MAK-683

Alternative_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
Description

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).
CAS Number

1951408-58-4
Structure Available

Yes
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
Tag Line

aApotent EED (embryonic ectoderm development protein) inhibitor
Storage Condition

-20°C
Shipping Condition

gel pack
Shelf Life

36 months
PubChem CID

121412508
PubChem CID Link
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
Data Sheet Link
MSDS Available

Yes

Identity

HGNC:17574
Gene

ALPK3
Long gene name

alpha kinase 3
Synonyms
- MAK
- KIAA1330
- Midori
Synonyms name
- myocyte induction differentiation originator
- muscle alpha-kinase
GenBank acession
- AY044449
Locus

15q25.3
Discovery year

2004-12-01
Entrez gene record

57538
Pubmed identfication
- 10021370
RefSeq identity
- NM_020778
Classification
- I-set domain containing
VEGA ID

OTTHUMG00000148667