MC4455

MC4455 (Compound 1a) potently inhibits the LSD1/CoREST and PRMT5/MEP50 complex with IC₅₀ values of 0.104, 0.014 μM and shows high selectivity over PRMT1 and PRMT7 in cell-free biochemical assays^[1].
MC4455 increases the protein unfolding temperature of LSD1/CoREST complex by 8.4°C^[1].
MC4455 engages both PRMT5 and LSD1 in MV4-11 human AML cells, and reduces SDMA and increased H3K4me2 levels^[1].
MC4455 (50 nM; 3 days) recapitulates the transcriptomic and splicing changes of combined PRMT5 and LSD1 inhibition in MV4-11 human AML cells, including activation of myeloid differentiation pathways and suppression of proliferation-associated pathways^[1].
MC4455 (6 days) promotes myeloid differentiation of MV4-11 human AML cells, increasing CD11b-positive cell levels more effectively than single-agent or combination PRMT5/LSD1 inhibition, and increasing CD68-positive cell levels comparably to combination treatment^[1].

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