Home Proteases Secretase inhibitor Compound 11 For research use only.

Compound 11

Compound 11, a non-toxic and selective δ-secretase inhibitor (IC50=0.7 μM, in fluorescence-based assay) that interacts with both the active site and allosteric site of δ-secretase in Co-crystal structure analysis. The IC50 value of the compound 11 towards δ-secretase in Pala cells is 0.8 μM.

Compound 11 Chemical Structure

Compound 11 Chemical Structure

CAS No. 842964-18-5

Purity & Quality Control

Batch: E036301 DMSO]44 mg/mL]false]Ethanol]4 mg/mL]false]Water]Insoluble]false Purity: 99.07%
99.07

Compound 11 Related Products

Biological Activity

Description Compound 11, a non-toxic and selective δ-secretase inhibitor (IC50=0.7 μM, in fluorescence-based assay) that interacts with both the active site and allosteric site of δ-secretase in Co-crystal structure analysis. The IC50 value of the compound 11 towards δ-secretase in Pala cells is 0.8 μM.
Targets
Secretase [1]
(in fluorescence-based assay)		 δ-secretase [1]
(in Pala cells assay)
0.7 μM 0.8 μM
In vitro
In vitro

Compound 11 inhibit δ-secretase in Pala cells, with an IC50 of 7 μM. Compounds 11 is highly permeable assessed by Caco-2 monolayer permeability screen. The human liver microsomal stability screen demonstrates that following 30 min of incubation, 76% of compound 11 remained in human liver microsomes.[1]
Cell Research Cell lines Pala cells, HepG2 cells
Concentrations 24 h
Incubation Time 50 μM
Method

Cells are incubated with various concentrations of compound 11 with the Pala cells for 2 h at 37 °C. Cells are collected, washed twice with PBS and lysed in Lysis Buffer. The protein concentrations are normalized via a Bradford assay and lysates are assayed with 5 μM Cbz-Ala-Ala-Asn-AMC.
In Vivo
In vivo

Chronic treatment with δ-secretase inhibitor 11 markedly decreases the brain asparaginyl endopeptidase (AEP) activity, reduces the generation of Aβ1-40/42 and ameliorates memory loss. The inhibition of AEP with this reagent not only reduces the AEP-cleaved tau fragments and tau hyperphosphorylation, but also attenuates neuroinflammation in the form of microglial activation. Treatment with δ-secretase inhibitor 11 prevents the synaptic loss and alleviated dendritic disruption in senescence-accelerated mouse prone 8 (SAMP8) mouse brain.[2]
Animal Research Animal Models senescence-accelerated mouse prone 8 (SAMP8) mice
Dosages 10 mg/kg
Administration o.g.

Chemical Information & Solubility

Molecular Weight 220.23 Formula

C10H12N4O2
CAS No. 842964-18-5 SDF --
Smiles NC1=CC=C(N2CCOCC2)C3=NON=C13
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 44 mg/mL ( (199.79 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 4 mg/mL

Water : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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