565771
γ-Secretase Inhibitor X
≥90% (HPLC), liquid, γ-secretase inhibitor, Calbiochem®
同義詞:
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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經驗公式（希爾表示法）:
C39H52N4O6
分子量：:
672.85
UNSPSC Code:
12352200
NACRES:
NA.54
Assay:
≥90% (HPLC)
Form:
liquid
Quality level:
Storage condition:
OK to freeze, desiccated, protect from light
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產品名稱
γ-Secretase Inhibitor X, InSolution, ≥90%, 1 mM
Quality Level
assay
≥90% (HPLC)
form
liquid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, desiccated, protect from light
shipped in
ambient
storage temp.
−20°C
1 of 1
本產品 | |||
|---|---|---|---|
| assay ≥90% (HPLC) | assay ≥95% (HPLC) | assay ≥95% (HPLC) | assay ≥98% (HPLC) |
| form liquid | form solid | form liquid | form lyophilized |
| 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. −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 |
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.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
Aβtotal
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
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).
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.
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.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
存儲類別/等級
10 - Combustible liquids
wgk
WGK 1
flash_point_f
188.6 °F - closed cup - (Dimethylsulfoxide)
flash_point_c
87 °C - closed cup - (Dimethylsulfoxide)
分析證明 (COA)
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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
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
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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