EZH2-IN-14

• CAT Number: I042467
• CAS Number: 1979157-17-9
• Molecular Formula: C31H39N7O2
• Molecular Weight: 541.69
• Purity: ≥95%
• Synonyms: N-[(4,6-dimethyl-2-oxo-1H-pyridin-3-yl)methyl]-1-propan-2-yl-6-[6-(4-propan-2-ylpiperazin-1-yl)pyridin-3-yl]indazole-4-carboxamide
• InChI: InChI=1S/C31H39N7O2/c1-19(2)36-9-11-37(12-10-36)29-8-7-23(16-32-29)24-14-25(27-18-34-38(20(3)4)28(27)15-24)30(39)33-17-26-21(5)13-22(6)35-31(26)40/h7-8,13-16,18-20H,9-12,17H2,1-6H3,(H,33,39)(H,35,40)
• InChIKey: XHJAGCFBPKQPDU-UHFFFAOYSA-N
• SMILES: CC1=CC(=C(C(=O)N1)CNC(=O)C2=C3C=NN(C3=CC(=C2)C4=CN=C(C=C4)N5CCN(CC5)C(C)C)C(C)C)C

EZH2-IN-14 (Cat No.: I042467) is a potent and selective small-molecule inhibitor of enhancer of zeste homolog 2 (EZH2), a histone methyltransferase that catalyzes trimethylation of histone H3 at lysine 27 (H3K27me3), leading to gene silencing. Overactive EZH2 is associated with various cancers, particularly lymphomas and solid tumors. EZH2-IN-14 blocks this epigenetic repression, reactivating tumor suppressor genes and inhibiting cancer cell proliferation. It is widely used in cancer epigenetics research and as a promising lead compound for developing targeted therapies against EZH2-driven malignancies.

Reference

[1]. Anqi Ma, et al. Discovery of a first-in-class EZH2 selective degrader. Nat Chem Biol. 2020 Feb;16(2):214-222.
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