β-actin-IN-1

β-actin-IN-1 (compound C25) selectively and covalently binds to Cys272 of β-actin at an allosteric site, inhibits β-actin polymerization, and shows high selectivity for β-actin over α-actin and γ-actin^[1].
β-actin-IN-1 (0.001-100 μM; 72 h) inhibits the proliferation of osteosarcoma 143B, HOS, SJSA-1, MG63, MNNG/HOS, A549, MGC803 and HCT116 tumor cells with IC₅₀ values of 0.015, 0.042, 0.20, 0.048, 0.043, 1.2, 0.42 and 0.45 μM respectively, and it presents weaker cytotoxicity against normal HEK293T cells with an IC₅₀ of 0.23 μM, leading to a selectivity index of 15.33^[1].
β-actin-IN-1 (10-40 nM; 10 days) reduces 143B cell colony formation^[1].
β-actin-IN-1 (10-40 nM; 24 h) inhibits 143B cell migration in wound healing and transwell assays^[1].
β-actin-IN-1 (10-40 nM; 2 h) disrupts the actin cytoskeleton and reduces phalloidin-stained actin filaments in 143B cells^[1].
β-actin-IN-1 (0.1 μM) shows a T_1/2 of 3.88 min and a CL_int of 541 mL/min/g in human liver microsomes, and a T_1/2 of 1.27 min and a CL_int of 1656 mL/min/g in mouse liver microsomes^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.