HDAC-IN-35 (Compound 14) is an effective and selective inhibitor of VEGFR-2 and HDAC, with IC50 values of 13.2 and 0.166 μM for VEGFR-2 and HDAC6, respectively.

HDAC8:1.99 μM, VEGFR2:13.2 μM, HDAC1:7.23 μM, HDAC6:0.166 μM

HDAC-IN-35 (Compound 14) (0-10 μM, 48 h) shows anticancer effects in different cancer cells [1]. HDAC-IN-35 (0-10 μM, 48 h) exhibits potent anti-angiogenic activity with a GI >50 (50% growth inhibition) value of 1.0 μM on human endothelial progenitor cells (EPCs) through a VEGFR-2-dependent pathway, without obvious systemic toxicity [1]. HDAC-IN-35 exhibits moderate VEGFR-2 inhibitory activities and displays the anticancer effects by inhibiting the enzymatic activity of HDAC [1]. HDAC-IN-35 (0-10 μM, 24 h) concentration-dependently impedes the capillary-like tube formation in human EPCs [1]. Cell Viability Assay [1] Cell Line: A549, PC-3, and SK-Hep-1 Concentration: 0-10 μM Incubation Time: 48 h Result: Showed anticancer effects with IC 50 values of 3.4, 1.9 and 3.2 μM against A549, PC-3, and SK-Hep-1 cells. Western Blot Analysis [1] Cell Line: A549, PC-3, and SK-Hep-1, and human EPCs Concentration: 0, 5, and 10 μM Incubation Time: 24 h Result: Increased the amount of acetylated α-tubulin and histone H3 in a concentration-dependent manner in cancer cells. Induced mild inhibition of the phosphorylation of VEGFR-2 in human EPCs.