| Molecular Weight: | 568.59 |
| Formula: | C29H31F3N6O3 |
| Purity: | ≥ 98% |
| CAS#: | 1421227-53-3 |
| Solubility: | DMSO up to 100 mM |
| Chemical Name: | N-(6-(4-(2-((4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)amino)-2-oxoethyl)phenoxy)pyrimidin-4-yl)cyclopropanecarboxamide |
| Storage: | Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year. |
Biological Activity:
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.
Products are for research use only. Not for human use.
