DAPT

DAPT (GSI-IX) is a potent and orally active γ-secretase inhibitor with IC50s of 115 nM and 200 nM for total amyloid-β (Aβ) and Aβ42, respectively. DAPT inhibits the activation of Notch 1 signaling and induces cell differentiation. DAPT also induces autophagy and apoptosis. DAPT has neuroprotection activity and has the potential for autoimmune and lymphoproliferative diseases, degenerative disease and cancers treatment[1][2].

208255-80-5

GSI-IX

12352005

H302, H315, H319, H335

Amyloid-β; Apoptosis; Autophagy; Notch; Organoid; γ-secretase

Reference compound

Apoptosis; Autophagy; Neuronal Signaling; Stem Cell/Wnt

Cancer-programmed cell death

Cancer; Inflammation/Immunology; Neurological Disease

https://www.medchemexpress.com/DAPT.html

10mM

99.97

DMSO : 62.5 mg/mL (ultrasonic)

FC1=CC(F)=CC(CC(N[C@H](C(N[C@H](C(OC(C)(C)C)=O)C2=CC=CC=C2)=O)C)=O)=C1

C23H26F2N2O4

432.46

H302, H315, H319, H335

[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]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.|[3]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.|[4]Tanimizu N, et al. Intrahepatic bile ducts are developed through formation of homogeneous continuous luminal network and its dynamic rearrangement in mice. Hepatology. 2016 Jul;64 (1) :175-88.|[5]Michael T. Chang, et al. Notch Drives Proliferation And Radiation Resistance Of Cancer Stem Cells In Adenoid Cystic Carcinoma. Yale University. January 2016.|[6]Majumder S, et al. Shifts in podocyte histone H3K27me3 regulate mouse and human glomerular disease. J Clin Invest. 2018 Jan 2;128 (1) :483-499.|[7]Yixin Tao, et al. β-catenin activation in hair follicle dermal stem cells induces ectopic hair outgrowth and skin fibrosis. J Mol Cell Biol. 2018 May 16.

Room Temperature

-20°C, 3 years; 4°C, 2 years (Powder)

Reference compound1