DB-310
DB-310 is a selective immunoproteasome LMP2 inhibitor with an IC50 value of 80.62 nM. DB-310 inhibits the production of IL-1α in microglia. DB-310 improves cognitive function in the Tg2576 transgenic mouse model of Alzheimer's disease. DB-310 can be used for research related to Alzheimer's disease.
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- CAS No.: 2338531-17-0
- Formule: C30H38N6O6
- Masse moléculaire:578.66
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
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Activité biologique
Description
IC50 & Target
[1]|
IL-1α |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| RPMI-8226 | IC50 |
10000 nM
Compound: 28; DB-310
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Inhibition of LMP7/Beta 5 subunit chymotrypsin-like activity in human RPM18226 cell lysates using Suc-LLVY-AMC as substrate after 1 hr by fluorescence based microplate reader analysis
Inhibition of LMP7/Beta 5 subunit chymotrypsin-like activity in human RPM18226 cell lysates using Suc-LLVY-AMC as substrate after 1 hr by fluorescence based microplate reader analysis
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[PMID: 32189500] |
In Vitro
DB-310 (1-3 μM; 4 h) inhibits the activity of LMP2 in DLD-1/ABCB1 cells with overexpressed ABCB1, and is not a substrate of the ABCB1 efflux transporter, suggesting its potential to cross the blood-brain barrier[1].
DB-310 (3 μM; 24 h) significantly inhibits the production of IL-1α in LPS (HY-D1056)-stimulated BV-2 mouse microglia[1].
DB-310 (24 h) inhibits TNF-α-induced epithelial-mesenchymal transition in human retinal pigment epithelial cell line ARPE-19, and maintains the normal morphology and marker expression of cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:BV-2 murine microglial cells (LPS-stimulated)
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Concentration:3 μM (co-incubated with LPS)
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Incubation Time:24 h
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Result:Significantly suppressed IL-1α production in LPS-stimulated BV-2 cells.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Tg2576 mice (9-month-old)[1]
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Dosage:10 mg/kg
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Administration:i.p.; twice weekly; 3 weeks
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Result:Improved escape latency on days 3-5 and escape distance on day 5 of the Morris water maze test compared to vehicle-treated controls.
Reduced serum IL-1α levels, significantly lower than vehicle-treated controls.
Completely preserved the orderly mosaic structure of the RPE, whereas vehicle-treated mice showed severe RPE disruption.
Chemical Information
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CAS No. 2338531-17-0
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Masse moléculaire 578.66
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Formule C30H38N6O6
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SMILES
O=C([C@H]1N(CCC1)C(CNC(C2=NC=CN=C2)=O)=O)N[C@@H](CC3=CC=CC=C3)C(N[C@@H](CC(C)C)C([C@]4(CO4)C)=O)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
DB-310 Related Classifications
HY-182325 Related Classifications
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