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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：

粉末 Keep in dark place,Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 60 mg/mL(138.74 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

无水乙醇: 8 mg/mL(18.5 mM)，配合低频超声助溶，注意：无水乙醇开封后，易挥发，也会吸收空气中的水分，导致溶解能力下降，请避免使用开封较久的乙醇
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].
作用机制 DAPT targets the C-terminal fragment of PS which represents the catalytic center of γ-secretase, especially the transmembrane domain 7 or more C-terminal region. DAPT can completely abolish the proteolytic activity of γ-secretase.[5][6]
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 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]Qi Y, et al. Combined small-molecule inhibition accelerates the derivation of functional cortical neurons from human pluripotent stem cells. Nat Biotechnol. 2017 Feb;35(2):154-163.

[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.