MAK-683 | B1972

MAK-683 is a potent EED (embryonic ectoderm development protein) inhibitor and an allosteric inhibitor of polycomb repressive complex 2 (PRC2), with potential antineoplastic activity. MAK683 selectively binds to the domain of EED that interacts with trimethylated lysine 27 on histone 3 (H3K27me3), which leads to a conformational change in the EED H3K27me3-binding pocket and prevents the interaction of EED with the histone methyltransferase enhancer zeste homolog 2 (EZH2).

MAK-683 is a potent EED (embryonic ectoderm development protein) inhibitor and an allosteric inhibitor of polycomb repressive complex 2 (PRC2), with potential antineoplastic activity. MAK683 selectively binds to the domain of EED that interacts with trimethylated lysine 27 on histone 3 (H3K27me3), which leads to a conformational change in the EED H3K27me3-binding pocket and prevents the interaction of EED with the histone methyltransferase enhancer zeste homolog 2 (EZH2).

B1972 | MAK-683 DataSheet

Alternate Name/Synonyms: N-[(5-fluoro-2,3-dihydro-1-benzofuran-4-yl)methyl]-8-(2-methylpyridin-3-yl)-[1,2,4]triazolo[4,3-c]pyrimidin-5-amine

Appearance: Crystalline solid

Formulation: N/A

CAS Number: 1951408-58-4

Structure Available?: Yes

Peptide sequence: N/A

Salt Form: No

Molecular Formula: C₂₀H₁₇FN₆O

Molecular Weight: 376.39

Cell-Permeable?: Yes

Purity: ≥98% by HPLC

Solubilities: DMSO (~15 mg/ml)

Handling: Protect from air and light

Country of Origin: USA

Tag Line: aApotent EED (embryonic ectoderm development protein) inhibitor

MDL Number: N/A

PubChem CID: 121412508

SMILES: CC1=C(C=CC=N1)C2=CN=C(N3C2=NN=C3)NCC4=C(C=CC5=C4CCO5)F

InChi: InChI=1S/C20H17FN6O/c1-12-13(3-2-7-22-12)16-10-24-20(27-11-25-26-19(16)27)23-9-15-14-6-8-28-18(14)5-4-17(15)21/h2-5,7,10-11H,6,8-9H2,1H3,(H,23,24)

InChi Key: XLIBABIFOBYHSV-UHFFFAOYSA-N