Stemcell, 100-1645, A-485

Influence gene expression and reduce cell growth in a variety of cancers with A-485, a selective, competitive inhibitor (IC50 = 60 nM) of the histone acetyltransferases p300 and CREB-binding protein (CBP). p300 and CBP regulate transcription by acetylating the histone tail or by functioning as transcriptional co-activators. A-485 selectively binds to the catalytic active site of p300 and competes with acetyl-coenzyme A to inhibit p300 activity (Lasko et al. Nature, 2017). The inhibitory effect of A-485 on histone acetylation is most pronounced on histone H3 lysine 18 (H3K18) and lysine 27 (H3K27) sites (Weinert et al. Cell, 2018).

A-485 has been used for:

CANCER RESEARCH

· Reduce cell growth, growth hormone secretion and expression of key oncogenes in mouse pituitary adenoma cells in vitro and in a mouse xenograft model (Ji et al. J Clin Endocrinol Metab, 2022).

· Inhibit human breast cancer cell growth by disrupting estrogen receptor function (Waddell et al. Cancers (Basel), 2021).

· Induce senescence through reactive oxygen species production to activate autophagy pathway, resulting in cell growth arrest of human lung cancer cells (Ansari et al. Cancer Gene Ther, 2023).

· Induce apoptosis and differentiation of mouse leukemia stem cells and delay leukemia progression in a mouse acute myeloid leukemia model (Pan et al. Blood Adv, 2023).