BG45 is an HDAC I type inhibitor with IC50 of 289 nM, 2.0 μM, 2.2 μM and >20 μM for HDAC3/1/2/6 in cell-free assays, respectively.

HDAC3:289 nM, HDAC2:2.2 μM, HDAC1:2 μM

BG45显著抑制多种MM细胞的生长，并诱导依赖于caspase的凋亡。在RPMI8226细胞中，BG45与bortezomib协同增强细胞毒性。[1]

在携带人类MM细胞株MM.1S异种移植物的小鼠中，BG45（50 mg/kg，腹腔注射）显著抑制MM肿瘤生长。当与硼替佐米联用时，BG45（50 mg/kg，腹腔注射）增强了硼替佐米引发的细胞毒性。[1]

Kinase assays: Initial rate constants are measured at 21 °C in the presence of 100 mM HEPES (pH 7.5), 0.3 mg/mL poly(Glu-Tyr) peptide substrate, 10 mM MgCl2, 1 mg/mL bovine serum albumin, 5% DMSO, 20 nM MET-KD and various concentrations of ATP and SGX523. Total reaction volumes (20 μL) are quenched with 20 μL Kinase-Glo detection buffer. Luminescence is detected in a plate-reading luminometer and the results are analyzed by nonlinear regression.

The growth inhibitory effects of BG45 in MM cell lines are assessed by measuring 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrasodium bromide (MTT) dye absorbance. To measure proliferation of MM cells, the rate of DNA synthesis is measured by [3H]thymidine uptake.(Only for Reference)