LTURM34

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Chemical Structure| 1879887-96-3 同义名 : -
CAS号 : 1879887-96-3
货号 : A231935
分子式 : C24H18N2O3S
纯度 : 98%+
分子量 : 414.48
MDL号 : MFCD30536366
存储条件：

Pure form Sealed in dry, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 : -
动物实验配方：
生物活性
靶点

  • DNA-PK

    DNA-PK, IC50:0.034 μM

  • 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.
实验方案
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
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.