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AP C5 is a potent and selective protein kinase G type II (PKG2) inhibitor (pIC50 = 7.2). Displays >20-fold selectivity for PKG2 over PKG1 and PKA (pIC50 values are 4.6 and 4.8 for PKG1 and PKA, respectively). Blocks 8-pCPT-cGMP-dependent VASP phosphorylation in intestinal organoids. Also attenuates toxin-stimulated anion secretory responses in mouse intestinal tissue.
AP C5 is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Kinase Inhibitor Library. Find out more about compound libraries available from Tocris.
|Storage||Store at -20°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
The following data is based on the product molecular weight 275.31. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||3.63 mL||18.16 mL||36.32 mL|
|5 mM||0.73 mL||3.63 mL||7.26 mL|
|10 mM||0.36 mL||1.82 mL||3.63 mL|
|50 mM||0.07 mL||0.36 mL||0.73 mL|
References are publications that support the biological activity of the product.
Bijvelds et al (2018) Selective inhibition of intestinal guanosine 3',5'-cyclic monophosphate signaling by small-molecule protein kinase inhibitors. J.Biol.Chem. 293 8173 PMID: 29653944
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Keywords: AP C5, AP C5 supplier, APC5, protein, kinase, g, type, 2, II, inhibitors, inhibits, guanosine, 3,5-cyclic, monophosphate, dependent, Protein, Kinase, G, 6626, Tocris Bioscience
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We developed a model system to form purified alternative pathway (AP) C5 convertases on C3b-coated beads and quantify C5 conversion via functional analysis of released C5a.
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