An inhibitor of PRC2-mediated trimethylation of H3K27
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MAK-683

Item No. 29316

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[(5-fluoro-2,3-dihydro-4-benzofuranyl)methyl]-8-(2-methyl-3-pyridinyl)-1,2,4-triazolo[4,3-c]pyrimidin-5-amine
CAS Number
1951408-58-4
Molecular Formula
C20H17FN6O
Formula Weight
376.4
Purity
≥98%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
DMSO: 15 mg/ml
λmax
298 nm
SMILES
FC1=CC=C(OCC2)C2=C1CNC3=NC=C(C4=C(C)N=CC=C4)C5=NN=CN35
InChi Code
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
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    1 mg

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    10 mg

    $653

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    Cayman Chemical
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    Product Description

    MAK-683 is an inhibitor of trimethylation of histone 3 lysine 27 (H3K27) by polycomb repressive complex 2 (PRC2), a complex that includes embryonic ectoderm development protein (EED).1 MAK-683 has an IC50 value of 5.9 nM in an EED-H3K27me3 peptide competition binding assay and inhibits H3K27 trimethylation in G401 cells (IC50 = 2.6 nM). It inhibits proliferation of KARPAS422 B cell lymphoma cells with an IC50 value of 3 nM.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Chan, H.M., Gu, X.-J., Huang, Y., et al. Triazolopyrimidine compounds and uses thereof. (2016).