MAK-683

MAK-683 is a potent inhibitor of embryonic ectoderm development protein (EED) and allosteric inhibitor of polycomb repressive complex 2 (PRC2), with potential antineoplastic activity. Upon administration, 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).

Product information

CAS Number: 1951408-58-4

Molecular Weight: 376.39

Formula: C20H17FN6O

Synonym:

EED inhibitor-1

MAK-683

MAK 683

MAK683

EED inhibitor 1

EED inhibitor1

Chemical Name: 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

Smiles: CC1=NC=CC=C1C1=CN=C(NCC2=C(F)C=CC3OCCC2=3)N2C=NN=C21

InChiKey: XLIBABIFOBYHSV-UHFFFAOYSA-N

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)

Technical Data

Appearance: Solid Power.

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: Soluble in DMSO

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

References:

1. Chan, Ho Man, et al. TRIAZOLOPYRIMIDINE COMPOUNDS AND USES THEREOF. US20160176882 A1.
2. Huang D, et al. Binding Modes of Small-Molecule Inhibitors to the EED Pocket of PRC2. Chemphyschem. 2020 Feb 4;21(3):263-271.

Products are for research use only. Not for human use.