AdipoGen Life Sciences

Compound E

CHF 110.00
In stock
AG-CR1-0081-C250250 µgCHF 110.00
AG-CR1-0081-M0011 mgCHF 250.00
AG-CR1-0081-M0055 mgCHF 900.00
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Product Details
Synonyms γ-Secretase Inhibitor XXI; (2S)-2-([(3,5-Difluorophenyl)acetyl]amino)-N-[(3S)-1-methyl-2-oxo-5-phenyl-2,3-dihydro-1H-1,4-benzodiazepin-3-yl]propanamide
Product Type Chemical
Properties
Formula

C27H24F2N4O3

MW 490.5
CAS 209986-17-4
Purity Chemicals ≥98% (HPLC)
Appearance White to off-white solid.
Solubility Soluble in DMSO.
Identity Determined by 1H-NMR.
InChi Key JNGZXGGOCLZBFB-IVCQMTBJSA-N
Smiles C[C@H](NC(=O)CC1=CC(F)=CC(F)=C1)C(=O)N[C@H]1N=C(C2=CC=CC=C2)C2=C(C=CC=C2)N(C)C1=O
Shipping and Handling
Shipping AMBIENT
Short Term Storage +4°C
Long Term Storage -20°C
Use/Stability Stable for at least 2 years after receipt when stored at -20°C.
Documents
MSDS Download PDF
Product Specification Sheet
Datasheet Download PDF
Description
  • Cell permeable, potent, selective, non-transition state and non-competitive γ-secretase inhibitor.
  • Notch processing inhibitor.
  • Only weakly affects presenilinase activity.
Product References
  1. Presenilin-1 and -2 are molecular targets for gamma-secretase inhibitors: D. Seiffert, et al.; J. Biol. Chem. 275, 34086 (2000)
  2. Presenilin-dependent gamma-secretase activity modulates thymocyte development: P. Doerfler, et al.; PNAS 98, 9312 (2001)
  3. Pharmacological knock-down of the presenilin 1 heterodimer by a novel gamma -secretase inhibitor: implications for presenilin biology: D. Beher, et al.; J. Biol. Chem. 276, 45394 (2001)
  4. gamma -Secretase cleavage and nuclear localization of ErbB-4 receptor tyrosine kinase: C.Y. Ni, et al.; Science 294, 2179 (2001)
  5. Regulated intramembrane proteolysis of the p75 neurotrophin receptor modulates its association with the TrkA receptor: K.M. Jung, et al.; J. Biol. Chem. 278, 42161 (2003)
  6. Identification of a new presenilin-dependent zeta-cleavage site within the transmembrane domain of amyloid precursor protein: G. Zhao, et al.; J. Biol. Chem. 279, 50647 (2004)
  7. Activating mutations of NOTCH1 in human T cell acute lymphoblastic leukemia: A.P. Weng, et al.; Science 306, 269 (2004)
  8. Determination of guinea-pig cortical gamma-secretase activity ex vivo following the systemic administration of a gamma-secretase inhibitor: S. Grimwood, et al.; Neuropharmacology 48, 1002 (2005)
  9. Jagged/Notch signalling is required for a subset of TGFβ1 responses in human kidney epithelial cells: K.C. Nyhan, et al.; Biochim. Biophys. Acta 1803, 1386 (2010)
  10. Investigating the amyloid-beta enhancing effect of cGMP in neuro2a cells: E. Calcagno, et al.; Mech. Ageing Dev. 166, 1 (2017)
  11. Selective inhibition of phosphodiesterase 4D increases tau phosphorylation at Ser214 residue: V. Villa, et al.; BioFactors ahead of print (2022)
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