A cell-permeable pyrazole compound that is shown to prevent
in vitro tubulin polymerization (IC
50 = 0.2 μM) by targeting Colchicine (Cat. No.
234115) binding site (Kd = 0.3 μM) in cell-free assays and induce blebs formation in HUVEC cultures by perturbing both tubulin microtubles and actin cytoskeleton structures. Unrelated to its effects on actin and tubulin filaments, XRP44X is also reported to block the activations of Ras and its downstream effector molecules, such as Raf, MEK, Erk, Rsk, and Net (Elk-3/SAP-2/Erp), upon FGF-2 (Cat. No.
341595) stimulation. Potently inhibits the growth of HUVEC, NIH3T3, as well as 9 other cancer cell lines in antiproliferation assays (IC
50 ≤11.3 nM).
