An inhibitor of the Mad2-Cdc20 interaction
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M2I-1 is an inhibitor of the protein-protein interaction between the spindle assembly checkpoint protein mitotic arrest deficient 2 (Mad2) and cell division cycle 20 (Cdc20), a coactivator of the anaphase-promoting complex/cyclosome (APC/C).1 It inhibits Mad2 binding to Cdc20111-138 when used at concentrations ranging from 6.25 to 100 μM. M2I-1 (25 μM) reduces increases in mitotic duration induced by paclitaxel in HeLa cells. M2I-1 (20-120 μM) reduces 4-cell embryo and blastocyst formation in hydrogen peroxide-exposed mouse zygotes, as well as increases the rate of sex chromosome mosaicism in male mouse in vitro fertilization-derived embryos.2
1.Kastl, J., Braun, J., Prestel, A., et al.Mad2 inhibitor-1 (M2I-1): A small molecule protein-protein interaction inhibitor targeting the mitotic spindle assembly checkpointACS Chem. Biol.10(7)1661-1666(2015) 2.Huang, Y., Ha, S., Li, Z., et al.CHK1-CENP B/MAD2 is associated with mild oxidative damage-induced sex chromosome aneuploidy of male mouse embryos during in vitro fertilizationFree Radic. Biol. Med.137181-193(2019)
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