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CAS No.: 1879887-96-3

LTURM34 Catalog No. CSN22555

Synonyms: Lturm34

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.

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400-920-2911

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靶点选择性

生物活性

实验方案

技术信息

生物活性

描述DNA-dependent protein kinase (DNA-PK) is a very large holoenzyme comprised of the p470 kDa DNA-PK catalytic subunit (DNA-PK_cs) 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.
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.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.4127 mL
- 12.0634 mL
- 24.1268 mL
- 5 mM
- 0.4825 mL
- 2.4127 mL
- 4.8254 mL
- 10 mM
- 0.2413 mL
- 1.2063 mL
- 2.4127 mL

技术信息

CAS号

1879887-96-3

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C24H18N2O3S

运输

蓝冰

分子量

414.48

别名

Lturm34

溶解度

DMSO	13.14 mg/mL (31.7 mM)
Water	insoluble

动物实验配方

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