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  1. Epigenetics
  2. Epigenetic Reader Domain Histone Acetyltransferase
  3. GSK 4027

GSK 4027 是一種 PCAF/GCN5 溴結(jié)構(gòu)域的化學探針,作用于 PCAF,pIC50 為 7.4±0.11。

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GSK 4027 Chemical Structure

GSK 4027 Chemical Structure

CAS No. : 2079896-25-4

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規(guī)格 價格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ¥1430
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1 mg ¥590
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5 mg ¥1300
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10 mg ¥2200
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25 mg ¥4500
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Other Forms of GSK 4027:

MCE 顧客使用本產(chǎn)品發(fā)表的 1 篇科研文獻

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

GSK 4027 is a chemical probe for the PCAF/GCN5 bromodomain with an pIC50 of 7.4±0.11 for PCAF in a time-resolved fluorescence resonance energy transfer (TR-FRET) assay.

IC50 & Target

pIC50: 7.4±0.11 (PCAF)[1]

細胞效力
(Cellular Effect)
Cell Line Type Value Description References
HEK293 IC50
60 nM
Compound: (R,R)-32; GSK4027
Displacement of Halo-tagged histone H3.3 from NanoLuc-tagged full length human PCAF bromodomain expressed in HEK293 cells after 18 hrs by NanoBRET assay
Displacement of Halo-tagged histone H3.3 from NanoLuc-tagged full length human PCAF bromodomain expressed in HEK293 cells after 18 hrs by NanoBRET assay
[PMID: 28002667]
體外研究
(In Vitro)

GSK 4027 is a PCAF/GCN5 bromodomain chemical probe. p300/CREB binding protein associated factor (PCAF/KAT2B) and general control nonderepressible 5 (GCN5/KAT2A) are multidomain proteins that have been implicated in retroviral infection, inflammation pathways, and cancer development. GSK 4027 also demonstrates potency toward BRD4 BD1 and BRD9 inTR-FRET assay with pIC50s of <4.3 and 5.1±0.08, respectively. The selectivity of GSK 4027 against the wider bromodomain family is assessed in the BROMOscan panel with pKi of 8.9 and 8.9 for PCAF and GCN5, respectively. GSK 4027 shows equipotent activity against PCAF and GCN5 with Ki of 1.4 nM for both bromodomains. As expected due to the encouraging measured artificial membrane permeability (500 nm/s), treatment of HEK293 cells with GSK 4027 displace full length PCAF from histone H3.3 with little drop-off from the biochemical assay and a pIC50 7.2 (IC50 60 nM)[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

377.28

Formula

C17H21BrN4O

CAS 號
性狀

固體

顏色

Light yellow to yellow

運輸條件

Room temperature in continental US; may vary elsewhere.

儲存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
溶解性數(shù)據(jù)
細胞實驗: 

DMSO 中的溶解度 : 50 mg/mL (132.53 mM; 超聲助溶; 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 2.6506 mL 13.2528 mL 26.5055 mL
5 mM 0.5301 mL 2.6506 mL 5.3011 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, 2 years; -20°C, 1 year。-80°C儲存時,請在2年內(nèi)使用, -20°C儲存時,請在1年內(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

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
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, 2 years; -20°C, 1 year。-80°C儲存時,請在2年內(nèi)使用, -20°C儲存時,請在1年內(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 2.6506 mL 13.2528 mL 26.5055 mL 66.2638 mL
5 mM 0.5301 mL 2.6506 mL 5.3011 mL 13.2528 mL
10 mM 0.2651 mL 1.3253 mL 2.6506 mL 6.6264 mL
15 mM 0.1767 mL 0.8835 mL 1.7670 mL 4.4176 mL
20 mM 0.1325 mL 0.6626 mL 1.3253 mL 3.3132 mL
25 mM 0.1060 mL 0.5301 mL 1.0602 mL 2.6506 mL
30 mM 0.0884 mL 0.4418 mL 0.8835 mL 2.2088 mL
40 mM 0.0663 mL 0.3313 mL 0.6626 mL 1.6566 mL
50 mM 0.0530 mL 0.2651 mL 0.5301 mL 1.3253 mL
60 mM 0.0442 mL 0.2209 mL 0.4418 mL 1.1044 mL
80 mM 0.0331 mL 0.1657 mL 0.3313 mL 0.8283 mL
100 mM 0.0265 mL 0.1325 mL 0.2651 mL 0.6626 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:
GSK 4027
目錄號:
HY-101027
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