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SYN-3050-M001 1 mg INQ
SYN-3050-M005 5 mg INQ
SYN-3050-M010 10 mg INQ
SYN-3050-M050 50 mg INQ
SYN-3050-M100 100 mg INQ
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Product Data
Synonyms 1-Cyclopentyl-N-[(1,2-dihydro-4,6-dimethyl-2-oxo-3-pyridinyl)methyl]-6-[4-(4-morpholinylmethyl)phenyl]-1H-indazole-4-carboxamide
Formula C32H37N5O3
MW 539.7
CAS 1396772-26-1
Purity ≥95%
Appearance Solid.
Solubility Soluble in DMSO.
Origin Manufactured by SynKinase.
Other Product Data Target: EZH2 | Kinase Group: N/A | Substrate: N/A

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Our product description may differ slightly from the original manufacturers product datasheet.
Product Type Chemical
Shipping and Handling
Shipping AMBIENT
Short Term Storage +4°C
Long Term Storage -20°C
Use/Stability Stable for at least 2 years after receipt when stored at -20°C.
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Product Description

EPZ005687 is a potent and selective inhibitor of the lysine methyltranferase EZH2, the enzymatic subunit of polycomb repressive complex 2 (PRC2) with Ki of 24nM. It acts competitively with the EZH2 substrate S-adenosylmethionine. EPZ005687 has greater than 500-fold selectivity against 15 other protein methyltransferases and has 50-fold selectivity against EZH1. It blocks trimethylation of the PRC2 target histone 3 lysine 27 (IC50=80nM), decreasing the proliferation of lymphoma cells carrying mutant, but not wild-type, EZH2.

Product References

  1. A selective inhibitor of EZH2 blocks H3K27 methylation and kills mutant lymphoma cells: S.K. Knutson, et al.; Nat. Chem. Biol. 8, 890 (2012)
  2. Targeting EZH2-mediated methylation of H3K27 inhibits proliferation and migration of Synovial Sarcoma in vitro: J.K. Shen, et al.; Sci. Rep. 6, 25239 (2016)
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