Accéder au contenu
Merck

565790

Compound E

≥95% (HPLC), solid, γ-secretase inhibitor, Calbiochem®

Synonyme(s) :

γ-Secretase Inhibitor XXI, Compound E, (S,S)- 2-[2-(3,5-Difluorophenyl)-acetylamino]-N-(1-methyl-2-oxo-5-phenyl-2,3-dihydro-1H-benzo[e][1,4]diazepin-3-yl)-propionamide, Compound E

Se connecter pour consulter les tarifs organisationnels et contractuels.

Sélectionner une taille de conditionnement

A propos de cet article

Formule empirique (notation de Hill) :
C27H24F2N4O3
Numéro CAS:
209986-17-4
Poids moléculaire :
490.50
MDL number:
MFCD04974531
UNSPSC Code:
12352200
NACRES:
NA.77
Assay:
≥95% (HPLC)
Form:
solid
Storage condition:
OK to freeze
protect from light

Principaux documents

Voir toute la documentation
Service technique
Besoin d'aide ? Notre équipe de scientifiques expérimentés est là pour vous.
Laissez-nous vous aider
Service technique
Besoin d'aide ? Notre équipe de scientifiques expérimentés est là pour vous.
Laissez-nous vous aider

Nom du produit

γ-Secretase Inhibitor XXI, Compound E, This g-secretase inhibitor, CAS 209986-17-4, is a cell-permeable, potent, selective, non-transition-state analog inhibitor of γ-secretase and Notch processing. Lowers Aβ levels in APP transgenic mice

SMILES string

Fc1cc(cc(c1)CC(=O)N[C@@H](C)C(=O)NC2N=C(c4c(cccc4)N(C2=O)C)c3ccccc3)F

InChI

1S/C27H24F2N4O3/c1-16(30-23(34)14-17-12-19(28)15-20(29)13-17)26(35)32-25-27(36)33(2)22-11-7-6-10-21(22)24(31-25)18-8-4-3-5-9-18/h3-13,15-16,25H,14H2,1-2H3,(H,30,34)(H,32,35)/t16-,25?/m0/s1

InChI key

JNGZXGGOCLZBFB-YPHZTSLFSA-N

assay

≥95% (HPLC)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
protect from light

color

white

solubility

DMSO: 10 mg/mL

shipped in

ambient

storage temp.

2-8°C

Catégories apparentées

Biochem/physiol Actions

Cell permeable: yes
Primary Target
γ-secretase and Notch processing Ab40 in CHO cells overexpressing wild type bAPP
Product does not compete with ATP.
Reversible: no
Target IC50: 300 pM for Aβ40 in CHO cells overexpressing wild typeβAPP; 240 pM for Aβ40, 370 pM for Aβ42, and 320 pM for NICD, respectively, in HEK293 cells stably transfected with βAPP695 and mNotchΔE(M1727V); 100 pM for both Aβ40

Disclaimer

Toxicity: Standard Handling (A)

General description

A cell-permeable, potent, selective, peptidomimetic, non-transition-state analog inhibitor of γ-secretase and Notch processing (IC50 = 300 pM for Aβ40 in CHO cells overexpressing wild type βAPP; 240 pM for Aβ40, 370 pM for Aβ42, and 320 pM for NICD, respectively, in HEK293 cells stably transfected with βAPP695 and mNotchΔE(M1727V); 100 pM for both Aβ40 and Aβ42 in SH-SY5Y cells stably transfected with SPA4CT). Lowers Aβ levels in several APP transgenic mouse models. Reported to bind to presenilins and suppress the proteolytic cleavage of transmembrane protein substrates, including APLP1 and APLP2, CD44, ErbB4, E-cadherin, low density lipoprotein receptor-related proteins, Notch ligands, and p75NTR. Only weakly affects presenilinase activity at much higher concentrations (200-400 µM).

Other Notes

Milano, J., et al. 2004. Toxicol. Sci.82, 341.
Jung, K.M., et al. 2003. J. Biol. Chem.278, 42161.
Murakami, D., et al. 2003. Oncogene22, 1511.
Campbell, W.A., et al. 2003. J. Neurochem.85, 1563.
Berechid, B.E., et al., 2002. J. Biol. Chem.277, 8154.
Lee, H.J., et al. 2002. J. Biol. Chem.277, 6318.
May, P., et al. 2002. J. Biol. Chem.277, 18736.
Scheinfeld, M.H., et al. 2002. J. Biol. Chem.277, 44195.
Ni, C. Y., et al. 2001. Science294, 2179.
Beher, D., et al. 2001. J. Biol. Chem.276, 45394.
Doerfler, P., et al. 2001. Proc. Natl. Acad. Sci. USA98, 9312.
Seiffert, D., et al. 2000. J. Biol. Chem.275, 34086.

Packaging

Packaged under inert gas

Preparation Note

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Legal Information

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

Classe de stockage

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

Certificats d'analyse (COA)

Recherchez un Certificats d'analyse (COA) en saisissant le numéro de lot du produit. Les numéros de lot figurent sur l'étiquette du produit après les mots "Lot" ou "Batch".

Déjà en possession de ce produit ?

Retrouvez la documentation relative aux produits que vous avez récemment achetés dans la Bibliothèque de documents.

Consulter la Bibliothèque de documents

Claire E McGhee et al.
ACS central science, 7(11), 1809-1820 (2021-11-30)
Lithium has been a drug for bipolar disorders (BD) for over 70 years; however, its usage has been limited by its narrow therapeutic window (between 0.6 and 1.2 mM). Understanding the cellular distribution of lithium ions (Li+) in patient cells
Kenichi Makino et al.
Journal for immunotherapy of cancer, 10(1) (2022-02-02)
Dendritic cells (DCs) play critical roles in regulating the innate and adaptive immune responses, and have long been a major focus of cancer immunotherapy. Accumulating evidence suggests that conventional type 1 DCs (cDC1s) excel in cross-presentation of exogenous antigens on
Christine E Eyler et al.
Genome biology, 21(1), 174-174 (2020-07-17)
Tumors can evolve and adapt to therapeutic pressure by acquiring genetic and epigenetic alterations that may be transient or stable. A precise understanding of how such events contribute to intratumoral heterogeneity, dynamic subpopulations, and overall tumor fitness will require experimental
Louise Thiry et al.
ASN neuro, 14, 17590914211073381-17590914211073381 (2022-01-14)
Human induced pluripotent stem cells (hiPSCs) derived from healthy and diseased individuals can give rise to many cell types, facilitating the study of mechanisms of development, human disease modeling, and early drug target validation. In this context, experimental model systems
Deli Hong et al.
Cancer research, 82(2), 248-263 (2021-11-24)
Neuroendocrine to nonneuroendocrine plasticity supports small cell lung cancer (SCLC) tumorigenesis and promotes immunogenicity. Approximately 20% to 25% of SCLCs harbor loss-of-function (LOF) NOTCH mutations. Previous studies demonstrated that NOTCH functions as a SCLC tumor suppressor, but can also drive
Afficher tous les articles scientifiques apparentés

Notre équipe de scientifiques dispose d'une expérience dans tous les secteurs de la recherche, notamment en sciences de la vie, science des matériaux, synthèse chimique, chromatographie, analyse et dans de nombreux autres domaines..

Contacter notre Service technique