WS6 is a highly potent and selective small molecule that promotes pancreatic β cell proliferation in rodent and human primary islets, identified by a high-throughput, cell-based screening using rodent pancreatic β cells. It can induce proliferation of mouse R7T1 cells with an EC₅₀ ~0.28 µM, and induce up to 4% of rat β cells and 3% of human β cells to proliferate, with a similar EC₅₀ of 0.4 μM. WS6 induces proliferation of primary rat and human β cells in intact islet format at 0.2-1.0 µM concentration. In the RIP-DTA mouse model of β cell ablation, WS6 demonstrated excellent in vivo effect on normalizing blood glucose and inducing concomitant increases in β cell proliferation and β cell number. Affinity pulldown and kinase profiling studies implicate Erb3 binding protein-1 and the IκB kinase pathway in the mechanism of action of WS6.

How to Use:

• In vitro: WS6 was used at 0.5-1 µM concentration in beta cell proliferation assays.
• In vivo: WS6 was intraperitoneally (IP) dosed to mice 5 mg/kg every other day.

Reference:

• 1. Shen W, et al. Small-Molecule Inducer of β Cell Proliferation Identified by High-Throughput Screening. (2013) J Am Chem Soc. In press.

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