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LTURM34 {[allProObj[0].p_purity_real_show]}

货号:A231935

LTURM34 shows potent inhibition of DNA-PK (IC50 0.034 μM) with excellent selectivity over the Class I PI3K isoforms (IC50 all > 5 μM) and inhibits the proliferation of a wide range of tumor cell lines.

LTURM34 化学结构 CAS号:1879887-96-3
LTURM34 化学结构
CAS号:1879887-96-3
LTURM34 3D分子结构
CAS号:1879887-96-3
LTURM34 化学结构 CAS号:1879887-96-3
LTURM34 3D分子结构 CAS号:1879887-96-3
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LTURM34 纯度/质量文件 产品仅供科研

货号:A231935 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 DNA-PK 其他靶点 纯度
PI-103 ++

DNA-PK, IC50: 23 nM

99%+
CC-115 +++

DNA-PK, IC50: 0.013 μM

mTOR 98+%
Samotolisib 99%+
NU 7026 +

DNA-PK, IC50: 0.23 μM

PI3K 98+%
PIK-75 HCl ++++

DNA-PK, IC50: 2 nM

99%+
PP121 +

DNA-PK, IC50: 60 nM

VEGFR,PDGFR 99%+
KU-0060648 ++++

DNA-PK, IC50: 5 nM

98%
KU-57788 +++

DNA-PK, IC50: 14 nM

99%+
LTURM34 ++

DNA-PK, IC50: 0.034 μM

98%+
SF2523 +++

DNA-PK, IC50: 9 nM

99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

LTURM34 生物活性

靶点
  • DNA-PK

    DNA-PK, IC50:0.034 μM

描述 DNA-dependent protein kinase (DNA-PK) is a very large holoenzyme comprised of the p470 kDa DNA-PK catalytic subunit (DNA-PKcs) and the Ku heterodimer consisting of the p86 (Ku 80) and p70 (Ku 70) subunits. It is best known for its nonhomologous end joining (NHEJ) activity, which repairs double-strand DNA (dsDNA) breaks (DSBs)[1]. LTURM34 is a specific DNA-PK inhibitor with an IC50 value of 34 nM, and it exhibits 170-fold selectivity for DNA-PK over phosphoinositide 3-kinase (PI3K). The IC50s are 5.8 and 8.5 μM for PI3K β and δ, respectively[2]. LTURM34 was more consistently active against the selected cell lines compared with its analogues, but at best showed 54% inhibition against the HOP-92 non-small cell lung cancer line[2]
作用机制 Mechanism: LTURM34 could govern the strength of the interaction of the ring carbonyl with the Lys124 of DNA-PK as compared.

LTURM34 参考文献

[1]Chung JH. The role of DNA-PK in aging and energy metabolism. FEBS J. 2018 Jun;285(11):1959-1972. doi: 10.1111/febs.14410. Epub 2018 Mar 12. PMID: 29453899; PMCID: PMC5986591.

[2]Morrison R, Al-Rawi JM, Jennings IG, Thompson PE, Angove MJ. Synthesis, structure elucidation, DNA-PK and PI3K and anti-cancer activity of 8- and 6-aryl-substituted-1-3-benzoxazines. Eur J Med Chem. 2016 Mar 3;110:326-39. doi: 10.1016/j.ejmech.2016.01.042. Epub 2016 Jan 27. PMID: 26854431.

LTURM34 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.41mL

0.48mL

0.24mL

12.06mL

2.41mL

1.21mL

24.13mL

4.83mL

2.41mL

LTURM34 技术信息

CAS号1879887-96-3
分子式C24H18N2O3S
分子量 414.476
别名
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,2-8°C

溶解度

DMSO: 65 mg/mL(156.82 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

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