CRA-026440

CRA-026440 is a potent, broad-spectrum HDAC inhibitor. The K_i values against recombinant HDAC isoenzymes HDAC1, HDAC2, HDAC3, HDAC6, HDAC8, and HDAC10 are 4, 14, 11, 15, 7, and 20 nM respectively. CRA-026440 shows antitumor and antiangiogenic activities^[1]. CRA-026440 is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups. IC50 & Target:Ki: 4 nM (HDAC1), 14 nM (HDAC 2), 11 nM (HDAC3), 15 nM (HDAC6), 7 nM (HDAC8), 20 nM (HDAC10)^[1] In Vitro:CRA-026440 has antiproliferative effect on HUVEC endothelial cells with a GI₅₀ value of 1.41 μM^[1].
CRA-026440 (0.1-10 μM; 18 hours) results in the accumulation of acetylated histone and acetylated tubulin, leading to an inhibition of tumor cell growth and the induction of apoptosis^[1].
CRA-026440 (0.1-10 μM; 5 days) inhibits ex vivo angiogenesis in a dose-dependent manner^[1]. In Vivo:CRA-026440 (100 mg/kg; i.v.; daily; for three consecutive days) results in a statistically significant reduction in tumor growth in mice harboring HCT116 or U937 human tumor xenografts^[1].