Resminostat (RAS2410; 4SC-201) is a potent inhibitor ofHDAC1,HDAC3andHDAC6, with meanIC₅₀values of 42.5, 50.1, 71.8 nM, respectively, and shows less potent activities againstHDAC8, with anIC₅₀of 877 nM.

Resminostat (RAS2410; 4SC-201; 5 μM) induces histone acetylation in myeloma cells. Resminostat hydrochloride displays a substrate competitive binding mode with a mean K_ivalue 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 (IC₅₀for 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].

349.40

C₁₆H₁₉N₃O₄S

864814-88-0

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