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Merck

565771

γ-Secretase Inhibitor X

≥90% (HPLC), liquid, γ-secretase inhibitor, Calbiochem®

Synonym(s):

InSolution γ-Secretase Inhibitor X, L-685,458, {1S-Benzyl-4R-[1-(1S-carbamoyl-2-phenethylcarbamoyl)-1S-3-methylbutylcarbamoyl]-2R-hydroxy-5-phenylpentyl}carbamic Acid tert-butyl Ester

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About This Item

Empirical Formula (Hill Notation):
C39H52N4O6
Molecular Weight:
672.85
UNSPSC Code:
12352200
NACRES:
NA.54

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Product Name

γ-Secretase Inhibitor X, InSolution, ≥90%, 1 mM

assay

≥90% (HPLC)

form

liquid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
desiccated
protect from light

shipped in

ambient

storage temp.

−20°C

Quality Level

100

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This Item
565789565794565770
γ-Secretase Inhibitor X InSolution, ≥90%, 1 mM

Sigma-Aldrich

565771

γ-Secretase Inhibitor X

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.

Sigma-Aldrich

565789

γ-Secretase Inhibitor XX

β-Secretase Inhibitor IV InSolution, ≥95%

Sigma-Aldrich

565794

β-Secretase Inhibitor IV

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).

Sigma-Aldrich

565770

γ-Secretase Inhibitor IX

form

liquid

form

solid

form

liquid

form

lyophilized

assay

≥90% (HPLC)

assay

≥95% (HPLC)

assay

≥95% (HPLC)

assay

≥98% (HPLC)

manufacturer/tradename

Calbiochem®

manufacturer/tradename

Calbiochem®

manufacturer/tradename

Calbiochem®

manufacturer/tradename

Calbiochem®

Quality Level

100

Quality Level

100

Quality Level

100

Quality Level

100

storage temp.

−20°C

storage temp.

−20°C

storage temp.

−70°C

storage temp.

−20°C

storage condition

OK to freeze, protect from light, desiccated

storage condition

OK to freeze, protect from light

storage condition

OK to freeze, avoid repeated freeze/thaw cycles, desiccated (hygroscopic), protect from light

storage condition

OK to freeze, protect from light

Biochem/physiol Actions

Cell permeable: yes
Primary Target
Aβtotal
Product does not compete with ATP.
Reversible: no
Target IC50: Aβtotal 17 nM, Aβ40 48 nM, and Aβ42 67 nM in SHSY5Y cells overexpressing spβA4CTF

Disclaimer

Toxicity: Standard Handling (A)

General description

A cell-permeable hydroxyethylene dipeptide isostere that acts as a potent and highly specific inhibitor of γ-secretase (Aβ total IC50 = 17 nM; Aβ40 IC50 = 48 nM; and Aβ42 IC50 = 67 nM in SH-SY5Y cells overexpressing spβA4CTF). Binds to presenilin and blocks Notch intracellular domain production. Also reported to block the formation of εCTF, resulting in the accumulation of α- and βCTF. Functions as a transition state analog mimic at the catalytic site of an aspartyl protease, however, it exhibits over 100-fold greater selectivity for γ-secretase than for cathepsin D.

Other Notes

Weidemann, A., et al. 2002. Biochemistry41, 2825.
Doerfler, P., et al. 2001. Proc. Natl. Acad. Sci. USA98, 9312.
Li, Y.M., et al. 2000. Proc. Natl. Acad. Sci. USA97, 6138.
Shearman, M.S., et al. 2000. Biochemistry39, 8698.

Packaging

Packaged under inert gas

Physical form

A 1 mM (250 µg in 372 µl or 500 µg in 744 µl) solution in DMSO.

Preparation Note

Following initial thaw, aliquot and freeze (-20°C).

Legal Information

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

Storage Class

10 - Combustible liquids

wgk

WGK 1

flash_point_f

188.6 °F - closed cup - (Dimethylsulfoxide)

flash_point_c

87 °C - closed cup - (Dimethylsulfoxide)

Certificates of Analysis (COA)

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Giulia Puliatti et al.
Progress in neurobiology, 227, 102482-102482 (2023-06-16)
Several studies including ours reported the detrimental effects of extracellular tau oligomers (ex-oTau) on glutamatergic synaptic transmission and plasticity. Astrocytes greatly internalize ex-oTau whose intracellular accumulation alters neuro/gliotransmitter handling thereby negatively affecting synaptic function. Both amyloid precursor protein (APP) and
Sylvia M Lee et al.
Cancer, 121(3), 432-440 (2014-09-25)
Aberrant Notch activation confers a proliferative advantage to many human tumors, including melanoma. This phase 2 trial assessed the antitumor activity of RO4929097, a gamma-secretase inhibitor of Notch signaling, with respect to the progression-free and overall survival of patients with
Lukas P Feilen et al.
eLife, 11 (2022-05-18)
Cleavage of membrane proteins in the lipid bilayer by intramembrane proteases is crucial for health and disease. Although different lipid environments can potently modulate their activity, how this is linked to their structural dynamics is unclear. Here, we show that
Nicole L Stott Bond et al.
Biomedicines, 11(1) (2023-01-22)
Lung cancer maintains a relatively small survival rate (~19%) over a 5-year period and up to 80-85% of all lung cancer diagnoses are Non-Small Cell Lung Cancer (NSCLC). To determine whether metformin reduces non-small cell lung cancer (NSCLC) LL/2 cell
Edgar Dawkins et al.
The Journal of biological chemistry, 299(4), 103027-103027 (2023-02-23)
Imbalances in the amounts of amyloid-β peptides (Aβ) generated by the membrane proteases β- and γ-secretase are considered as a trigger of Alzheimer's disease (AD). Cell-free studies of γ-secretase have shown that increasing membrane thickness modulates Aβ generation but it
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