Mitosis Inhibitor, AK301

A cell permeable piperazine derivative that induces irreversible mitotic arrest in colon cancer cells (IC₅₀ = 115 nM in HT29 cells) and increases their sensitivity to TNF-induced apoptosis (EC₅₀ = 172 nM). Also shown to enhance FasL and TRAIL-induced caspase-3 activity in colon cancer cells. Binds to the chochicine-binding domain on b-tubulin with high affinity, although in a different orientation than cholchicine, and reduces tubulin polymerization with formation of multiple microtubule organizing centers with Aurora kinase A and g-tubulin. Induces G2/M arrest in both HT29 colon cancer cells and WI38 lung fibroblasts, however, this effect is more pronounced in cancer cells.

Cell permeable: yes

Primary Target
tubulin

Reversible: yes

Packaged under inert gas

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

Chopra, A. S., et al. 2013. J. Bio. Chem.289, 2978.

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

Toxicity: Standard Handling (A)