EBI-2511 is a novel and orally available benzofuran derived EZH2 inhibitors that was discovered through a scaffold hopping approach based on the clinical compound of EPZ-6438.
MS049 (MS 049; MS-049) is a potent and selective inhibitor of protein arginine methyltransferases-PRMT4 and PRMT6 with potential antineoplastic activity.
OICR-9429 (OICR9429) is a novel, potent and selective antagonist of the interaction between WDR5 and the peptide regions of MLL and Histone 3, disrupting Wdr5-MLL interaction with IC50 of 5 uM.
This product is discontinued due to commercial reason. Tazemetostat (formerly known as EPZ-6438 or E7438; Tazverik) is an orally bioavailable, potent, and selective EZH2 (Enhancer of Zeste-Homolog 2) inhibitor with antineoplastic activity.
Entacapone (OR-611) is an approved anti-PD/Parkinson’s Disease medication acting as a specific and peripherally active catechol-O-methyltransferase (COMT) inhibitor (IC50 = 151 nM).
GSK3326595 (EPZ015938) is a novel, potent, orally bioactive, and selective inhibitor of protein arginine methyltransferase 5 (PRMT5).
MI-503 (MI503) is a novel, orally bioavailable and potent Menin-MLL interaction inhibitor (IC50= 14.7 nM) with potential anticancer activity.
UNC0642 (UNC-0642) is a novel, potent, selective, dual inhibitor of G9a/GLP (histone methyltransferases) with antitumor activity.
CMP-5 (PRMT5-IN-5) is a first-in-class and specific PRMT5 inhibitor with anticancer (B-cell lymphomas) and immunomodulatory activity.
DCLX069 (DCLX-069) is a novel, SAM-competitive and selective PRMT1 (protein arginine methyltransferase 1) inhibitor (IC50 =17.9 µM) with anticancer effects.