HLC40

HLC40 potently inhibits MLL1 histone methyltransferase activity in in vitro cell-free biochemical assay with an IC₅₀ of 0.82 μM^[1].
HLC40 potently and selectively inhibits proliferation of MV4-11 and MOLM-13 MLL-rearranged AML cells with IC₅₀ values of 8.92 μM and 7.07 μM, respectively, while showing minimal activity against MLL wild-type K562 cells (IC₅₀ = 49.68 μM)^[1].
HLC40 exhibits minimal antagonistic activity against the CysLT1 receptor in stable HEK-293 cells, with an IC₅₀ = 5.28 μM^[1].
HLC40 (2.5-10 μM; 72 h) induces concentration-dependent apoptosis in MV4-11 and MOLM-13 MLL-rearranged AML cells, with apoptosis rates reaching up to 30.31% in MV4-11 cells at 10 μM^[1].
HLC40 (0.625-10 μM; 24 h) activates the apoptotic pathway in MOLM-13 MLL-rearranged AML cells, as shown by concentration-dependent upregulation of cleaved caspase-3^[1].
HLC40 (0.625-10 μM; 24 h) suppresses global H3K4 mono-, di-, and trimethylation in a concentration-dependent manner in MOLM-13 MLL-rearranged AML cells^[1].
HLC40 (20 μM; 2 h) directly engages intracellular WDR5 in MOLM-13 MLL-rearranged AML cells, as evidenced by pronounced thermal stabilization of WDR5 at temperatures up to 61°C^[1].
HLC40 (10 μM; 24 h) disrupts WDR5-mediated transcriptional activation in MV4-11 MLL-rearranged AML cells, suppressing proliferative programs and upregulating negative cell cycle regulators^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.