Description
BG45 is an HDAC class I inhibitor with selectivity for HDAC3 (IC50 = 289 nM). It inhibits HDAC1, HDAC2, and HDAC6 with greatly reduced potency (IC50s = 2, 2.2, and >20 μM, respectively). At concentrations up to 50 mg/kg, BG45 alone or in combination with bortezomib has been shown to dose-dependently inhibit tumor growth in a mouse model of multiple myeloma.
Uses
BG45 acts as an HDAC class I inhibitor with selectvity for HDAC3. HDACs represent novel targets for anti-tumer drugs treating various cancers including multiple myeloma cancer.
Definition
ChEBI: N-(2-aminophenyl)-2-pyrazinecarboxamide is an aromatic amide.
in vitro
bg45 is reported as an hdac class i inhibitor with selectivity for hdac3 over hdac1, 2. consistent with hdac3 knockdown data, bg45 significantly inhibited mm cell growth dose-dependently. importantly, bg45 also triggered a potent growth inhibitory effect against patient-derived mm cells, without affecting normal donor pbmcs [1].
in vivo
bg45 significantly inhibited mm tumor growth in a dose-dependent fashion. for example, significant differences were observed in control versus bg45 15 mg/kg, control versus bg45 50 mg/kg, and bg45 15 mg/kg versus bg45 50 mg/kg at day 22. moreover, bg45 50 mg/kg in combination with bortezomib enhanced either single agent activity further. these results confirmed that bg45 triggers in vivo anti-mm activities [1].
References
[1] minami j, suzuki r, mazitschek r, gorgun g, ghosh b, cirstea d, hu y, mimura n, ohguchi h, cottini f, jakubikova j, munshi nc, haggarty sj, richardson pg, hideshima t, anderson kc. histone deacetylase 3 as a novel therapeutic target in multiple myeloma. leukemia. 2014 mar;28(3):680-9.
