KDM4-IN-3

• CAT Number: I045337
• CAS Number: 1068515-53-6
• Molecular Formula: C17H14N4O
• Molecular Weight: 290.32
• Purity: ≥95%
• Synonyms: 2-(1H-benzimidazol-2-yl)-5-methyl-4-phenyl-1H-pyrazol-3-one
• InChI: InChI=1S/C17H14N4O/c1-11-15(12-7-3-2-4-8-12)16(22)21(20-11)17-18-13-9-5-6-10-14(13)19-17/h2-10,20H,1H3,(H,18,19)
• InChIKey: YNQAUNMBAVKOIN-UHFFFAOYSA-N
• SMILES: CC1=C(C(=O)N(N1)C2=NC3=CC=CC=C3N2)C4=CC=CC=C4

KDM4‑IN‑3 (Cat No.: I045337) is a small‑molecule inhibitor of the histone lysine demethylase KDM4 family (JMJD2), designed to target epigenetic regulators of histone H3 lysine 9 and 36 methylation. It has a biochemical potency with an IC₅₀ around 871 nM, exhibits good cellular permeability, and induces cytotoxicity in prostate cancer cell lines (e.g. DU‑145, LNCaP) at low micromolar concentrations (GI₅₀ ≈ 8 µM) while also elevating H3K9me₃ levels. Molecular formula C₁₇H₁₄N₄O, MW 290.32, CAS 1068515‑53‑6. It serves as a valuable research chemical probe for studying epigenetic mechanisms and exploring KDM4-targeted anticancer strategies.

Reference

[1]. Carter DM, et al. Enhanced Properties of a Benzimidazole Benzylpyrazole Lysine Demethylase Inhibitor: Mechanism-of-Action, Binding Site Analysis, and Activity in Cellular Models of Prostate Cancer. J Med Chem. 2021 Oct 14;64(19):14266-14282.
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