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product name WS6


Description: WS6 is a β cell proliferation inducer via modulation of Erb3 binding protein-1 (EBP1) and the IκB kinase pathway. WS6 is a small-molecule inducer of β cell proliferation. In mouse β cell line R7T1, WS6 induced cell proliferation with EC50 value of 0.28 µM. WS6 was very active in primary human and rodent islets. In primary rat and human β cells, WS6 induced rat β cell proliferation with EC50 value of 0.4 µM and increased 4% of rat β cells and 3% of human β cells to proliferate.

References: J Am Chem Soc. 2013 Feb 6;135(5):1669-72.



Molecular Weight (MW)

568.59
Formula

C29H31F3N6O3
CAS No.

1421227-53-3
Storage

-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)

DMSO: 100 mg/mL (175.9 mM)
Water: <1 mg/mL
Ethanol: 100 mg/mL (175.9 mM)
Solubility (In vivo)

 
Synonyms

 

other peoduct :

In Vitro

In vitro activity: WS6 induces R7T1 cell proliferation with EC50 of 0.28 μM, and promotes β cell proliferation in rodent and human primary islets. Both Erb3 binding protein-1 and the IκB kinase pathway are confirmed to function in the mechanism of action of WS6.


Kinase Assay:


Cell Assay: 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.

In Vivo In RIP-DTA mouse model of β cell ablation, WS6 (50 mg/kg p.o.) ameliorates diabetes, and induces concomitant increases in β cell proliferation and β cell number
Animal model RIP-DTA mouse model
Formulation & Dosage 50 mg/kg; p.o.
References J Am Chem Soc. 2013 Feb 6;135(5):1669-72.

BYL-721

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Author: Sodium channel