MC4455 

MC4455 is a LSD1/PRMT5 dual inhibitor. MC4455 inhibits the LSD1/CoREST and PRMT5/MEP50 complex with IC₅₀ values of 0.104 μM and 0.014 μM. MC4455 covalently binds to LSD1’s FAD cofactor, stabilizes the LSD1/CoREST complex. MC4455 induces myeloid differentiation, alters transcriptomic profiles, drives alternative splicing changes, and impairs leukemic cell viability in AML cells. MC4455 can be used for the research of acute myeloid leukemia^[1].

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.

457.57

C₂₇H₃₁N₅O₂

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• [1]. Param NJ, et al. A synergistic interaction between PRMT5 and LSD1 inhibitors in AML. Sci Adv. 2026;12(13):eaea4059.  [Content Brief]