DNMT/HDAC-IN-1 (Compound 15a) is a dual DNMT and HDAC inhibitor with IC50 values of 56.84 nM for HDAC1 and 17.39 nM for HDAC6. DNMT/HDAC-IN-1 can induce apoptosis and is useful in tumor research.

HDAC6:17.39 nM, HDAC1:56.84 nM

DNMT/HDAC-IN-1 significantly inhibited proliferation of K562 and U937 with IC50 values of 2.85 mM and 1.06 mM, respectively. [1] In Western Blot Analysis, U937 cells treated with 0, 1, 2.5, and 5 μM for 12 hours showed increased acetylation of histone H3K9 and H4K8 and elevated P16 expression. In Apoptosis Analysis, U937 cells treated with 2.5, 5, and 10 μM for 36 hours exhibited induced apoptosis.

In an animal model using female BALB/c wild-type mice [2], a dosage of 50 mg/kg was administered intravenously daily for 21 days, resulting in inhibited tumor growth.