EML741 is a selective inhibitor of the histone methyltransferases G9a and GLP, characterized by an IC50 value of 23 nM for G9a and a Kd of 1.13 μM. Additionally, EML741 inhibits DNMT1 with an IC50 of 3.1 μM while demonstrating no significant effect on DNMT3a or DNMT3b. This compound exhibits low cytotoxicity, is membrane permeable, and is capable of crossing the blood-brain barrier, making it a valuable tool for epigenetic research and potential therapeutic applications.
EML741 is a selective inhibitor of the histone methyltransferases G9a and GLP, characterized by an IC50 value of 23 nM for G9a and a Kd of 1.13 μM. Additionally, EML741 inhibits DNMT1 with an IC50 of 3.1 μM while demonstrating no significant effect on DNMT3a or DNMT3b. This compound exhibits low cytotoxicity, is membrane permeable, and is capable of crossing the blood-brain barrier, making it a valuable tool for epigenetic research and potential therapeutic applications.
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