)

PU139 (25 mg/kg; i.p.) synergizes with Doxorubicin used as a prototypic chemotherapeutic drug in growth inhibition[1].

MCE 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 號
性狀

固體

顏色

Off-white to yellow

運輸條件

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

4°C, sealed storage, away from moisture

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

溶解性數(shù)據(jù)
細胞實驗： 

DMSO 中的溶解度 : 10 mg/mL (40.61 mM; 超聲助溶 (<60°C); 吸濕的 DMSO 對產(chǎn)品的溶解度有顯著影響，請使用新開封的 DMSO)

配制儲備液
濃度 溶劑體積 質(zhì)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
查看完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C儲存時，請在6個月內(nèi)使用，-20°C儲存時，請在1個月內(nèi)使用。

  • 摩爾計算器

  • 稀釋計算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

質(zhì)量
=
濃度
×
體積
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

C1

×
體積 (start)

V1

=
濃度 (final)

C2

×
體積 (final)

V2

動物溶解方案計算器
請輸入動物實驗的基本信息：

給藥劑量

mg/kg

動物的平均體重

g

每只動物的給藥體積

μL

動物數(shù)量

只
由于實驗過程有損耗，建議您多配一只動物的量
計算結(jié)果
工作液所需濃度 : mg/mL
純度 & 產(chǎn)品資料

純度: 99.14%

參考文獻

完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C儲存時，請在6個月內(nèi)使用，-20°C儲存時，請在1個月內(nèi)使用。

可選溶劑 濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 4.0607 mL 20.3037 mL 40.6075 mL 101.5187 mL
5 mM 0.8121 mL 4.0607 mL 8.1215 mL 20.3037 mL
10 mM 0.4061 mL 2.0304 mL 4.0607 mL 10.1519 mL
15 mM 0.2707 mL 1.3536 mL 2.7072 mL 6.7679 mL
20 mM 0.2030 mL 1.0152 mL 2.0304 mL 5.0759 mL
25 mM 0.1624 mL 0.8121 mL 1.6243 mL 4.0607 mL
30 mM 0.1354 mL 0.6768 mL 1.3536 mL 3.3840 mL
40 mM 0.1015 mL 0.5076 mL 1.0152 mL 2.5380 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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產(chǎn)品名稱：
PU139
目錄號：
HY-124696
需求量：