193551-00-7

CAY10398 is an inhibitor of histone deacetylase (HDAC1) with an IC₅₀ value of 10 μM. Similar potency is observed with trapoxin A and B, whereas trichostatin A is more potent inhibitor of the enzyme. Trichostatin A also selectively inhibits the removal of acetyl groups from the amino-terminal lysine residues of core histones, which modulates the access of transcription factors to the underlying genomic DNA. However, trichostatin A is much more expensive than CAY10398. CAY10398 thus represents a selective and cost-effective compound for the inhibition of HDAC.

A histone deacetylase (HDAC1) inhibitor

[1] STACY W. REMISZEWSKI. Inhibitors of Human Histone Deacetylase: Synthesis and Enzyme and Cellular Activity of Straight Chain Hydroxamates[J]. Journal of Medicinal Chemistry, 2002, 45 4: 753-757. DOI: 10.1021/jm015568c
[2] SYBILLE WITTICH. Effect of inhibitors of histone deacetylase on the induction of cell differentiation in murine and human erythroleukemia cell lines.[J]. Anti-Cancer Drugs, 2005, 16 6: 635-643. DOI: 10.1097/00001813-200507000-00008
[3] NANIKA COETZEE. Epigenetic inhibitors target multiple stages of Plasmodium falciparum parasites.[J]. ACS Applied Electronic Materials, 2020: 2355. DOI: 10.1038/s41598-020-59298-4