New Histone Methyltransferase Inhibitors

Catalog No.	Product Name	Information
E1291	SETDB1-TTD-IN-1	SETDB1‑TTD‑IN‑1 is a SETDB1 methyltransferase activator and a competitive inhibitor of the SETDB1 tandem tudor domain (SETDB1‑TTD), binding SETDB1‑TTD with a Kd of 88 nM and showing strong selectivity over other tudor and bromodomain proteins. It enhances SETDB1 catalytic activity, promoting Akt1 Lys64 methylation and subsequent Akt1 Thr308 phosphorylation and activation. By blocking SETDB1‑TTD binding to histone H3 peptides, it drives global gene‑expression changes and functions as a tool compound to study SETDB1‑TTD, including in breast cancer models.
E6689	Pociredir	Pociredir(FTX-6058) is a potent, orally bioavailable inhibitor of Embryonic Ectoderm Development (EED), a core regulatory subunit of the polycomb repressive complex 2 (PRC2). By disrupting this epigenetic mechanism, the compound downregulates key fetal globin repressors to robustly induce fetal hemoglobin (HbF) protein expression in both cellular and murine models.
≡ All Histone Methyltransferase Inhibitors