DAPT

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Chemical Structure| 208255-80-5 同义名 : GSI-IX; LY-374973; N-(2FPhAc)Ala-phenyl-Gly t-butyl ester.; DAPT peptide
CAS号 : 208255-80-5
货号 : A150458
分子式 : C23H26F2N2O4
纯度 : 99%+
分子量 : 432.46
MDL号 : MFCD04974585
存储条件:

Pure form Keep in dark place, sealed in dry, store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月

溶解度 : -
动物实验配方:

IP 2% DMSO+2% Tween80+40% PEG300+water 5 mg/mL clear

PO 0.5% CMC-Na 27 mg/mL suspension

生物活性
描述 DAPT (GSI-IX), a powerful and orally bioavailable γ-secretase inhibitor, exhibits IC50 values of 115 nM for total amyloid-β (Aβ) and 200 nM for Aβ42. It blocks Notch 1 signaling activation and promotes cell differentiation. Additionally, DAPT triggers autophagy and apoptosis, offers neuroprotective effects, and holds therapeutic potential for autoimmune, lymphoproliferative disorders, degenerative diseases, and cancer[1][2]. DAPT (GSI-IX) (GMP) refers to DAPT manufactured according to GMP standards. GMP-compliant small molecules function effectively as supporting agents in the production of cell therapies. DAPT acts as a potent, orally administrable γ-secretase inhibitor[1][2].
细胞研究
细胞系 浓度 检测类型 检测时间 活性说明 数据源
A549 10 μM Growth Inhibition Assay 24h decreases the cell viability combined with PTE 23671619
A549 CD133− 2 μM Growth Inhibition Assay 48 h enhances cell growth inhibition induced by CDDP 24502949
A549 CD133+ 2 μM Growth Inhibition Assay 48 h enhances cell growth inhibition induced by CDDP 24502949
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.31mL

0.46mL

0.23mL

11.56mL

2.31mL

1.16mL

23.12mL

4.62mL

2.31mL

参考文献

[1]Dovey HF, et al. Functional gamma-secretase inhibitors reduce beta-amyloid peptide levels in brain. J Neurochem. 2001 Jan;76(1):173-81.

[2]Li S, et al. DAPT protects brain against cerebral ischemia by down-regulating the expression of Notch 1 and nuclear factor κB in rats. Neurol Sci. 2012 Dec;33(6):1257-64.

[3]Zhou JX, et al. γ-secretase inhibition combined with NSC 119875 enhances apoptosis of nasopharyngeal carcinoma cells.Exp Ther Med. 2012 Feb;3(2):357-361.