BAY 598 is a potent and selective competitive inhibitor of SMYD2 lysine methyltransferase, IC50 values are 27 and 58 nM for biochemical and cellular activity assays, respectively.

SMYD2:27 nM

METHODS: PDAC cells SW1990 and MIA PaCa2 were treated with BAY-598 (10 µM) and doxorubicin (1 µM) for 48 h. Cell viability was determined by MTT assay.
RESULTS: PDAC cells were highly sensitive to acute treatment with the low-dose combination of doxorubicin and BAY-598. [1]

METHODS: To detect antitumor activity in vivo, BAY-598 (50 mg/kg once daily) and gemcitabine (100 mg/kg every three days) were administered intraperitoneally to NSG mice bearing SW1990 xenografts for 27 days.
RESULTS: The combination of gemcitabine and BAY-598 attenuated the growth of SW1990 xenografts compared to monotherapy. [1]
METHODS: To assay anti-tumor activity in vivo, BAY-598 (10-100 mg/kg, PEG 400/water 8:2) was administered orally to BALB/c nude mice bearing KYSE-150 xenografts once daily for three days.
RESULTS: BAY-598 was able to inhibit SMYD2 methylation activity in tumor cells in vivo. [2]