2. Neuronal Signaling
  3. Amyloid-β
  4. SCH 900229

SCH 900229 is a potent γ-secretase inhibitor with selective activity against PS1. The Aβ40 IC50 value of SCH 900229 is 1.3 nM, showing its excellent ability in reducing Aβ. SCH 900229 has shown good Aβ-lowering effects after oral administration in preclinical animal models. SCH 900229 has been advanced to human clinical trials for further development of compounds for the inhibition of Alzheimer's disease.

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SCH 900229

SCH 900229 Chemical Structure

CAS No. : 1100361-36-1

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Description

SCH 900229 is a potent γ-secretase inhibitor with selective activity against PS1. The Aβ40 IC50 value of SCH 900229 is 1.3 nM, showing its excellent ability in reducing Aβ. SCH 900229 has shown good Aβ-lowering effects after oral administration in preclinical animal models. SCH 900229 has been advanced to human clinical trials for further development of compounds for the inhibition of Alzheimer's disease[1].

Cellular Effect
Cell Line Type Value Description References
HEK293 IC50
1 nM
Compound: (-)-16, SCH-900229
Inhibition of PS2 gamma-secretase expressed in HEK cells harboring Awe-Lon gene assessed as reduction of amyloid beta-42 production
Inhibition of PS2 gamma-secretase expressed in HEK cells harboring Awe-Lon gene assessed as reduction of amyloid beta-42 production
[PMID: 24900404]
HEK293 IC50
1 nM
Compound: (-)-1a
Inhibition of gamma secretase-mediated amyloid beta42 production in HEK293 cells transfected with human APPSOW and APPLON after 5 hrs by sandwich immunoassay
Inhibition of gamma secretase-mediated amyloid beta42 production in HEK293 cells transfected with human APPSOW and APPLON after 5 hrs by sandwich immunoassay
[PMID: 23265892]
HEK293 IC50
1 nM
Compound: 1, SCH 900229
Inhibition of gamma-secretase (unknown origin) expressed in HEK293 cells co-expressing Awe-Lon mutant assessed as reduction of amyloid beta-42 production
Inhibition of gamma-secretase (unknown origin) expressed in HEK293 cells co-expressing Awe-Lon mutant assessed as reduction of amyloid beta-42 production
[PMID: 23265902]
HEK293 IC50
1.3 nM
Compound: (-)-1a
Inhibition of gamma secretase-mediated amyloid beta40 production in HEK293 cell membranes transfected with human APPSOW and APPLON mutant after 5 hrs by sandwich immunoassay
Inhibition of gamma secretase-mediated amyloid beta40 production in HEK293 cell membranes transfected with human APPSOW and APPLON mutant after 5 hrs by sandwich immunoassay
[PMID: 23265892]
HEK293 IC50
1.3 nM
Compound: (-)-1a; SCH 900229
Inhibition of gamma-secretase in HEK293 cell membranes expressing human APP Swedish/London double mutant assessed as reduction in amyloid beta 40 formation after 1 hr by electrochemiluminescence based immunoassay
Inhibition of gamma-secretase in HEK293 cell membranes expressing human APP Swedish/London double mutant assessed as reduction in amyloid beta 40 formation after 1 hr by electrochemiluminescence based immunoassay
[PMID: 27836402]
HEK293 IC50
1.3 nM
Compound: 1, SCH 900229
Inhibition of gamma-secretase (unknown origin) expressed in HEK293 cell membrane co-expressing Awe-Lon mutant assessed as reduction of amyloid beta-40 production
Inhibition of gamma-secretase (unknown origin) expressed in HEK293 cell membrane co-expressing Awe-Lon mutant assessed as reduction of amyloid beta-40 production
[PMID: 23265902]
HEK293 IC50
4 nM
Compound: (-)-16, SCH-900229
Inhibition of PS1 gamma-secretase expressed in HEK cells harboring Awe-Lon gene assessed as reduction of amyloid beta-40 production
Inhibition of PS1 gamma-secretase expressed in HEK cells harboring Awe-Lon gene assessed as reduction of amyloid beta-40 production
[PMID: 24900404]
HEK293 IC50
4 nM
Compound: (-)-1a
Inhibition of gamma secretase-mediated amyloid beta40 production in HEK293 cells transfected with human APPSOW and APPLON after 5 hrs by sandwich immunoassay
Inhibition of gamma secretase-mediated amyloid beta40 production in HEK293 cells transfected with human APPSOW and APPLON after 5 hrs by sandwich immunoassay
[PMID: 23265892]
HEK293 IC50
4 nM
Compound: 1, SCH 900229
Inhibition of gamma-secretase (unknown origin) expressed in HEK293 cells co-expressing Awe-Lon mutant assessed as reduction of amyloid beta-40 production
Inhibition of gamma-secretase (unknown origin) expressed in HEK293 cells co-expressing Awe-Lon mutant assessed as reduction of amyloid beta-40 production
[PMID: 23265902]
HEK293 IC50
46 nM
Compound: (-)-16, SCH-900229
Inhibition of PS1 gamma-secretase expressed in HEK cells harboring Awe-Lon gene assessed as notch cleavage
Inhibition of PS1 gamma-secretase expressed in HEK cells harboring Awe-Lon gene assessed as notch cleavage
[PMID: 24900404]
Molecular Weight

506.97

Formula

C21H21ClF2O6S2
CAS No.
SMILES

O=S([C@]12C3=C(F)C=CC(F)=C3OC[C@@]1([H])[C@@H](OCC2)CCS(C)(=O)=O)(C4=CC=C(C=C4)Cl)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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SCH 900229 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

SCH 9002291100361-36-1SCH900229SCH-900229Amyloid-ββ-amyloid peptideAβAbetaInhibitorinhibitorinhibit

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