WDR5-IN-1 is a highly selective inhibitor of WD repeat domain 5 (WDR5), demonstrating a binding affinity (Kd) of less than 0.02 nM. It effectively inhibits the MLL1 histone methyltransferase activity with an IC50 of 2.2 nM, leading to reduced MYC recruitment at WDR5-displaced genes. This compound exhibits significant anti-proliferative effects in neuroblastoma (CHP-134) and Burkitt’s lymphoma (Ramos) cell lines, making it a valuable tool for research in cancer biology and epigenetics.
WDR5-IN-1 is a highly selective inhibitor of WD repeat domain 5 (WDR5), demonstrating a binding affinity (Kd) of less than 0.02 nM. It effectively inhibits the MLL1 histone methyltransferase activity with an IC50 of 2.2 nM, leading to reduced MYC recruitment at WDR5-displaced genes. This compound exhibits significant anti-proliferative effects in neuroblastoma (CHP-134) and Burkitt’s lymphoma (Ramos) cell lines, making it a valuable tool for research in cancer biology and epigenetics.
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