Gö6976 #12060

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:

378.43 g/mol

Purity:

>99%

Molecular Formula:

C₂₄H₁₈N₄O

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.