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Eg5-I is a potent inhibitor of Eg5, both in vitro and in cells (IC50s = 127 and 190 nM, respectively).1 It is an analog of S-trityl-L-cysteine (STLC), but is more potent and has better solubility than STLC. Eg5-I blocks bipolar spindle formation and inhibits the growth of cancer cells, with an average GI50 value of 360 nM against a broad panel of tumor cells (GI50 range = 10 nM to 3 µM).1 It ranges from 140- to 1200-fold more potent against cancer cells than monastrol (Item No. 15044), which also acts by inhibiting Eg5.2,1
WARNING This product is not for human or veterinary use.
1. Synthesis and characterization of tritylthioethanamine derivatives with potent KSP inhibitory activity. Bioorg. Med. Chem. 19(18), 5446-5453 (2011).
2. Elucidating the functionality of kinesins: An overview of small molecule inhibitors. Semin. Cell Dev. Biol. 22(9), 935-945 (2011).