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13621
SB216763
Activators & Inhibitors
Chemical Modulators

SB216763 #13621

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SB216763: Image 1
Western blot analysis of extracts from 293T cells, untreated (-) or treated with SB216763 (4 hr) at the indicated concentrations, using Non-phospho (Active) β-Catenin (Ser33/37/Thr41) (D13A1) Rabbit mAb #8814 (upper), β-Catenin (D10A8) XP® Rabbit mAb #8480 (middle), or β-Actin (D6A8) Rabbit mAb #8457 (lower).
SB216763: Image 2
Chemical structure of SB216763.

Product Usage Information

SB216763 is supplied as a lyophilized powder. For a 25 mM stock, reconstitute the 5 mg in 538.8 µl DMSO. Working concentrations and length of treatment can vary depending on the desired effect, but it is typically used at 5-25 µM for 3-24 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 371.2 g/mol
Purity >98%
Molecular Formula C19H12Cl2N2O2
CAS 280744-09-4
Solubility Soluble in DMSO at 24mg/ml.

Background

The maleimide derivative SB216763 is a potent and selective cell permeable inhibitor of glycogen synthase kinase 3 (GSK-3). Research studies using peptide-based protein kinase assays show that SB216763 inhibits GSK-3α in an ATP competitive manner with an IC50 of 34 nM, and is an equally effective GSK3-β inhibitor. Similar assays demonstrate that SB216763 (at concentrations up to 10 µM) does not inhibit as many as 24 other serine/threonine and tyrosine protein kinases (1). As a consequence of inhibiting GSK-3, SB216763 stimulates glycogen synthesis in human liver cells (EC50 3.6 µM) via glycogen synthase activation and induces expression of a β-catenin regulated reporter gene in HEK293 cells (1). Furthermore, SB216763 induces accumulation of β-catenin, a key downstream effector in the Wnt signaling pathway, in many cell types (2-5). Additional research indicates that SB216763 can prevent neuronal cell death induced by PI3 kinase pathway inhibition (2). Glycogen synthase kinase 3 inhibitors such as SB216763 can be important research tools in studying the functional role of GSK-3 in cell signaling pathways.
  1. Coghlan, M.P. et al. (2000) Chem Biol 7, 793-803.
  2. Cross, D.A. et al. (2001) J Neurochem 77, 94-102.
  3. Piazza, F. et al. (2010) BMC Cancer 10, 526.
  4. Zhou, F. et al. (2011) Mol Biol Cell 22, 3533-40.
  5. Gebhardt, R. et al. (2010) J Cell Mol Med 14, 1276-93.

Limited Uses

Except as otherwise expressly agreed in a writing signed by a legally authorized representative of CST, the following terms apply to Products provided by CST, its affiliates or its distributors. Any Customer's terms and conditions that are in addition to, or different from, those contained herein, unless separately accepted in writing by a legally authorized representative of CST, are rejected and are of no force or effect.

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's 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's 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.
Cell Signaling Technology is a trademark of Cell Signaling Technology, Inc.
XP is a registered trademark of Cell Signaling Technology, Inc.
To Purchase # 13621S
Product # Size Price
13621S
5 mg $ 111