产品说明书

Compound 401

Print
Chemical Structure| 168425-64-7 同义名 : -
CAS号 : 168425-64-7
货号 : A279135
分子式 : C16H15N3O2
纯度 : 98+%
分子量 : 281.309
MDL号 : MFCD10568147
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 9 mg/mL(31.99 mM)，配合低频超声，并水浴加热至45℃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
动物实验配方：
生物活性
描述 DNA-dependent protein kinase (DNA-PK) is a key enzyme involved in the repair of DNA double strand breaks (DSBs). Compound 401 is a synthetic inhibitor of DNA-PK (IC50 = 0.28 μM) that also targets mTOR (IC50 = 5.3 μM) but not p110α/p85α PI3K in vitro[3]. Compound 401 inhibited mTOR activity in Raptor immunoprecipitates by 67% or 78% at 5 μM or 10 μM, respectively. In serum-starved Rat-1 fibroblast, 401 (10 μM) nearly completely decreased the phosphorylation of both S6K1 Thr389 and Akt Ser473 but with little effect on PI3K activity. In TSC1/cells, proliferation was strongly inhibited when exposed to 401 for 1 day (54%) or 2 days (84%). Growth inhibition by 401 was dose-dependent with a half-maximal effect at roughly 2 μM which is due in part to suppression of mTORC2/Akt signaling[3].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.55mL

0.71mL

0.36mL

17.77mL

3.55mL

1.78mL

35.55mL

7.11mL

3.55mL
参考文献

[1]Ballou LM, Selinger ES, et al. Inhibition of mammalian target of rapamycin signaling by 2-(morpholin-1-yl)pyrimido[2,1-alpha] isoquinolin-4-one. J Biol Chem. 2007 Aug 17;282(33):24463-70.

[2]Griffin RJ, Fontana G, et al. Selective benzopyranone and pyrimido[2,1-a] isoquinolin-4-one inhibitors of DNA-dependent protein kinase: synthesis, structure-activity studies, and radiosensitization of a human tumor cell line in vitro. J Med Chem. 2005 Jan 27;48(2):569-85.

[3]Ballou LM, Selinger ES, Choi JY, Drueckhammer DG, Lin RZ. Inhibition of mammalian target of rapamycin signaling by 2-(morpholin-1-yl)pyrimido[2,1-alpha]isoquinolin-4-one. J Biol Chem. 2007 Aug 17;282(33):24463-70