Catalog No.: PC-22834Not For Human Use, Lab Use Only.
XMD8-92 a specific small-molecule inhibitor of Big mitogen-activated protein kinase 1 (BMK1, ERK5) with Kd of 80 nM, IC50 of 1.5 uM in cell-free assays.
XMD8-92 a specific small-molecule inhibitor of Big mitogen-activated protein kinase 1 (BMK1, ERK5) with Kd of 80 nM, IC50 of 1.5 uM in cell-free assays. XMD8-92 weakly inhibits TNK1 (IC50 = 10 μM) and ACK1 (aka TNK2, IC50 = 18 μM), does not inhibit MEK5, TNK1 and PLK4. XMD8-92 (1 uM) effectively blocks growth factor-induced activation of cellular BMK1, but not the structurally similar ERK1/2 in HeLa cells. XMD8-92 dramatically reduced the BMK1-dependent transactivating activity of MEF2C, a known substrate for BMK1. XMD8-92 shows anti-tumor effect by blocking tumor cell proliferation and tumor-associated angiogenesis, through promyelocytic leukemia protein (PML).
