BRD3308

For research use only.

Catalog No.S8962

BRD3308 Chemical Structure

CAS No. 1550053-02-5

BRD3308 is a potant and highly selective inhibitor of HDAC3 with IC50 of 54 nM, 1.26 μM and 1.34 μM for HDAC3, HDAC1 and HDAC2, respectively. BRD3308 activates HIV-1 transcription. BRD3308 suppresses pancreatic β-cell apoptosis induced by inflammatory cytokines (glucolipotoxic stress) and increases functional insulin release.

Purity & Quality Control

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Biological Activity

Description BRD3308 is a potant and highly selective inhibitor of HDAC3 with IC50 of 54 nM, 1.26 μM and 1.34 μM for HDAC3, HDAC1 and HDAC2, respectively. BRD3308 activates HIV-1 transcription. BRD3308 suppresses pancreatic β-cell apoptosis induced by inflammatory cytokines (glucolipotoxic stress) and increases functional insulin release.
Targets
HDAC3 [1]
(Cell-free assay)
HDAC1 [1]
(Cell-free assay)
HDAC2 [1]
(Cell-free assay)
54 nM 1.26 μM 1.34 μM
In vitro

BRD3308 is a derivative of the ortho-aminoanilide HDAC inhibitor CI-994 and is developed to be highly selective for inhibition of HDAC3 with an IC50 value that is 23-fold lower for HDAC3 than for HDAC1 or 22. HDAC3 selective inhibition induces expression of HIV and exposure to BRD3308 allows the recovery of latent HIV-1 from patient cells.[1]

In vivo

Selective inhibition of HDAC3 by BRD3308 prevents diabetes onset in female NOD mice. HDAC3 treatment in vivo prevents pancreatic islet infiltration and protects β-cells from apoptosis. β-cell proliferation is increased in animals treated with BRD3308. HDAC3 treatment in vivo prevents white adipose tissue infiltration in NOD mice.[2]

Protocol

Cell Research:

[1]

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  • Cell lines: 2D10 cells, J89 cells, THP89 cells, J-Lat 6.3 cells
  • Concentrations: 5 μM, 10 μM, 15 μM, 30 μM
  • Incubation Time: 6 h, 12 h, 18 h, 24 h
  • Method:

    BRD3308 (15 μM) is added to aliquots of resting CD4+ T cells which are then plated in limiting dilution replicates of 2.5 or 1 million, 0.5 million, and 0.1 million cells and incubated at 37℃ under 5% CO2. BRD3308 is removed from the cultures after 24 hours.


    (Only for Reference)
Animal Research:

[2]

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  • Animal Models: Female NOD/ShiLTJ (NOD) mice
  • Dosages: 0.1 mg/kg, 1 mg/kg, 10 mg/kg
  • Administration: IP
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 57 mg/mL (198.4 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 287.29
Formula

C15H14FN3O2

CAS No. 1550053-02-5
Storage powder
in solvent
Synonyms N/A
Smiles CC(=O)NC1=CC=C(C=C1)C(=O)NC2=C(C=C(C=C2)F)N

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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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HDAC Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID