CPI-1205 Inhibitor

CPI-1205 is a highly potent and selective inhibitor of EZH2(IC50 : 0.002uM, EC50 : 0.032uM) .

Vaswani RG, et al. Identification of (R)-N-((4-Methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-2-methyl-1-(1-(1-(2,2,2-trifluoroethyl)piperidin-4-yl)ethyl)-1H-indole-3-carboxamide (CPI-1205), a Potent and Selective Inhibitor of Histone Methyltransferase EZH2, Suitable for Phase I Clinical Trials for B-Cell Lymphomas. J Med Chem. 2016 Nov 10;59(21):9928-9941.
Vaswani RG, et al. Identification of (R)-N-((4-Methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-2-methyl-1-(1-(1-(2,2,2-trifluoroethyl)piperidin-4-yl)ethyl)-1H-indole-3-carboxamide (CPI-1205), a Potent and Selective Inhibitor of Histone Methyltransferase EZH2, Suitable for Phase I Clinical Trials for B-Cell Lymphomas. J Med Chem. 2016 Nov 10;59(21):9928-9941.
Gulati N, Beguelin, Wendy, Giulino-Roth L. Enhancer of zeste homolog 2 (EZH2) inhibitors[J]. Leukemia & Lymphoma, 2018:1-12.
Gulati N, Beguelin, Wendy, Giulino-Roth L. Enhancer of zeste homolog 2 (EZH2) inhibitors[J]. Leukemia & Lymphoma, 2018:1-12.

Small volumes of CPI-1205, inhibitor vial(s) may occasionally become entrapped in the seal of the product vial during shipment and storage. If necessary, briefly centrifuge the vial on a tabletop centrifuge to dislodge any liquid in the container`s cap. Certain products may require to ship with dry ice and additional dry ice fee may apply.

MBS5759303 is an inhibitor targeting CPI-1205.