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EPZ-6438

Cat. No. M2677

EPZ-6438 Structure

Synonym: E7438

Size Price Availability Quantity
10mg USD 80 In stock
50mg USD 190 In stock
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Quality Control
Biological Activity

EPZ-6438 is a potent, and selective EZH2 inhibitor with Ki and IC50 of 2.5 nM and 11 nM, exhibiting a 35-fold selectivity versus EZH1 and >4,500-fold selectivity relative to 14 other HMTs.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 572.74
Formula C34H44N4O4
CAS Number 1403254-99-8
Purity >99%
Solubility DMSO 10 mg/mL
Storage at -20°C
Related EZH2 Products
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CPI-169 racemate is the racemate form of CPI-169, which is a novel and potent EZH2 inhibitor with IC50 <1 nM(inhibition of the catalytic activity of PRC2); decreases cellular levels of H3K27me3 with an EC50 of 70 nM, and triggers cell cycle arrest and apoptosis in a variety of cell lines.

GSK343

GSK343 is a potent and selective EZH2 inhibitor with IC50 of 4 nM, showing 60 fold selectivity against EZH1, and >1000 fold selectivity against other histone methyltransferases.

EPZ005687

EPZ005687 is a potent and selective inhibitor of EZH2 with Ki of 24 nM, 50-fold selectivity against EZH1 and 500-fold selectivity against 15 other protein methyltransferases.

GSK126

GSK126 is a potent, highly selective, S-adenosyl-methionine-competitive, small-molecule inhibitor of EZH2 methyltransferase activity.

  Catalog
Abmole Inhibitor Catalog 2017




Keywords: EPZ-6438, E7438 supplier, EZH2, inhibitors

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