BAY-6035 / Bayer - LARVOL DELTA

Discovery of the SMYD3 Inhibitor BAY-6035 Using Thermal Shift Assay (TSA)-Based High-Throughput Screening. (PubMed, SLAS Discov) - "Moreover, we describe a congeneric negative control to BAY-6035. In summary, BAY-6035 is a novel selective and potent SMYD3 inhibitor probe that will foster the exploration of the biological role of SMYD3 in diseased and nondiseased tissues."

Journal • Oncology • FLT1 • HER-2 • SMYD3

POTENTIAL SYNERGY OF EPIGENETIC MODIFIERS WITH TYROSINE KINASE INHIBITORS IN FLT3-ITD AML (ASPHO 2019) - "...The epigenetic probes were then studied in combination with a TKI (Quizartinib- AC220) over a 72-hour period...A 35-70% decrease in cell proliferation was noted with certain bromodomain inhibitors (GSK6853, L-Moses), lysine methyl-transferase inhibitors (Bay 598, Bay6035), EZH2/H1 inhibitors (GSK343, UNC1999) and PRMT inhibitors (MSO23, SGC707) when used in combination with low dose TKI compared to no or minimal inhibitory effect when these inhibitors were used without a TKI. These preliminary findings support the need to confirm epigenetic target inhibition in FLT3-ITD leukemia and further investigate cellular mechanism of effects such as apoptosis, cell cycle and differentiation. Additionally the effect of combination therapy of TKI and epigenetic agent will need to be evaluated in patient samples as well as on FLT3-ITD leukemia initiating cells in vitro and in vivo."