EED-IN-5 

EED-IN-5 is an orally active, EZH2-selective trisubstituted pyridine-based EED-H3K27me3 inhibitor and immunomodulator with anti-inflammatory activity. The IC₅₀ value of EED-IN-5 against EED is 28.21 nM. In mouse models, EED-IN-5 preferentially and persistently accumulates in lymph nodes after oral administration. By reducing the H3K27me3 level of dendritic cells and inhibiting their migration, EED-IN-5 decreases the infiltration of specific dendritic cells, macrophages and T cells into the spinal cord and brain. EED-IN-5 exhibits hERG inhibitory activity, shows negative results in the Mini-Ames test, and causes no obvious toxicity upon long-term high-dose administration. EED-IN-5 can be used for the research of multiple sclerosis^[1].

EED-IN-5 (compound 21) (5 μM; 24 h) reduces the level of H3K27me3 in DC2.4 cells by 60.64% and inhibits CCL19/CCL21-induced cell migration^[1].
EED-IN-5 inhibits hERG channel currents in stably transfected HEK293T cells, with an IC₅₀ of 1.2 μM^[1].
EED-IN-5 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-5 (compound 21) (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 the experimental autoimmune encephalomyelitis (EAE) model of female C57BL/6 mice^[1].
EED-IN-5 (100 mg/kg; p.o.; twice daily; for consecutive 30 days) shows no obvious acute or subacute toxicity in the C57BL/6 mouse model (equal numbers of male and female mice). The mice exhibit normal weight gain, no significant abnormalities in routine blood test results and liver and kidney function indices, and no histopathological damage to major organs including the heart, liver, spleen, lung, and kidney^[1].
EED-IN-5 (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.

403.45

C₂₃H₂₂FN₅O

N#CC1=CC(NCC2=C(F)C=CC3=C2CCO3)=NC=C1C4=CN=C(CN(C)C)C=C4

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.