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DAPT (GSI-IX) γ-secretase inhibitor,potent and specific

Catalog No.A8200
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10mM (in 1mL DMSO)
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Evaluation Sample
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Sample solution is provided at 25 µL, 10mM.

Product Citations

1. Wu F, Wu D, et al. "Generation of hepato-biliary organoids from human induced pluripotent stem cells." J Hepatol. 2019 Jan 7. pii: S0168-8278(19)30002-9. PMID:30630011
2. MXinwei Feng, Junfeng Lu, et al. "Mycobacterium smegmatis Induces Neurite Outgrowth and Differentiation in an Autophagy-Independent Manner in PC12 and C17.2 Cells." Front. Cell. Infect. Microbiol., 19 June 2018.
3. Tang J, Zhou H, et al. "Dual-Mode Imaging-Guided Synergistic Chemo- and Magnetohyperthermia Therapy in a Versatile Nanoplatform To Eliminate Cancer Stem Cells." ACS Appl Mater Interfaces. 2017 Jul 19;9(28):23497-23507.  PMID:28661121
4. Fan Y, Gao X, Chen J, et al. "HIV Tat Impairs Neurogenesis through Functioning As a Notch Ligand and Activation of Notch Signaling Pathway." J Neurosci. 2016 Nov 2;36(44):11362-11373. PMID:27807176
5. Zhou, Xuanxuan, et al. "Tetrahydroxystilbene glucoside extends mouse lifespan via up-regulating neural Klotho and down-regulating neural insulin/insulin-like growth factor 1." Neurobiology of Aging (2014).

Quality Control

Chemical structure


Related Biological Data

The result shows the level of Aβ40 and Aβ42 decreased as the DAPT concentration increased. Compared with Aβ42, the level of Aβ420 decreased more rapidly with increasing DAPT concentration.

Related Biological Data

The Neuro-2A cells (transfected with Klotho) were treated with DAPT for 16 h. The transfected Neuro-2A without DAPT treatment was assigned as control. Un-transfected Neruo-2A was assigned as wild type cells (wt). The protein levels of Klotho and Klotho (sub) from cells lysate were analyzed using Klotho and Flag antibody respectively. Gamma-secretase inhibitor DAPT could cleave Klotho stub. After treatment with DAPT, 5 kDa fragment was found in transfected cells, which was not seen in wt and control group.

Related Biological Data


Related Biological Data


Related Biological Data


Related Biological Data


Related Biological Data


Biological Activity

Description DAPT (GSI-IX) is a novel inhibitor of γ-secretase with IC50 of 20 nM in HEK 293 cells.
IC50 20 nM          


Cell experiment [1]:

Cell lines

SHG -44 human glioma cell line

Preparation method

The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months.

Reaction Conditions

5d; 1.0 μM


Cell viability in each group was detected by MTT. Compared with those in group A (control), proliferation of SHG -44 cells in group B (0.5 μM), C (1μM), D (5 μM) and E (10 μM) were inhibited by DAPT. For group B and A, the results were significantly different (P<0.05). However, cell viability of group B was significantly higher than those in group C, D and E (P<0.05). The results showed that increased inhibition effect was related to increased DAPT concentrations. However there was no difference among group C, D and E (P>0.05). It indicated that DAPT is a concentration-dependent inhibitor that may obviously inhibit SHG-44 cells proliferation. As concentration of DAPT higher than 1.0 μmol/L showed no more obvious disparities in cell inhibition, concentration of 1.0 μmol/L was our prioriy.

Animal experiment [2]:

Animal models

Male Balb/C mice

Dosage form

10 mg/kg/day; subcutaneously injected


CT26 colon adenocarcinoma cells (5 × 105 cells) in 500 μL of Phosphate buffer solution (PBS) were inoculated subcutaneously into the dorsum of all mice. Administration of DAPT significantly reduced serum sVEGFR1, while could not change serum VEGF concentration in control mice. Immunohistochemical study of the tumors showed that CD31 positive cells were reduced after DAPT administration (280.6 ± 81 vs. 386 ± 59.9 CD31 positive cells/mm2), although it was not statistically significant.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.


[1] Liu X, Xu Q R, Xie W F, et al. DAPT suppresses the proliferation of human glioma cell line SHG-44[J]. Asian Pacific journal of tropical medicine, 2014, 7(7): 552-556.

[2] Kalantari E, Saeidi H, Kia N S, et al. Effect of DAPT, a gamma secretase inhibitor, on tumor angiogenesis in control mice[J]. Advanced biomedical research, 2013, 2.

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Chemical Properties

Cas No. 208255-80-5 SDF Download SDF
Synonyms gamma-Secretase Inhibitor IX, DAPT, GSI-IX
Chemical Name tert-butyl (2S)-2-[[(2S)-2-[[2-(3,5-difluorophenyl)acetyl]amino]propanoyl]amino]-2-phenylacetate
Canonical SMILES CC(C(=O)NC(C1=CC=CC=C1)C(=O)OC(C)(C)C)NC(=O)CC2=CC(=CC(=C2)F)F
Formula C23H26F2N2O4 M.Wt 432.46
Solubility ≥21.623mg/mL in DMSO Storage Store at 4°C
Physical Appearance A solid Shipping Condition Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.


DAPT, N-[N-(3,5-Difluorophenacetyl)-L-alanyl]-S-phenylglycine t-butyl Ester, is a potent and specific inhibitor of  γ-secretase, a multimeric membrane protein complex that catalyzes proteolytic cleavage of amyloid precursor protein (APP) resulting in the accumulation of amyloi-β (Aβ) peptides which is associated with early on-set of familial Alzheimer’s disease (AD). It directly binds to the C-terminal fragment of the catalytic center of γ-secretase, presenilin (PS), especially within the transmenbrane domain 7 or more C-terminal region, resulting in the synthesis of a photoactivable DAPT derivative. Through oral administration, DAPT  dose-dependently reduced Aβ peptides levels in vivo in Plasma and cerebrospinal fluid in young (6 months old, plaque-free) and aged (17 months old, plaque-bearing) Tg2576 mice.


Thomas A. Lanz, Carol S. Himes, Giovanni Pallante, Lisa Adams, Shinji Yamazaki, Ben Amore, and Kalpana M. Merchant. The γ-secretase inhibitor N-[N-(3,5-Difluorophenacetyl)-L-alanyl]-S-phenylglycine t-butyl Ester reduces Aβ levels in vivo in plasma and cerebrospinal fluid in young (plague-free) and aged (plaque-bearing) Tg2576 mice. The Journal of Pharmacology and Experimental Therapeutics 2003: 305 (3) 864-871

Yuichi Morohashi, Toshiyuki Kan, Yusuke Tominari, Haruhiko Fuwa, Yumiko Okamura, Naoto Watanabe, Chihiro Sato, Hideaki Natsugari, Tohru Fukuyama, Takeshi Iwatsubo, and Taisuke Tomita. C-terminal fragment of presenilin is the molecular target of a dipeptidic γ-secretase-specific inhibitor DAPT (N-[N-(3,5-Difluorophenacetyl)-L-alanyl]-S-phenylglycine t-butyl Ester). The Journal of Biological Chemistry 2006: 281(21) 14670-14676