An EZH2 inhibitor
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Zeprumetostat

Item No. 44976

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[(1,2-dihydro-4,6-dimethyl-2-oxo-3- pyridinyl)methyl]-5-ethyl-6-[ethyl(tetrahydro-2H-pyran-4-yl)amino]- 2-(1-piperidinylmethyl)-4-benzofurancarboxamide
CAS Number
2098545-98-1
Synonyms
  • SHR2554
Molecular Formula
C32H44N4O4
Formula Weight
548.7
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
Acetonitrile: Slightly Soluble: 0.1-1 mg/ml
SMILES
CC(NC1=O)=CC(C)=C1CNC(C2=C3C(OC(CN4CCCCC4)=C3)=CC(N(CC)C5CCOCC5)=C2CC)=O
InChi Code
InChI=1S/C32H44N4O4/c1-5-25-28(36(6-2)23-10-14-39-15-11-23)18-29-26(17-24(40-29)20-35-12-8-7-9-13-35)30(25)32(38)33-19-27-21(3)16-22(4)34-31(27)37/h16-18,23H,5-15,19-20H2,1-4H3,(H,33,38)(H,34,37)
InChi Key
YLZVNQZYAYVUCW-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $149

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    5 mg

    $335

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    10 mg

    $447

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    Product Description

    Zeprumetostat is an inhibitor of enhancer of zeste homolog 2 (EZH2; IC50 = 0.87 nM for the wild-type enzyme).1 It is selective for EZH2 over a panel of 24 histone and DNA methyltransferases (IC50s = >10,000 nM for all) but also inhibits EZH1 (IC50 = 19.1 nM). Zeprumetostat also inhibits the EZH2 mutants EZH2Y641C, EZH2Y641F, EZH2Y641N, EZH2Y641S, and EZH2Y641G (IC50s = 16.8, 2.68, 1.79, 5.07, and 1.13 nM, respectively). It reduces the levels of trimethylated lysine 27 on histone H3 (H3K27Me3) in Pfeiffer diffuse large B cell lymphoma (DLBCL) cells (IC50 = 1.63 nM) and induces cell cycle arrest at the G1phase and apoptosis in the same cells. Zeprumetostat (60 and 120 mg/kg), in combination with HBI 8000 (chidamide; Item No. 13686), reduces tumor growth in patient-derived xenograft (PDX) mouse models of DLBCL.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Wang, X., Wang, D., Ding, N., et al. The synergistic anti-tumor activity of EZH2 inhibitor SHR2554 and HDAC inhibitor chidamide through ORC1 reduction of DNA replication process in diffuse Large B Cell lymphoma. Cancers (Basel) 13(17), 4249 (2021).