tcsc1521 Resminostat

Resminostat is a potent inhibitor of HDAC1, HDAC3 and HDAC6, with mean IC₅₀ values of 42.5, 50.1, 71.8 nM, respectively, and shows less potent activities against HDAC8, with an IC₅₀ of 877 nM.

IC50 & Target: IC50: 42.5 nM (HDAC1), 50.1 nM (HDAC3), 71.8 nM (HDAC6), 877 nM (HDAC8)^[1]

In Vitro: Resminostat hydrochloride (Resminostat [HCl], 5 μM) induces histone acetylation in myeloma cells. Resminostat hydrochloride displays a substrate competitive binding mode with a mean K_i value of 27 nM. Resminostat hydrochloride (5 μM) induces histone hyperacetylation in myeloma cells. Resminostat inhibits cell growth, induces apoptosis and inhibits MM cell proliferation. Resminostat (5 μM) also modulates expression of bcl-2 family proteins and inhibits Akt pathway signalling downstream of Akt. Resminostat exerts synergistic activity against myeloma cells when combined with common and new anti-myeloma agents^[1]. Resminostat inhibits cell growth in head and neck squamous cell carcinoma cell lines, with IC₅₀s ranging from 0.775 μM to 1.572 μM (IC₅₀ for SCC25: 0.775 μM; CAL27: 1.572 μM; and FaDu: 0.899 μM). Resminostat (1.25 and 2.5 μM) has a synergistic effect with irradiation on HNSCC cell lines. Resminostat in combination with cisplatin induces a downregulation of survivin. However, Resminostat shows no effect on Mcl-1 and p-AKT expression^[2]. Resminostat reduces viability of HCC cells with the co-treatment of AZD-2014, with IC₅₀s ranging from 0.89 ± 0.12 μM to 0.07 ± 0.01 μM^[3].