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.
CAS Number: 1421227-53-3
Molecular Weight: 568.59
Chemical Name: N-(6-(4-(2-((4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)amino)-2-oxoethyl)phenoxy)pyrimidin-4-yl)cyclopropanecarboxamide
Appearance: Solid Power.
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO up to 100 mM
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined.
HS Tariff Code: 382200
How to use
WS6 was used at 0.5-1 µM concentration in beta cell proliferation assays.
WS6 was intraperitoneally (IP) dosed to mice 5 mg/kg every other day.
- 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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