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66244
GSK343
Activators & Inhibitors
Chemical Modulators

GSK343 #66244

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GSK343: Image 1
Western blot analysis of extracts from HeLa cells, untreated (-) or treated with GSK343 (48 hr) at the indicated concentrations, using Tri-Methyl-Histone H3 (Lys27) (C36B11) Rabbit mAb #9733 (upper) and Histone H3 (D1H2) XP® Rabbit mAb #4499 (lower).
GSK343: Image 2
Chemical structure of GSK343.

Product Usage Information

GSK343 is supplied as a lyophilized powder. For a 5 mM stock, reconstitute the 1 mg in 369.21 μl DMSO. Working concentrations and length of treatment can vary depending on the desired effect, but it is typically used at 5 nM-5 μM for 2-48 hr.

Storage

Store lyophilized or in solution at -20ºC, desiccated. In lyophilized form, the chemical is stable for 24 months. Once in solution, use within 3 months to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.

Product Description

Molecular Weight 541.7 g/mol
Purity >98%
Molecular Formula C31H39N7O2
CAS 1346704-33-3
Solubility Soluble in DMSO at 15mg/ml and EtOH at 2mg/ml.

Background

GSK343 inhibits EZH2 and EZH1 histone-lysine N-methyltransferase activity through competitive inhibition of the cofactor S-Adenosyl-l-methionine (SAM). IC50 values for EZH2 and EZH1 are 4 nM and 60 nM, respectively (1). Research studies show that GSK343 displays more than 1000-fold selectivity relative to other methyltransferases (1,2). These studies demonstrate that GSK343 induces cancer cell autophagy and enhances the anti-cancer effects of the multi-kinase inhibitor, sorafenib (3).
  1. Konze, K.D. et al. (2013) ACS Chem Biol 8, 1324-34.
  2. Amatangelo, M.D. et al. (2013) Cell Cycle 12, 2113-9.
  3. Liu, T.P. et al. (2015) Anticancer Drugs 26, 139-47.

Limited Uses

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Products are labeled with For Research Use Only or a similar labeling statement and have not been approved, cleared, or licensed by the FDA or other regulatory foreign or domestic entity, for any purpose. Customer shall not use any Product for any diagnostic or therapeutic purpose, or otherwise in any manner that conflicts with its labeling statement. Products sold or licensed by CST are provided for Customer as the end-user and solely for research and development uses. Any use of Product for diagnostic, prophylactic or therapeutic purposes, or any purchase of Product for resale (alone or as a component) or other commercial purpose, requires a separate license from CST. Customer shall (a) not sell, license, loan, donate or otherwise transfer or make available any Product to any third party, whether alone or in combination with other materials, or use the Products to manufacture any commercial products, (b) not copy, modify, reverse engineer, decompile, disassemble or otherwise attempt to discover the underlying structure or technology of the Products, or use the Products for the purpose of developing any products or services that would compete with CST products or services, (c) not alter or remove from the Products any trademarks, trade names, logos, patent or copyright notices or markings, (d) use the Products solely in accordance with CST Product Terms of Sale and any applicable documentation, and (e) comply with any license, terms of service or similar agreement with respect to any third party products or services used by Customer in connection with the Products.

For Research Use Only. Not For Use In Diagnostic Procedures.
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To Purchase # 66244
Cat. # Size Qty. Price
66244S
1 mg
$ 80