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HDAC8/BRPF1-IN-1 (Compound 23a) is a dual inhibitor of HDAC8 and BRPF1 with an IC50 of 443 nM against human HDAC8 and a Kd of 67 nM against human BRPF1. HDAC8/BRPF1-IN-1 shows low in vitro activity against HDAC1 and 6[1].

hHDAC8: 443 nM (IC₅₀); hBRPF1: 67 nM (Ki)

[1] Ghazy E, et al. Design, synthesis, and biological evaluation of dual targeting inhibitors of histone deacetylase 6/8 and bromodomain BRPF1. Eur J Med Chem. 2020 Aug 15;200:112338. DOI:10.1016/j.ejmech.2020.112338