1. Metabolic Enzyme/Protease Immunology/Inflammation
  2. Proteasome Interleukin Related
  3. 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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DB-310

DB-310 Chemical Structure

CAS No. : 2338531-17-0

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Description

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[1].

IC50 & Target[1]

IL-1α

 

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.

ELISA Assay[1]

Cell Line: BV-2 murine microglial cells (LPS-stimulated)
Concentration: 3 μM (co-incubated with LPS)
Incubation Time: 24 h
Result: Significantly suppressed IL-1α production in LPS-stimulated BV-2 cells.
In Vivo

DB-310 (10 mg/kg; i.p.; twice weekly; 3 weeks) improves cognitive function, reduces serum IL-1α levels, and preserves RPE structural integrity in Tg2576 Alzheimer's disease mice[1].

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

Animal Model: Tg2576 mice (9-month-old)[1]
Dosage: 10 mg/kg
Administration: i.p.; twice weekly; 3 weeks
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.
Molecular Weight

578.66

Formula

C30H38N6O6

CAS No.
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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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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  • 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.

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Product Name:
DB-310
Cat. No.:
HY-182325
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