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γ-Secretase inhibitor
ALX-270-416-M005 5 mg 130.00 USD
ALX-270-416-M025 25 mg 474.00 USD
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Replaces Prod. #: BML-PI154

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.

Product Details

Alternative Name:N-[N-(3,5-Difluorophenacetyl-L-alanyl)]-S-phenylglycine t-butyl ester, γ-Secretase inhibitor IX
Purity:≥98% (HPLC)
Identity:Determined by NMR.
Appearance:White to off-white solid.
Solubility:Soluble in 100% ethanol, DMSO (20mg/ml) or dichloromethane.
Shipping:Ambient Temperature
Long Term Storage:-20°C
Use/Stability: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.
Regulatory Status:RUO - Research Use Only
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Product Literature References

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;
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;
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;
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
Inside-out Regulation of Ectodomain Cleavage of Cluster-of-Differentiation-44 [CD44] and of Neuregulin-1 requires Substrate Dimerization: M. Hartmann, et al.; J. Biol. Chem. 290, 17041 (2015), Application(s): Cell Culture, Abstract; Full Text
DLL1-mediated Notch activation regulates endothelial identity in mouse fetal arteries: I. Sorensen, et al.; Blood 113, 5680 (2009), Abstract;
Release of a membrane-bound death domain by gamma-secretase processing of the p75NTR homolog NRADD: K. Gowrishankar, et al.; J. Cell. Sci. 117, 4099 (2004), Abstract;
Presenilin endoproteolysis mediated by an aspartyl protease activity pharmacologically distinct from gamma-secretase: W.A. Campbell, et al.; J. Neurochem. 85, 1563 (2003), Abstract;
The gamma-secretase inhibitor N-[N-(3,5-difluorophenacetyl)-L-alanyl]-S-phenylglycine t-butyl ester reduces A beta levels in vivo in plasma and cerebrospinal fluid in young (plaque-free) and aged (plaque-bearing) Tg2576 mice: T.A. Lanz et al.; J. Pharmacol. Exp. Ther. 305, 864 (2003), Abstract;
A gamma-secretase inhibitor blocks Notch signaling in vivo and causes a severe neurogenic phenotype in zebrafish: A. Geling et al.; EMBO Rep. 3, 688 (2002), Abstract;
Functional gamma-secretase inhibitors reduce beta-amyloid peptide levels in brain: H.F. Dovey, et al.; J. Neurochem. 76, 173 (2001), Abstract;

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