ZLD1039 is a highly selective and orally bioavailable inhibitor of the EZH2 enzyme, targeting its role in the polycomb repressive complex 2 (PRC2). This compound demonstrates potent inhibition of PRC2 enzymatic activity against both wild-type and mutant EZH2 variants, with IC50 values of 5.6 nM for wild-type, 15 nM for Y641F, and 4.0 nM for A677G. ZLD1039 has been shown to inhibit breast tumor growth and metastasis, making it a valuable tool for research in cancer biology and therapeutic exploration.
ZLD1039 is a highly selective and orally bioavailable inhibitor of the EZH2 enzyme, targeting its role in the polycomb repressive complex 2 (PRC2). This compound demonstrates potent inhibition of PRC2 enzymatic activity against both wild-type and mutant EZH2 variants, with IC50 values of 5.6 nM for wild-type, 15 nM for Y641F, and 4.0 nM for A677G. ZLD1039 has been shown to inhibit breast tumor growth and metastasis, making it a valuable tool for research in cancer biology and therapeutic exploration.
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