BACH2 inhibitor compound 8 is a potent, dual BACH2/BACH1 inhibitor.
Compound 8 inhibits BACH1/2 cellular activity with EC50 of 2.28 uM by Hmox1 ELISA assay in HepG2 cells, which express Bach1, but no Bach2.
Compound 8 has EC50 of in 1.7 uM in Bach1 knockout Hap1 cells, which then only express Bach2 (Supplemental Figure 12, J Clin Invest. 2021 Dec 15;131(24):e153876.).
Compound 8 lowered glycemia and increased plasma insulin levels in diabetic mice, and restored insulin secretion in diabetic mice and human islets.
