Biochem/physiol Actions

Primary TargetMidkine

Reversible: yes

Cell permeable: yes

General description

A cell-permeable imidazothiazolyl-chromenone compound that reduces cellular midkine/MDK protein level in H441 lung adenocarcinoma cells in a dose-dependent manner (by >90% in 48 h at 25 nM) via a yet unidentified mechanism. Shown to inhibit the viability of MDK-positive HEK293, H441, and H520 cells (by ≥60% at 500 nM in 48 h), but not MDK-negative NHLF or HEK293 (by ﹤15% at 500 nM in 48 h), via apoptosis induction as a result of PI 3-K/AKT signaling inhibition. Intraperitoneal injection is reported to be efficacious in retarding H441 tumor expansion in mice (9 mg/kg; 3X to 5X per wk) in vivo.

A cell-permeable imidazothiazolyl-chromenone compound that reduces cellular midkine/MDK protein level in H441 lung adenocarcinoma cells in a dose-dependent manner (by >90% in 48 h at 25 nM) via a yet unidentified mechanism, while exhibiting little effect toward cellular level of PTN or VEGF. Shown to inhibit the viability of MDK-positive HEK293, H441, and H520 cells (by ≥60% at 500 nM in 48 h), but not MDK-negative NHLF (normal human lung fibroblast) or HEK293 (by ﹤15% at 500 nM in 48 h), via apoptosis induction as a result of PI 3-K/AKT signaling, but not Erk or p38, pathway inhibition. Intraperitoneal injection is reported to be efficacious in retarding H441 tumor expansion in mice (75% vs 400% increase in tumor volume in 10 d with or without treatment; 3 to 5 times 9 mg/kg i.p. dosing per wk) in vivo.

Legal Information

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

Other Notes

Hao, H., et al. 2013. PLoS ONE8, e71093.

Packaging

Packaged under inert gas

10 mg in Glass bottle

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Warning

Toxicity: Standard Handling (A)