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 cyt
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Product Description
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.
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.
