WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 406263
CAS#: 1396772--26-1
Description: EPZ005687 is a potent inhibitor of EZH2 (K(i) of 24 nM). EPZ005687 has greater than 500-fold selectivity against 15 other protein methyltransferases and has 50-fold selectivity against the closely related enzyme EZH1. The compound reduces H3K27 methylation in various lymphoma cells; this translates into apoptotic cell killing in heterozygous Tyr641 or Ala677 mutant cells, with minimal effects on the proliferation of wild-type cells.
MedKoo Cat#: 406263
Name: EPZ-005687
CAS#: 1396772--26-1
Chemical Formula: C32H37N5O3
Exact Mass: 539.28964
Molecular Weight: 539.66788
Elemental Analysis: C, 71.22; H, 6.91; N, 12.98; O, 8.89
EPZ005687, purity > 98%, is in stock. The same day shipping out after order is received.
Synonym: EPZ005687; EPZ 005687; EPZ-005687; EPZ5687; EPZ-5687; EPZ 5687.
IUPAC/Chemical Name: 1-cyclopentyl-N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-6-(4-(morpholinomethyl)phenyl)-1H-indazole-4-carboxamide.
InChi Key: ZOIBZSZLMJDVDQ-UHFFFAOYSA-N
InChi Code: InChI=1S/C32H37N5O3/c1-21-15-22(2)35-32(39)28(21)18-33-31(38)27-16-25(17-30-29(27)19-34-37(30)26-5-3-4-6-26)24-9-7-23(8-10-24)20-36-11-13-40-14-12-36/h7-10,15-17,19,26H,3-6,11-14,18,20H2,1-2H3,(H,33,38)(H,35,39)
SMILES Code: O=C(C1=CC(C2=CC=C(CN3CCOCC3)C=C2)=CC4=C1C=NN4C5CCCC5)NCC6=C(C)C=C(C)NC6=O
The following data is based on the product molecular weight 539.66788 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
1: Knutson SK, Wigle TJ, Warholic NM, Sneeringer CJ, Allain CJ, Klaus CR, Sacks JD, Raimondi A, Majer CR, Song J, Scott MP, Jin L, Smith JJ, Olhava EJ, Chesworth R, Moyer MP, Richon VM, Copeland RA, Keilhack H, Pollock RM, Kuntz KW. A selective inhibitor of EZH2 blocks H3K27 methylation and kills mutant lymphoma cells. Nat Chem Biol. 2012 Nov;8(11):890-6. doi: 10.1038/nchembio.1084. Epub 2012 Sep 30. PubMed PMID: 23023262.
