2. Neuronal Signaling Metabolic Enzyme/Protease
  3. Beta-secretase Cathepsin Amyloid-β
  4. NB-533

NB-533 is an orally active and brain-penetrant BACE-1 inhibitor with a human IC50 of 0.002 μM. NB-533 also inhibits human cathepsin D with an IC50 of 0.001 μM. NB-533 inhibits amyloidogenic amyloid precursor protein (APP) processing and reduces Aβ40 release. NB-533 reduces brain levels of APP metabolite C99 and Aβ40 in transgenic mice. NB-533 can be used for the research of Alzheimer’s disease.

For research use only. We do not sell to patients.

NB-533

NB-533 Chemical Structure

CAS No. : 1146544-18-4

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NB-533 Related Antibodies

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Cathepsin B Cathepsin C Cathepsin D Cathepsin E Cathepsin K Cathepsin L Cathepsin S

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Description

NB-533 is an orally active and brain-penetrant BACE-1 inhibitor with a human IC50 of 0.002 μM. NB-533 also inhibits human cathepsin D with an IC50 of 0.001 μM. NB-533 inhibits amyloidogenic amyloid precursor protein (APP) processing and reduces Aβ40 release. NB-533 reduces brain levels of APP metabolite C99 and Aβ40 in transgenic mice. NB-533 can be used for the research of Alzheimer’s disease[1].

IC50 & Target[1]

BACE1

0.002 μM (IC50)

Cathepsin D

0.001 μM (IC50)

Cellular Effect
Cell Line Type Value Description References
CHO IC50
24 μM
Compound: 14, NB-533
Inhibition of BACE1 expressed in CHO cells expressing human recombinant APP assessed as amyloid beta40 aggregation
Inhibition of BACE1 expressed in CHO cells expressing human recombinant APP assessed as amyloid beta40 aggregation
[PMID: 19195887]
In Vitro

NB-533 potently inhibits human BACE-1 enzyme with an IC50 of 0.002 μM[1].
NB-533 inhibits Aβ40 release from human APP-transfected CHO cells with an IC50 of 0.024 μM[1].
NB-533 inhibits human cathepsin D with an IC50 of 0.001 μM[1].
NB-533 has an efflux ratio (BA/AB) of 9.4 in MDCK mdr1a cells, showing reduced P-glycoprotein susceptibility[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

NB-533 Related Antibodies
In Vivo

NB-533 (100 μmol/kg; p.o.; double-dose at 0 and 3 h) significantly reduces forebrain C99 by 20% and CSF Aβ40 by 26% in APP51/16 transgenic mice[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: APP51/16 transgenic mice (expressing wild-type human APP under a brain-specific promoter)[1]
Dosage: 100 μmol/kg
Administration: p.o.; at 0 and 3 hours
Result: Reached brain levels of 0.53 μmol/kg, with no detectable effect on measured endpoints.
Reached brain levels of 1.5 μmol/kg, resulting in a significant 20% reduction in forebrain C99 and a significant 26% reduction in CSF Aβ40; no significant reduction in brain Aβ40 was observed.
Molecular Weight

557.81

Formula

C33H55N3O4
CAS No.
SMILES

O[C@@H]([C@@]1([H])NC([C@@H](N(C(CCCCCCCC[C@H](C1)C)=O)C)C)=O)CN[C@@H]2C3=CC(C(C)C)=CC=C3OC(C)(C2)C
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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NB-533 Related Classifications

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This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2
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:

NB-5331146544-18-4NB533NB 533Beta-secretaseCathepsinAmyloid-βBACEβ-Secretase β-amyloid peptideAβAbetatransgenic miceBACE-1CHO cellsAPPC99MDCK mdr1a cellsalzheimer’s diseaseamyloid precursor proteinAβ40cathepsin DInhibitorinhibitorinhibit

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