Compound E A cell permeable non-competitive γ-secretase inhibitor

Compound E (CAS 209986-17-4)

Compound E | CAS 209986-17-4 is rated 5.0 out of 5 by 2.
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Synonym: γ-Secretase Inhibitor; GSI
Application: A cell permeable non-competitive γ-secretase inhibitor
CAS Number: 209986-17-4
Purity: ≥98%
Molecular Weight: 490.50
Molecular Formula: C27H24F2N4O3
* Refer to Certificate of Analysis for lot specific data (including water content).
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Compound E is a cell permeable non-competitve inhibitor of γ-secretase. Studies indicate that γ-secretase is a multifunctional transmembrane protein complex that enzymatically catalyzes the cleavage of single-pass transmembrane proteins. One of the most common substrates for this enzyme is amyloid precursor protein. Once cleaved this protein produces amyloid plaques in brain tissue often seen in Alzheimer's disease. Thus Compound E is a useful research tool in Alzheimer's disease.


References

1. Hofeldt, F D., et al., 1975. Postprandial hypoglycemia. Fact or fiction? JAMA : the journal of the American Medical Association. 233(12): 1309. PMID: 1174196
2. Seiffert, D., et al., 2000. Presenilin-1 and -2 are molecular targets for gamma-secretase inhibitors. The Journal of biological chemistry. 275(44): 34086-91. PMID: 10915801
3. Doerfler, P., et al., 2001. Presenilin-dependent gamma-secretase activity modulates thymocyte development. Proceedings of the National Academy of Sciences of the United States of America. 98(16): 9312-7. PMID: 11470902
4. Beher, D., et al., 2001. Pharmacological knock-down of the presenilin 1 heterodimer by a novel gamma -secretase inhibitor: implications for presenilin biology. The Journal of biological chemistry. 276(48): 45394-402. PMID: 11574530
5. Ni, C Y., et al., 2001. gamma -Secretase cleavage and nuclear localization of ErbB-4 receptor tyrosine kinase. Science (New York, N.Y.). 294(5549): 2179-81. PMID: 11679632
6. Tian, Gaochao., et al., 2002. Linear non-competitive inhibition of solubilized human gamma-secretase by pepstatin A methylester, L685458, sulfonamides, and benzodiazepines. The Journal of biological chemistry. 277(35): 31499-505. PMID: 12072428
7. Francis, Ross., et al., 2002. aph-1 and pen-2 are required for Notch pathway signaling, gamma-secretase cleavage of betaAPP, and presenilin protein accumulation. Developmental cell. 3(1): 85-97. PMID: 12110170
8. Murakami, Daizo., et al., 2003. Presenilin-dependent gamma-secretase activity mediates the intramembranous cleavage of CD44. Oncogene. 22(10): 1511-6. PMID: 12629514
9. Jung, Kwang-Mook., et al., 2003. Regulated intramembrane proteolysis of the p75 neurotrophin receptor modulates its association with the TrkA receptor. The Journal of biological chemistry. 278(43): 42161-9. PMID: 12913006
10. Zou, Zhiying., et al., 2004. Linking receptor-mediated endocytosis and cell signaling: evidence for regulated intramembrane proteolysis of megalin in proximal tubule. The Journal of biological chemistry. 279(33): 34302-10. PMID: 15180987
11. Hansson, Camilla A., et al., 2004. Nicastrin, presenilin, APH-1, and PEN-2 form active gamma-secretase complexes in mitochondria. The Journal of biological chemistry. 279(49): 51654-60. PMID: 15456764
12. Weng, Andrew P., et al., 2004. Activating mutations of NOTCH1 in human T cell acute lymphoblastic leukemia. Science (New York, N.Y.). 306(5694): 269-71. PMID: 15472075
13. Zhao, Guojun., et al., 2004. Identification of a new presenilin-dependent zeta-cleavage site within the transmembrane domain of amyloid precursor protein. The Journal of biological chemistry. 279(49): 50647-50. PMID: 15485850
14. Grimwood, S., et al., 2005. Determination of guinea-pig cortical gamma-secretase activity ex vivo following the systemic administration of a gamma-secretase inhibitor. Neuropharmacology. 48(7): 1002-11. PMID: 15857627

Appearance :
Powder
Physical State :
Solid
Solubility :
Soluble in DMSO (10 mg/ml).
Storage :
Store at -20° C
Melting Point :
322.17° C (Predicted)
Boiling Point :
778.56° C at 760 mmHg (Predicted)
Density :
1.31 g/cm3 (Predicted)
Refractive Index :
n20D 1.62 (Predicted)
IC50 :
Aβ40 and Aβ42: IC50 = 0.1 nM (SH-SY5Y cells ); Aβ40: IC50 = 0.24 nM (HEK293 cells); Aβ40: IC50 = 0.3 nM (CHO cells); NICD: IC50 = 0.32 nM (HEK293 cells); Aβ42: IC50 = 0.37 nM (HEK293 cells)
pK Values :
pKa: 12.54 (Predicted), pKb: 3.05 (Predicted)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
PubChem CID :
11306390
MDL Number :
MFCD04974531
SMILES :
C[C@@H](C(=O)N[C@@H]1C(=O)N(C2=CC=CC=C2C(=N1)C3=CC=CC=C3)C)NC(=O)CC4=CC(=CC(=C4)F)F

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Compound E  Product Citations

See how others have used Compound E. Click on the entry to view the PubMed entry .

Citations 1 to 4 of 4 total

PMID: # 26910875  Liu, C. et al. 2016. Hepatology.

PMID: # 25339752  Conner, C. et al. 2014. J. Neurosci. 34: 14403-19.

PMID: # 24361736  Kanemoto, S. et al. 2014. Neuroscience. 261: 52-9.

PMID: # 23020188  Ogura, A. et al. 2013. Stem Cells Dev. 22: 374-82.

Citations 1 to 4 of 4 total
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Rated 5 out of 5 by from Our lab tested this in cell culture and works fine Our lab tested this in cell culture and works fine.
Date published: 2015-10-22
Rated 5 out of 5 by from Grimwood et al Grimwood et al. (PubMed ID 15857627) showed that the gamma-secretase inhibitor, compound E, lowered amyloid beta-peptide in guinea-pig plasma. -SCBT Publication Review
Date published: 2015-01-15
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