044679
CAS Number
209986-17-4Grade
Highly PurifiedMDL Number
MFCD04974531Molecular Formula
C27H24F2N4O3Molecular Weight
490.5EU Commodity Code
38220090Shipping Temp
RTStorage Temp
-20°CCompound E
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
Cell permeable, potent, selective, non-transition state and non-competitive gamma-secretase inhibitor. Notch processing inhibitor. Only weakly affects presenilinase activity.
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
Molecular Formula
C27H24F2N4O3
Appearance
White to off-white solid
1H-NMR
Conforms to reference
Storage and Stability
May be stored at RT for short-term only. Long-term storage is recommended at -20°C. For maximum recovery of product, centrifuge the original vial prior to removing the cap.
Important Note
This product as supplied is intended for research use only, not for use in human, therapeutic or diagnostic applications without the expressed written authorization of United States Biological.
Toxicity and Hazards
All products should be handled by qualified personnel only, trained in laboratory procedures.
Intended for research use only. Not for use in human, therapeutic, or diagnostic applications.
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: impli- cations 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 TGFbeta1 responses in human kidney epithelial cells: K.C. Nyhan, et al.; Biochim. Biophys. Acta 1803: 1386 (2010)USBio References
No references available