DAPT

ALX-270-416

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γ-Secretase inhibitor

Cell permeable inhibitor of γ-secretase (IC₅₀=115nM for total β-amyloid, IC₅₀=200nM for β-amyloid 1-42). It reduces Aβ levels in vivo in plasma and cerebrospinal fluid in young and aged Tg2576 mice. It blocks the proteolytic processing of neurotrophin receptor alike death domain protein (NRADD)Does not inhibit presenilinase. Antagonizes Notch signaling through inhibition of Notch processing. DAPT treatment can influence hematopoietic cell fate decisions and enhances neuronal differentiation in embryonic stem cell-derived embryoid bodies independent of sonic hedgehog (shh) signaling.

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Product Details

Alternative Name	N-[N-(3,5-Difluorophenacetyl-L-alanyl)]-S-phenylglycine t-butyl ester, γ-Secretase inhibitor IX
Appearance	White to off-white solid.
CAS	208255-80-5
Couple Target	Secretase
Couple Type	Inhibitor
Formula	C₂₃H₂₆F₂N₂O₄
Identity	Determined by NMR.
MW	432.5
Purity	≥98% (HPLC)
Solubility	Soluble in 100% ethanol, DMSO (20mg/ml) or dichloromethane.

Handling & Storage

Use/Stability	As indicated on product label or CoA when stored as recommended. Stock solutions are stable for up to 3 months when stored at -20°C.
Handling	Protect from light. Packaged under inert gas. After reconstitution, prepare aliquots and store at -20°C.
Long Term Storage	-20°C
Shipping	Ambient Temperature

Regulatory Status	RUO – Research Use Only

Comprehensive genomic features indicative for Notch responsiveness: Giaimo, B. D., Friedrich, T., et al.; Nucleic Acids Res. 52, 5179 (2024), Abstract
Alzheimer’s disease‐associated P460L variant of EphA1 dysregulates receptor activity and blood‐brain barrier function: H.A. Owens, et al.; Alzheimers Dement. 20, 2016 (2024), Abstract
AGEs-induced MMP-9 activation mediated by Notch1 signaling is involved in impaired wound healing in diabetic rats: P. Zhu, et al.; Diabetes Res. Clin. Pract. 186, 109831 (2022), Abstract
Notch-dependent and -independent functions of transcription factor RBPJ: Friedrich, T., Ferrante, F., et al.; Nucleic Acids Res. 50, 7925 (2022), Abstract
Development of alveolar and airway cells from human iPS cells: toward SARS-CoV-2 research and drug toxicity testing: K. Tsuji, et al.; J. Toxicol. Sci. 46, 425 (2021), Abstract
Notch-mediated re-specification of neuronal identity during central nervous system development: P. Engerer, et al.; Curr. Biol. 31, 1 (2021), Abstract
HDAC3 functions as a positive regulator in Notch signal transduction: Ferrante, F., Giaimo, B. D., et al.; Nucleic Acids Res. 48, 3496 (2020), Abstract
Gamma secretase dependent release of the CD44 cytoplasmic tail upregulates IFI16 in cd44-/- tumor cells, MEFs and macrophages: K. Schultz, et al.; PLoS One 13, e0207358 (2018), Abstract
A Paradoxical Tumor-Suppressor Role for the Rac1 Exchange Factor Vav1 in T Cell Acute Lymphoblastic Leukemia: Robles-Valero, J., Lorenzo-Martín, L. F., et al.; Cancer Cell 32, 608 (2017), Abstract
Downregulating Notch-1-induced cytostatic and anti-angiogenic effects on trophoblast cells is associated with early spontaneous abortion: N. Yu, et al.; Int. J. Clin. Exp. Pathol. 9, 7255 (2016), Application(s): Drug treatment, Full Text

Last modified: May 29, 2024

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DAPT

ALX-270-416

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