HD-TAC7 is a potent PROTAC HDAC degrader with IC50 values of 3.6 μM, 4.2 μM and 1.1 μM for HDAC1, HDAC2 and HDAC3, respectively. HD-TAC7 can decreases NF-κB p65 in RAW 264.7 macrophages. HD-TAC7 can be used for the research of inflammatory diseases like asthma and chronic obstructive pulmonary disease (COPD).
HD-TAC7 (10 μM; 24 hours) induces an increase of H3K27 acetylation in RAW 264.7 macrophages[1].
HD-TAC7 (10 μM; 2-48 hours) induces HDAC3 degradation reaching the maximal effect at 6h and lasted at least 48h[1].
HD-TAC7 (1 and 10 μM; 24 hours) downregulates NF-κB p65 in LPS-treated RAW 264.7 macrophages[1].
References:
[1]. Fangyuan Cao, et al. Induced protein degradation of histone deacetylases 3 (HDAC3) by proteolysis targeting chimera (PROTAC). Eur J Med Chem. 2020 Dec 15;208:112800.