Gap Junction Enhancer, PQ7

A cell-permeable quinoline derived compound with low toxicity that enhances gap junctional activity by about 16-fold (at ~500 nM) in T47D breast cancer cells and thereby potentiates the effect of chemotherapeutic agents. Blocks T47D cell colony formation (IC₅₀ = 100 nM) and reduce the growth of T47D xenograft tumors by 100% in Nu/Nu mice. Increases caspase-3, - 8, and -9 expression by 1.6, 2.8, and 3.8-fold, respectively to induce apoptotic cell death. Can work synergistically with cisplatin to reduce or totally eliminate tumor growth. Increases the expression of connexins 26, 32, and 43 to allow more efficient trafficking of cisplatin.

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.

Shishido, S.N., et al. 2013. PLos One.8, e67174.
Shishido, S.N., et al. 2012. PLos One.7,e444963.
Heiniger, B., et al. 2010. Anticancer Res.30, 3927.
Shi, A., et al. 2008. Bioor. Med. Chem. Lett.18, 3364.

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

Toxicity: Standard Handling (A)