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.
CAS Number: 926259-99-6
Molecular Weight: 214.22
Chemical Name: N-(2-aminophenyl)pyrazine-2-carboxamide
Appearance: Solid Power.
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO up to 100 mM
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined.
HS Tariff Code: 382200
How to use
BG45 was used at 10 µM final concentration in various in vitro assays.
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)
- Minami J., et al. Histone deacetylase 3 as a novel therapeutic target in multiple myeloma. (2014) Leukemia. 28(3): 680-9.
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