Biochem/physiol Actions

Reversible: yes

Cell permeable: yes

General description

A cell permeable, glucose-derived diversity oriented synthesized compound that acts as reversible inducer of PDX1 expression in human PANC-1 cells, primary human islets, and human duct derived cells in a dose-and time-dependent manner with maximal effect observed on day 9 at 5 µM. Its action is dependent on the presence of FOXA2 in cells as FOXA2 knockdown cells treated with this compound do not exhibit any effect on PDX1 expression. Shown to increase H3 acetylation and H3K4me3 and reduce H3K9me3, which is consistent with its transcriptional activation of PDX1. Prolonged treatment of PANC-1 cells (9 days) increases the expression of insulin mRNA and proteins levels. Does not affect cell number and does not influence apoptotic cell death in PANC-1 cells.

A cell permeable, glucose-derived diversity oriented synthesized compound that acts as reversible inducer of PDX1 expression in human PANC-1 cells, primary human islets, and human duct derived cells in a dose-and time-dependent manner with maximal effect observed on day 9 at 5 µM. Its action is dependent on the presence of FOXA2 in cells as FOXA2 knockdown cells treated with this compound do not exhibit any effect on PDX1 expression. Shown to increase H3 acetylation and H3K4me3 and reduce H3K9me3, which is consistent with its transcriptional activation of PDX1. Prolonged treatment of PANC-1 cells (9 days) increases the expression of insulin mRNA and proteins levels. Does not affect cell number and does not influence apoptotic cell death in PANC-1 cells.Please note that the molecular weight for this compound is batch-specific due to variable water content.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Other Notes

Yuan, Y., et al. 2013. Chem. Bio.20, 1513.

Packaging

5 mg in Glass bottle

Packaged under inert gas

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C. Unstable in DMSO.

Warning

Toxicity: Standard Handling (A)