Information
BRD3308 is a potant and highly selective inhibitor ofHDAC3with 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 (Cell-free assay); HDAC1 (Cell-free assay); HDAC2 (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.
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.
Cell Research(from reference)
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
G2203117