EED-IN-4 

EED-IN-4 is an orally active, EZH2-selective immunomodulator and EED-H3K27me3 inhibitor (EED, IC₅₀=28.21 nM) with anti-inflammatory activity. In mouse models, EED-IN-4 preferentially and persistently accumulates in lymph nodes after oral administration. By reducing the H3K27me3 level of dendritic cells and inhibiting their migration, EED-IN-4 reduces the infiltration of immune cells into the central nervous system and effectively alleviates spinal cord inflammation. EED-IN-4 shows weak inhibitory activity against hERG channels and is non-mutagenic, with no obvious toxicity observed upon long-term oral administration. EED-IN-4 can be used for the research of multiple sclerosis^[1].

EED-IN-4 (compound 19) (5 μM; 24 h) reduces the level of H3K27me3 in DC2.4 cells by 79.94% and inhibits cell migration induced by CCL19/CCL21^[1].
EED-IN-4 only weakly inhibits hERG channel currents in stably transfected HEK293T cells, with an IC₅₀ >10 μM^[1].
EED-IN-4 exhibits high selectivity for EED over the methyltransferase activity of EZH2^[1].
EED-IN-4 shows negative results in the Mini-Ames mutagenicity assay containing Salmonella typhimurium TA100^[1].

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

EED-IN-4 (compound 19) (40-80 mg/kg; p.o.; twice daily; from day 9 to day 30 post-immunization) dose-dependently alleviates clinical symptoms of the disease, reduces the degree of inflammatory infiltration in the spinal cord, and inhibits the activation and infiltration of dendritic cells, macrophages and pathogenic T cells in peripheral lymph nodes and the central nervous system in a female C57BL/6 mouse model of experimental autoimmune encephalomyelitis (EAE)^[1].
EED-IN-4 (100 mg/kg; p.o.; twice daily; for consecutive 30 days) shows no obvious acute or subacute toxicity in the C57BL/6 mouse model (with equal numbers of male and female mice). The mice exhibit normal body weight gain, no significant abnormalities in blood routine, liver and kidney function indices, and no histopathological damage in major organs including the heart, liver, spleen, lung and kidney^[1].
EED-IN-4 (80 mg/kg; intragastric administration (i.g.); single dose) preferentially and persistently accumulates in key immune lymph nodes including axillary, inguinal and cervical lymph nodes in healthy female C57BL/6 mice, with a concentration significantly higher than that of EED226, exhibiting favorable lymphoid tissue tropism^[1].

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

389.43

C₂₂H₂₀FN₅O

CN(C)C1=CC=C(C2=CN=C(NCC3=C(F)C=CC4=C3CCO4)C=C2C#N)C=N1

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Chen Z, et al. Discovery of Novel Trisubstituted Pyridine Derivatives as EED-H3K27me3 Inhibitors for the Treatment of Multiple Sclerosis. J Med Chem. 2026;69(6):6854-6884.