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12060
Gö6976
Activators & Inhibitors
Chemical Modulators

Gö6976 #12060

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Gö6976: Image 1

Chemical Structure of Gö6976.

Gö6976: Image 2

Western blot analysis of extracts from Jurkat cells, serum-starved overnight and untreated or treated with TPA #4174 (100 nM, 15 min) either with or without Gö6976 pretreatment (1 hr) at the indicated concentrations, using Phospho-SAPK/JNK (Thr183/Tyr185) (81E11) Rabbit mAb #4668 (upper) or SAPK/JNK (56G8) Rabbit mAb #9258 (lower).

Product Usage Information

Gö6976 is supplied as a lyophilized powder. For a 1 mM stock, reconstitute the 500 µg in 1.32 ml DMSO. Working concentrations and length of treatment can vary depending on the desired effect, but it is typically used as a pretreatment at 0.1-10 µM for 0.5-1 hr prior to treating with a stimulator or is used alone with varying treatment times lasting up to 24 hr. Soluble in DMSO at 25 mg/ml; very poorly soluble in ethanol and water with maximum solubility in water at ~1-5 µM.

Storage

Store lyophilized or in solution at -20ºC, desiccated. Protect from light. 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 378.4 g/mol
Purity

>99%

Molecular Formula

C24H18N4O

CAS 136194-77-9
Solubility Soluble in DMSO at 25mg/ml.

Background

Gö6976 is an ATP-competitive PKC inhibitor specific for Ca2+-dependent PKCα (IC50 = 2.3 nM) and PKCβ1 (IC50 = 6.2 nM) isozymes (1). It is also a potent inhibitor of PKD (IC50 = 20 nM) (2). Researchers have demonstrated that Gö6976 blocks JNK activation (3-5) and inhibits PKCα-mediated, TPA-stimulated phosphorylation of CREB at Ser133 (6,7). Gö6976 is also an effective inhibitor of the tyrosine kinases Jak2 and FLT3 (8), as well as TrkA and TrkB (9).

  1. Martiny-Baron, G. et al. (1993) J Biol Chem 268, 9194-7.
  2. Gschwendt, M. et al. (1996) FEBS Lett 392, 77-80.
  3. López-Bergami, P. et al. (2005) Mol Cell 19, 309-20.
  4. Wen, J. et al. (2011) J Neuroinflammation 8, 38.
  5. Lemonnier, J. et al. (2004) J Biol Chem 279, 259-64.
  6. Chung, Y.W. et al. (2011) J Biol Chem 286, 29681-90.
  7. Paruchuri, S. and Sjölander, A. (2003) J Biol Chem 278, 45577-85.
  8. Grandage, V.L. et al. (2006) Br J Haematol 135, 303-16.
  9. Behrens, M.M. et al. (1999) J Neurochem 72, 919-24.

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.
To Purchase # 12060S
Product # Size Price
12060S
500 µg $ 184