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Fig. 1 · Structure
Cat. No.
A11258
CAS No.
769169-27-9
Formula
C9H8ClF6NO3S2
Mol. Weight
391.74

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Begacestat (GSI-953)

Cat. No. A11258 CAS 769169-27-9

γ-secretase inhibitor

Begacestat is a novel, selective thiophene sulfonamide inhibitor of amyloid precursor protein gamma-secretase for the treatment of Alzheimer's disease.

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Biological Activity

Cellular Effect

Cell Line Activity Value Description Reference
CHO IC50 14.8 nM Inhibition of gamma secretase (unknown origin) mediated APP cleavage in CHO cells expressing APP Swedish KM/NL mutant assessed as reduction in amyloid beta 40 after 24 hrs by sandwich ELISA [PMID: 27045975]
CHO ED50 350 nM Inhibition of gamma-secretase in CHO cells assessed expressing NotchdeltaE assessed as inhibition of notch cleavage after overnight incubation by luciferase reporter gene assay [PMID: 23713656]
CHO IC50 353 nM Inhibition of gamma-secretase in CHO cells after overnight incubation by luciferase reporter gene assay [PMID: 23312944]
CHO ED50 7.8 nM Inhibition of gamma-secretase in CHO cells assessed expressing APPSw assessed as inhibition of amyloid beta(1 to x) secretion after overnight incubation by ELISA [PMID: 23713656]
HEK293 ED50 7.8 nM Inhibition of gamma-secretase in HEK293 cells after overnight incubation by Western blotting analysis [PMID: 23312944]
IMR-32 IC50 1.6 nM Inhibition of gamma-secretase in human IMR32 cell membrane using APP as substrate after 2 hrs by ELISA [PMID: 23312944]
IMR-32 IC50 10.5 nM Inhibition of gamma-secretase in human IMR32 cell membrane using Notch as substrate after 2 hrs by ELISA [PMID: 23312944]
SH-SY5Y IC50 8 nM Displacement of [3H]5-chloro-N-((2S,3R)-5,5,5-trifluoro-1-hydroxy-3-methylpentan-2-yl)thiophene-2-sulfonamide from gamma secretase in human SH-SY5Y cells by competitive binding assay [PMID: 19694467]

Specifications

Manufacturer Adooq Bioscience
Actions Inhibitor
CAS Number 769169-27-9
Applications γ-secretase inhibitor
Formula C9H8ClF6NO3S2
Molecular Weight 391.74
Synonyms GSI953
SMILES
OC[C@@H](NS(C1=CC=C(Cl)S1)(=O)=O)C(C(F)(F)F)C(F)(F)F

Storage & Solubility

In Vitro Solubility

Reported Solubility

No reported solubility data are available for this product.

Preparing Stock Solutions

Stock preparation is unavailable for this product molecular weight.

Calculated stock concentrations do not establish solvent solubility. Refer to the reported solubility data for experimental guidance.

Storage

Store powder at -20°C, keep desiccated.
In powder form, the chemical is stable for 36 months.
In solution, store at -20°C and use within 1 month to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.

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