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565770 Sigma-Aldrich

γ-Secretase Inhibitor IX - CAS 208255-80-5 - Calbiochem

Gamma-Secretase Inhibitor IX - CAS 208255-80-5, is a cell-permeable inhibitor of γ-secretase (Aβtotal IC₅₀ = 115 nM, Aβ42 IC₅₀ = 200 nM).

Synonym: γ-Secretase Inhibitor IX - CAS 208255-80-5 - Calbiochem, DAPT, N-[N-(3,5-Difluorophenacetyl-L-alanyl)]-S-phenylglycine t-Butyl Ester

  • CAS Number 208255-80-5

  • Empirical Formula (Hill Notation) C23H26F2N2O4

  • Molecular Weight 432.46

  •  MDL number MFCD04974585

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Properties

Quality Level   100
assay   ≥98% (HPLC)
form   lyophilized
mfr. no.   Calbiochem®
storage condition   OK to freeze
  protect from light
storage conditions   -20C
solubility   DMSO: 20 mg/mL
shipped in   ambient

Description

General description

A cell-permeable dipeptide that inhibits γ-secretase activity and suppresses Aβ production (Aβ total IC50 = 115 nM; Aβ42 IC50 = 200 nM). Reported to be functionally active in both HEK293 cells overexpressing human APP751 and neuronal cultures, however, it does not affect the secretion of amyloid-b precursor protein (APP). Effective in acutely lowering Ab in APPV717F-transgenic mice. Also effective in inhibiting the production of an ~6 kDa C-terminal cleavage product (CTFg) in HEK293 cells stably transfected with the Swedish mutant, βAPP695. Reported to reduce extracellular Aβ plaques and intracellular Aβ accumulation in 3xTgAD transgenic mice.

A cell-permeable dipeptide that suppresses Aβ production by blocking γ-secretase (Aβtotal IC50 = 115 nM, Aβ42 IC50 = 200 nM). Prevents Aβ34 generation in murine N2a cells and hAPP/hBACE-1 transfected human HEK 293 cells. Reported to be functionally active in both HEK 293 cells and neuronal cultures without affecting the secretion of amyloid-β precursor protein (APP). Also shown to lower Aβ levels acutely in APP-transgenic mice. Reported to reduce extracellular Aβ plaques and intracellular Aβ accumulation in 3xTgAD transgenic mice. A 25 mM (5 mg/462 µl) solution of γ-Secretase Inhibitor IX (Cat. No. 565784) in DMSO is also available.

Packaging

10 mg in Plastic ampoule

5 mg in Glass bottle

Packaged under inert gas

Biochem/physiol Actions

Cell permeable: yes

Product does not compete with ATP.

Reversible: no

Target IC50: 115 nM suppressing Aβtotal production; 200 nM suppressing Aβ42 production

Warning

Toxicity: Standard Handling (A)

Other Notes

Morohashi, Y., et al. 2006. J. Bio. Chem.Vol. 281, 14670.
Nishitomo, K. et al. 2006 J. Neurochem.99, 1555.
Oddo, S., et al. 2004. Neuron43, 321.
Dovey, H.F., et al. 2001. J. Neurochem.76, 173.
Sastre, M., et al. 2001. EMBO Rep.2, 835.
Vandermeeren, M., et al. 2001. Neurosci. Lett.315, 145.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Safety & Documentation

Safety Information

WGK Germany 
WGK 3
Flash Point(F) 
Not applicable
Flash Point(C) 
Not applicable
Protocols & Articles
Peer-Reviewed Papers
15

References

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