PIM-1 HDAC-IN-1 (compound 4d) is a potent inhibitor of PIM-1, with an IC 50 of 343.87 nM. It also exhibits strong inhibitory activity and selectivity against HDAC 1 and HDAC 6, with IC 50 values of 63.65 and 62.39 nM, respectively. Furthermore, PIM-1 HDAC-IN-1 demonstrates apoptosis-inducing potential in MCF-7 cell lines, specifically inducing pre-G1 apoptosis and causing cell cycle arrest at the G2 M phase [1].
HDAC NAMPT-IN-1 (compound 39h) simultaneously inhibits HDAC and NAMPT, exhibiting IC 50 values ranging from 0.72 to 37081 nM for HDAC and 1618 nM for NAMPT [1].
NMDAR HDAC-IN-1 (Compound 9d) is a potent dual inhibitor of N-methyl-D-aspartate receptors (NMDARs) and histone deacetylases (HDACs). It exhibits a high affinity (Ki = 0.59 μM) for NMDARs, while demonstrating significant inhibitory effects on various HDAC isoforms, including HDAC1, HDAC2, HDAC3, HDAC6, and HDAC8 with IC 50 values of 2.67 μM, 8.00 μM, 2.21 μM, 0.18 μM, and 0.62 μM, respectively. Moreover, NMDAR HDAC-IN-1 efficiently crosses the blood-brain barrier [1].
TubulinHDAC-IN-1 is a compound that functions as a dual inhibitor for tubulin and HDAC-IN-1. It achieves this by interacting with tubulin through CH π interaction and with HDAC8 through hydrogen bond interaction. This compound effectively inhibits tubulin polymerization and selectively targets HDAC8 with an IC50 of 150 nM. Additionally, TubulinHDAC-IN-1 demonstrates cytotoxicity against various human cancer cells, induces cell cycle arrest in the G2 M phase, and triggers cell apoptosis. This compound is valuable for studying hematologic and solid tumors, including neuroblastoma and leukemia [1].