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Biological Activity:

BG45 is a potent, selective and cell permeable HDAC3 inhibitor. It inhibits HDAC3 with IC50 of 289 nM. It has IC50 of 2.0 µM, 2.2 µM and >20 µM for HDAC1, HDAC2, and HDAC6 in cell-free assays, respectively. BG45 triggers significant MM cell growth inhibition via apoptosis, evidenced by caspase and poly (ADP-ribose) polymerase cleavage. BG45 alone and in combination with bortezomib triggers significant tumor growth inhibition in vivo in a murine xenograft model of human MM.

How to Use:

In vitro: BG45 was used at 10 µM final concentration in various in vitro assays.
In vivo: BG45 was dosed to mice bearing MM.1S xenograft by IP injection at 50 mg/kg (5 days a week), significantly inhibits MM tumor growth. (Formulation: 10% dimethylacetamide in 10% Kolliphor HS15 in PBS)

Reference:

• 1. Minami J., et al. Histone deacetylase 3 as a novel therapeutic target in multiple myeloma. (2014) Leukemia. 28(3): 680-9.