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.
For research use only. We do not sell to patients.
- CAS No.: 2338531-17-0
- Formula: C30H38N6O6
- Molecular Weight:578.66
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
IC50 & Target
[1]|
IL-1α |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| 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. Further protocols information, click here.
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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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Molecular Weight 578.66
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Formula 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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Protocol for Water Maze
The Morris Water Maze is a rodent spatial learning and memory assay in which a mouse or rat swims in opaque water to find an escape platform; in the hidden-platform version, the animal cannot see the platform and must use distal extra-maze cues to learn its fixed spatial location. The assay primarily measures hippocampus-dependent spatial learning during acquisition trials and spatial reference memory during probe trials after platform removal; readouts include escape latency, swim path length, swim speed, quadrant occupancy, platform-site crossings, and proximity to the former platform location.
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How to Choose the Right Model Animal
Choosing the right model animal is a validity-driven decision in which the species, strain, sex, age, genetic background, disease-induction method, outcome measures, and welfare burden must match the scientific question rather than laboratory tradition or convenience. A model should be selected by judging face validity, construct validity, and predictive validity: whether it resembles the human phenotype, whether it reproduces relevant mechanisms, and whether results are likely to predict human biology or treatment response. Animal studies often fail to translate because of species differences, weak disease resemblance, poor experimental design, inadequate reporting, publication bias, and underuse of randomization, blinding, and sample-size justification. Unresolved questions include how to rank competing models objectively, how much human-disease complexity must be reproduced for a given objective, and when non-animal systems such as organoids, ex vivo tissue, or computational models
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Alzheimer’s Disease Modeling
Alzheimer’s Disease (AD) is a neurodegenerative disorder characterized by a progressive decline in cognitive functions and loss of specific types of neurons and synapses. Alzheimer's symptoms can be simulated in mice by injecting drugs (such as Aβ) or genetically modified.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)