Chemical Structure of Gö6976.
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).
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.
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.
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).
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