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Cat. No. Name Size Price Add Cart
KI2643EPZ-643825 mg$670
EPZ-643850 mg$1072
EPZ-6438100 mg$1716
EPZ-6438200 mg$2744

Chemical Characteristic

Product NameEPZ-6438
SynonymsEPZ-6438; EPZ 6438; EPZ6438.
CAS No.1403254-99-8
Molecular Weight 572.74
FormulaC34H44N4O4
Chemical NameN-[(4,6-dimethyl-2-oxo-1H-pyridin-3-yl)methyl]-3-[ethyl(oxan-4-yl)amino]-2-methyl-5-[4-(morpholin-4-ylmethyl)phenyl]benzamide
Smilesc1(cc(c(c(c1)N(C1CCOCC1)CC)C)C(=O)NCc1c(=O)[nH]c(cc1C)C)c1ccc(cc1)CN1CCOCC1
Chemical Structure

Biological activities

EPZ-6438 is a potent and selective inhibitor of EZH2. EPZ-6438 inhibits EZH2 in a manner competitive with the substrate S-adenosylme-thionine(SAM) and noncompetitive with the peptide or nucleosome substrate. EPZ-6438 inhibits the activity of human PRC2-containing wild-type EZH2 with an IC50 of 2.5 nM. In vitro, EPZ-6438 specifically inhibits cellular H3K27 methylation and leads to selective apoptotic killing of SMARCB1 mutant MRT cells. In vivo, EPZ-6438 at dose of 125 mg/kg induces tumor stasis during the administration period and produces a significant tumor growth delay.[1]

Protocols

In vitro, EPZ-6438 is dissolved in DMSO.[1]

References

[1] Sarah K, et al. Durable tumor regression in genetically altered malignant rhabdoid tumors by inhibition of methyltransferase EZH2. Proc Natl Acad Sci. 2013, 110 (19): 7922-7927.

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KareBayTM provides scientists and clinicians with a wide range of biotechnological products and science lab supplies for chemical research and analyzing life processes. KareBay's extensive capabilities include commercializing reagents and kits, manufacturing biotech products and providing contract research services to organizations worldwide. Our many global labs, offices, and business partners enable KareBay to extend its products and services to its customer base around the world.

Our products are used for research, laboratory and further evaluation purposes. They are not for human use.
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