KU-57788 (Synonyms:NU7441)
目录号 : KM5429 CAS No. : 503468-95-9 纯度 : 98%

KU-57788 (NU7441) 是一种高效的选择性 DNA-PK 抑制剂,IC50 为 14 nM。 KU-57788 是 NHEJ 通路抑制剂。KU-57788 还抑制 PI3K 和 mTOR,IC50 分别为 5.0 和 1.7 μM。

规格 价格 是否有货 数量
5mg
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10mg
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50mg
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100mg
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200mg 询价 In-stock
500mg 询价 In-stock

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生物活性

KU-57788 (NU7441) is a highly potent and selective DNA-PK inhibitor with an IC50 of 14 nM. KU-57788 is an NHEJ pathway inhibitor. KU-57788 also inhibits PI3K and mTOR with IC50s of 5.0 and 1.7 μM, respectively.

体外研究

NU7441 (0.5 to 10 µM) inhibits the growth of liver cancer HepG2 cells dose- and time-dependently. NU7441 reduces pDNA-PKcs (S2056) protein expression in liver cancer cells. Furthermore, double treatment of NU7441 and 60Coγ IR affects DNA damage repair. NU7441 is solvent-exposed in BRD4, this inhibitor can be classified as a Type I BRD inhibitor. NU7441 reduces the frequency of NHEJ while increasing the rate of HDR following Cas9-mediated DNA cleavage.

体内研究

KU-57788 (0.5 to 10 µM) inhibits the growth of liver cancer HepG2 cells dose- and time-dependently. KU-57788 reduces pDNA-PKcs (S2056) protein expression in liver cancer cells. Furthermore, double treatment of KU-57788 and 60Coγ IR affects DNA damage repair. KU-57788 weakly inhibits BRD4 and BRDT with IC50s of 1 μM and 3.5 μM, respectively. KU-57788 is solvent-exposed in BRD4, this inhibitor can be classified as a Type I BRD inhibitor. KU-57788 reduces the frequency of NHEJ while increasing the rate of HDR following Cas9-mediated DNA cleavage.

分子式
C25H19NO3S
分子量
413.49
CAS号
503468-95-9
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 6.67 mg/mL (16.13 mM; ultrasonic and warming and heat to 60°C)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.4184 mL 12.0922 mL 24.1844 mL
5 mM 0.4837 mL 2.4184 mL 4.8369 mL
10 mM 0.2418 mL 1.2092 mL 2.4184 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°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO → 40% PEG300  → 5% Tween-80  → 45% saline

    Solubility: ≥ 0.67 mg/mL (1.62 mM); Clear solution

    此⽅案可获得 ≥ 0.67 mg/mL (1.62 mM,饱和度未知) 的澄清溶液。

    以 1 mL ⼯作液为例,取 100 μL 6.7000003 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加 ⼊ 50 μL Tween-80,混合均匀;然后继续加⼊ 450 μL ⽣理盐⽔定容⾄ 1 mL。

     
  • 2.

    请依序添加每种溶剂: 10% DMSO → 90% (20% SBE-β-CD in saline)

    Solubility: ≥ 0.67 mg/mL (1.62 mM); Clear solution

    此⽅案可获得 ≥ 0.67 mg/mL (1.62 mM,饱和度未知) 的澄清溶液。

    以 1 mL ⼯作液为例,取 100 μL 6.7000003 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD ⽣理盐⽔⽔溶液中,混 合均匀。

     
  • 3.

    请依序添加每种溶剂: 10% DMSO → 90% corn oil

    Solubility: ≥ 0.67 mg/mL (1.62 mM); Clear solution

    此⽅案可获得 ≥ 0.67 mg/mL (1.62 mM,饱和度未知) 的澄清溶液,此⽅案不适⽤于实验周期在半个⽉以上的实验。

    以 1 mL ⼯作液为例,取 100 μL 6.7000003 mg/mL 的澄清 DMSO 储备液加到 900 μL ⽟⽶油中,混合均匀。

科研文献
The molarity calculator equation
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
The dilution calculator equation
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2
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