WS6, β Cell Proliferation Inducer


Catalog No. size PriceQuantity
M60097-2D 10 mM DMSO (0.352 mL) $139
M60097-2S 2mg solid $139
M60097-10S 10mg solid $549

Description

Product Information
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.

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