AP-C5

• CAT Number: I014788
• CAS Number: 2234272-10-5
• Molecular Formula: C16H13N5
• Molecular Weight: 275.31
• Purity: ≥95%
• Synonyms: 4-(4-imidazol-1-ylphenyl)-N-prop-2-ynylpyrimidin-2-amine
• InChI: InChI=1S/C16H13N5/c1-2-8-18-16-19-9-7-15(20-16)13-3-5-14(6-4-13)21-11-10-17-12-21/h1,3-7,9-12H,8H2,(H,18,19,20)
• InChIKey: QKHQFSQJQKGFAA-UHFFFAOYSA-N
• SMILES: C#CCNC1=NC=CC(=N1)C2=CC=C(C=C2)N3C=CN=C3

AP-C5 displays selective inhibition of guanosine 3′,5′-cyclic monophosphate (cGMP)-dependent protein kinase II (cGKII) with a pIC50 of 7.2, which can be used for the research of diarrheal disease[1]. AP-C5 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
AP-C5 shows potent inhibition of cGMP-dependent cGKII-mediated protein phosphorylation and effective inhibition of cGMP-dependent, CFTR-mediated anion secretion in intestinal tissue[1].
AP-C5 potentiates cAMP signaling by PDE inhibition[1].
AP-C5 (20 μM) partially blocks the heat-stable toxin (STa)-mediated short-circuit current (Isc) response in mouse ileum[1].

Reference

[1]. Marcel J C Bijvelds, et al. Selective inhibition of intestinal guanosine 3′,5′-cyclic monophosphate signaling by small-molecule protein kinase inhibitors. J Biol Chem. 2018 May 25;293(21):8173-8181.
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