ALKBH1-IN-16

ALKBH1-IN-16 is a cell-permeant hydroxamate analog that effectively competes with α-KG to suppress ALKBH1 (KD = 3.27 µM and IC50 = 1.696 µM), a DNA demethylase. By engaging ALKBH1, ALKBH1-IN-16 prevents its interaction with DNA, increasing N6-Methyladenine (6mA) levels in cellular DNA and mimicking the effects of ALKBH1 suppression on gene regulation and signaling. Furthermore, ALKBH1-IN-16 inhibits the growth of U251 brain cancer cells (IC50 = 12.92 µM) and, at higher doses, targets COX-2, HDAC2, and HDAC7 (IC50 = 1.45, 8.74, and 18.62 µM, respectively), showcasing its wider inhibitory impact on enzymes linked to inflammation and gene expression.