HDAC-IN-52 is a pyridine-containing HDAC inhibitor, with IC50s of 0.189, 0.227, 0.440 and 0.446 μM for HDAC1, HDAC2, HDAC3, and HDAC10, respectively. HDAC-IN-52 can be used for the research of cancer.
HDAC-IN-52 (compound 8f) (72 hours) inhibits the proliferation of HCT116, A549 and K562 cells, with IC50s of 0.43, 1.28, and 0.37 μM, respectively[1].HDAC-IN-52 (1-5 μM; 24-48 h) induces remarkable leukaemia U937 cell death after 48 h, with 76% and 100% pre-G1 phase arrest, respectively[1].HDAC-IN-52 (1-5 μM; 48 h) increases mRNA expression of p21, BAX and BAK, downregulated cyclin D1 and BCL-2[1].
References:
[1]. Bello ED, et, al. Novel pyridine-containing histone deacetylase inhibitors strongly arrest proliferation, induce apoptosis and modulate miRNAs in cancer cells. Eur J Med Chem. 2022 Dec 15;247:115022.