WS6, a β cell proliferation inducer, regulates Erb3 binding protein-1 (EBP1) and the IκB kinase pathway.

Proliferation (β cells):0.28 μM

In the RIP-DTA mouse model with β-cell ablation, oral administration of WS6 (50 mg/kg) promotes β-cell proliferation, thereby ameliorating diabetes.

In R7T1 cells (EC50=0.28 μM), WS6 induces cell proliferation through the action on the Erb3 binding protein-1 and IκB kinase signaling pathways.

PARP assays are conducted in a buffer containing 50 mM Tris (pH 8.0), 1 mM DTT, 1.5 μM [3H]NAD+?(1.6 μCi/mmol), 200 nM biotinylated histone H1, 200 nM slDNA, and 1 nM PARP-1 or 4 nM PARP-2 enzyme. Reactions are terminated with 1.5 mM benzamide, transferred to streptavidin Flash plates, and counted using a TopCount microplate scintillation counter.

R7T1 cells are growth-arrested by removal of doxycycline for 2 days and plated into 384-well plates at a density of 3,000 cells/well in growth medium. Β cell proliferation is assessed using CellTiter Glo after 4 days. Fold increase in cell number is calculated by normalizing compound-treated wells to the median of DMSO-treated wells. (Only for Reference)