Biological Activity
YTHDC1 inhibitor 40 is a potent, selective m6A reader YTHDC1 inhibitor with ITC Kd of 49 nM, HTRF IC50 of 0.35 uM. Compound 40 shows antiproliferative activity against the acute myeloid leukemia (AML) cell lines THP-1, MOLM-13, and NOMO-1.YTHDC1 inhibitor 40 exhibits antiproliferative activity against THP-1 (GI50 = 3.2 μM), MOLM-13 (5.6 μM) and NOMO-1 (8.2 μM), respectively. YTHDC1 inhibitor 40 displays IC50 values of 89, 60, and 83 μM against YTHDF1, YTHDF2, and YTHDF3, respectively, indicating a 200-fold selectivity.YTHDC1 inhibitor 40 does not display significant inhibition of a panel of 58 protein kinases.YTHDC1 inhibitor 40 (2.5-10 uM) induces apoptosis in THP-1 cell line after 24 h treatment.YTHDC1 inhibitor 40 is a tool compound for studying the role of YTHDC1 in AML.
In Vitro
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In Vivo
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References & source
[1]. František Zálešák, et al. Structure-Based Design of a Potent and Selective YTHDC1 Ligand. J Med Chem. 2024 Jun 13;67(11):9516-9535.
Published experimental findings depend on the model and assay conditions. They do not guarantee equivalent performance in every application. For laboratory research use only.