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565770

Sigma-Aldrich

γ-Secretase Inhibitor IX

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

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Synonym(s):
γ-Secretase Inhibitor IX, DAPT, N-[N-(3,5-Difluorophenacetyl-L-alanyl)]-S-phenylglycine t-Butyl Ester
Empirical Formula (Hill Notation):
C23H26F2N2O4
CAS Number:
Molecular Weight:
432.46
MDL number:

Quality Level

assay

≥98% (HPLC)

form

lyophilized

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
protect from light

solubility

DMSO: 20 mg/mL

shipped in

ambient

storage temp.

−20°C

InChI

1S/C23H26F2N2O4/c1-14(26-19(28)12-15-10-17(24)13-18(25)11-15)21(29)27-20(16-8-6-5-7-9-16)22(30)31-23(2,3)4/h5-11,13-14,20H,12H2,1-4H3,(H,26,28)(H,27,29)/t14-,20-/m0/s1

InChI key

DWJXYEABWRJFSP-XOBRGWDASA-N

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This Item
565773565789565763
γ-Secretase Inhibitor IX Gamma-Secretase Inhibitor IX - CAS 208255-80-5, is a cell-permeable inhibitor of γ-secretase (Aβtotal IC₅₀ = 115 nM, Aβ42 IC₅₀ = 200 nM).

565770

γ-Secretase Inhibitor IX

γ-Secretase Inhibitor XII The γ-Secretase Inhibitor XII controls the biological activity of γ-Secretase. This small molecule/inhibitor is primarily used for Neuroscience applications.

565773

γ-Secretase Inhibitor XII

γ-Secretase Inhibitor XX This γ-secretase inhibitor, CAS 209984-56-5, is a cell-permeable dibenzazepine compound that lowers both brain and plasma Aβ40 levels by ~72% in Tg2576 mutant APP transgenic mouse model.

565789

γ-Secretase Inhibitor XX

γ-Secretase Inhibitor VI The γ-Secretase Inhibitor VI, also referenced under CAS 287196-57-0, controls the biological activity of γ-Secretase. This small molecule/inhibitor is primarily used for Neuroscience applications.

565763

γ-Secretase Inhibitor VI

form

lyophilized

form

solid

form

solid

form

solid

Quality Level

100

Quality Level

100

Quality Level

100

Quality Level

100

manufacturer/tradename

Calbiochem®

manufacturer/tradename

Calbiochem®

manufacturer/tradename

Calbiochem®

manufacturer/tradename

Calbiochem®

storage temp.

−20°C

storage temp.

−20°C

storage temp.

−20°C

storage temp.

−20°C

solubility

DMSO: 20 mg/mL

solubility

DMSO: 5 mg/mL

solubility

DMSO: 10 mg/mL

solubility

DMSO: 200 mg/mL

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.

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

Packaging

Packaged under inert gas

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

Storage Class

11 - Combustible Solids

wgk_germany

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable


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