Other Activators of PKG

  • 8- (2- Aminoethylthio)guanosine- 3', 5'- cyclic monophosphate ( 8-AET-cGMP )
  • N1- Aminoguanosine- 3', 5'- cyclic monophosphate ( 1-NH2-cGMP )
  • N2- (6- Aminohexyl)guanosine- 3', 5'- cyclic monophosphate ( 2-AH-cGMP )
  • 8- (2- Aminophenylthio)guanosine- 3', 5'- cyclic monophosphate ( 8-APT-cGMP )
  • 2- Aminopurine riboside- 3', 5'- monophosphate ( 2-NH2-cPuMP )
  • β- (4- Azidophenyl)- 1, N2- etheno- 8- bromoguanosine- 3', 5'- cyclic monophosphate ( 4-N3-PET-8-Br-cGMP )
  • 8- (2- [ Biotinyl]aminoethylthio)guanosine- 3', 5'- cyclic monophosphate ( 8-[Biotin]-AET-cGMP )
  • N2- (6- [ Biotinyl]aminohexyl)guanosine- 3', 5'- cyclic monophosphate ( 2-[Biotin]-AH-cGMP )
  • 8- Bromo- ß- phenyl- 1, N²- ethenoguanosine- 3', 5'-cyclic monophosphate ( 8-Br-PET-cGMP )
  • 8- Bromoguanosine- 3', 5'- cyclic monophosphate ( 8-Br-cGMP ), economy grade
  • 8- Bromoguanosine- 3', 5'- cyclic monophosphate ( 8-Br-cGMP ), fluorescence grade
  • 8- (4- Chlorophenylthio)- ß- phenyl- 1, N²- ethenoguanosine- 3', 5'- cyclic monophosphate ( 8-pCPT-PET-cGMP )
  • 8- (4- Chlorophenylthio)adenosine- 3', 5'- cyclic monophosphate ( 8-CPT-cAMP ), economy grade
  • 8- (4- Chlorophenylthio)adenosine- 3', 5'- cyclic monophosphate ( 8-CPT-cAMP ), fluorescence grade
  • 8- (4- Chlorophenylthio)guanosine- 3', 5'- cyclic monophosphate ( 8-pCPT-cGMP ), economy grade
  • 8- (4- Chlorophenylthio)guanosine- 3', 5'- cyclic monophosphate ( 8-pCPT-cGMP ), fluorescence grade
  • 7- Deazaguanosine- 3', 5'- cyclic monophosphate ( 7-CH-cGMP )
  • N2, 2'- O- Dibutyrylguanosine- 3', 5'- cyclic monophosphate ( DB-cGMP )
  • 8- (2- [ DY-547]- aminoethylthio)guanosine- 3', 5'- cyclic monophosphate ( 8-[DY-547]-AET-cGMP )
  • 8- (2- [ DY-647]- aminoethylthio)guanosine- 3', 5'- cyclic monophosphate ( 8-[DY-647]-AET-cGMP )
  • 8- (2- [ Fluoresceinyl]aminoethylthio)guanosine- 3', 5'- cyclic monophosphate ( 8-Fluo-cGMP )
  • Guanosine- 3', 5'- cyclic monophosphate ( cGMP )
  • Inosine- 3', 5'- cyclic monophosphate ( cIMP )
  • 8- (2- [7- Nitro- 4- benzofurazanyl]aminoethylthio)guanosine- 3', 5'- cyclic monophosphate ( 8-NBD-cGMP )
  • 8- Nitroguanosine- 3', 5'- cyclic monophosphate ( 8-NO2-cGMP )
  • 8- [ Pharos-450]- guanosine- 3', 5'- cyclic monophosphate ( 8-[φ-450]-cGMP )
  • 8- [ Pharos-575]- guanosine- 3', 5'- cyclic monophosphate ( 8-[φ-575]-cGMP )
  • β- Phenyl- 1, N2- ethenoguanosine- 3', 5'- cyclic monophosphate ( PET-cGMP )
     


  • 8- (2- Aminoethylthio)guanosine- 3', 5'- cyclic monophosphate ( 8-AET-cGMP )
       cyclic GMP functionalized for conjugation with markers and dyes or for immobilization.
       Dills et al., Biochemistry, 15, 3724 - 3730 (1976).
    A 029 5 uM/ ~2.1 mg, 5 x 5 uM CAS No.: [115974-70-4]

    N1- Aminoguanosine- 3', 5'- cyclic monophosphate ( 1-NH2-cGMP )
       Site-selective cyclic GMP analogue prefering site A of cGK, suitable for synergism studies.
       Corbin et al., J. Biol. Chem., 261, 1208 - 1214 (1986).
    A 041 5 uM/ ~1.9 mg, 5 x 5 uM CAS No.: [78033-42-8]

    N2- (6- Aminohexyl)guanosine- 3', 5'- cyclic monophosphate ( 2-AH-cGMP )
       Suitable as ligand in affinity chromatography of cGMP-binding proteins and for modification with fluorophores.
       Dills et al., Biochemistry 15, 3724 - 3730 (1976). Hebert et al., J. Biol. Chem., 273, 5557 - 5565 (1998).
    A 055 5 uM/ ~2.2 mg, 5 x 5 uM CAS No.: [205368-58-7]

    8- (2- Aminophenylthio)guanosine- 3', 5'- cyclic monophosphate ( 8-APT-cGMP )
       Isozyme-selective activator of cGMP-dependent protein kinase I a which prefers type I a over I ß by a factor of 200.
       Haynes, Br. J. Pharmacol., 130, 685 - 691 (2000); Cook & Haynes, Cell. Signal., 16, 253 - 261 (2004).
    A 032 5 uM/ ~2.4 mg, 5 x 5 uM CAS No.: [205368-58-7]

    2- Aminopurine riboside- 3', 5'- monophosphate ( 2-NH2-cPuMP )
       Fluorescent cyclic nucleotide, λexc 305 nm; λem 370 nm.
       Scheit, J. Carbohydr. Nucleosides, Nucleotides, 1, 385 - 399 (1974).
    A 027 5 uM/ ~1.8 mg, 5 x 5 uM CAS No.: [42467-66-3]

    β- (4- Azidophenyl)- 1, N2- etheno- 8- bromoguanosine- 3', 5'- cyclic monophosphate ( 4-N3-PET-8-Br-cGMP )
       Analogue for photoaffinity labelling of cGMP-responsive receptors, considered to be a isozyme-selective activator of cGMP-dependent
       protein kinase I α and β.
    A 102 1 uM/ ~0.6 mg, 5 x 1 uM CAS No.: [pending]

    8- (2- [ Biotinyl]aminoethylthio)guanosine- 3', 5'- cyclic monophosphate ( 8-[Biotin]-AET-cGMP )
       Biotin connected to the 8-position of cyclic GMP via a 15 atom spacer.
    B 025 1 uM/ ~0.8 mg, 5 x 1 uM CAS No.: [pending]

    N2- (6- [ Biotinyl]aminohexyl)guanosine- 3', 5'- cyclic monophosphate ( 2-[Biotin]-AH-cGMP )
       Biotin connected to the 2-position of cyclic GMP via a 19 atom spacer.
    B 032 1 uM/ ~0.8 mg, 5 x 1 uM CAS No.: [pending]

    8- Bromo- ß- phenyl- 1, N²- ethenoguanosine- 3', 5'-cyclic monophosphate ( 8-Br-PET-cGMP )
       Potent membrane-permeant activator of both isozymes I α and I ß of cGMP-dependent protein kinase while only a poor stimulator
       of type II.
       Sekhar et al., Mol. Pharmacol., 42, 103 - 108 (1992).
    P 003 10 uM/ ~5.5 mg, 5 x 10 uM CAS No.: [144510-04-3]

    8- Bromoguanosine- 3', 5'- cyclic monophosphate ( 8-Br-cGMP ), economy grade
       Activator of cGMP-dependent protein kinases I α, I ß & type II and cGMP-gated ion channels (cyclic GMP agonist).
       Rapoport et al., Proc. Natl. Acad. Sci. USA, 79, 6470 - 6474 (1982).
    B 004 E 50 mg/ ~111uM, 5 x 50 mg CAS No.: [51116-01-9]

    8- Bromoguanosine- 3', 5'- cyclic monophosphate ( 8-Br-cGMP ), fluorescence grade
       Activator of cGMP-dependent protein kinases I α, I ß & type II and cGMP-gated ion channels (cyclic GMP agonist).
       Rapoport et al., Proc. Natl. Acad. Sci. USA, 79, 6470 - 6474 (1982).
    B 004 50 uM/ ~22 mg, 5 x 50 uM CAS No.: [51116-01-9]

    8- (4- Chlorophenylthio)- ß- phenyl- 1, N²- ethenoguanosine- 3', 5'- cyclic monophosphate ( 8-pCPT-PET-cGMP)
       Highly membrane-permeant activator of cyclic GMP-dependent protein kinase, but most probably inhibitor of the retinal type cGMP-
       gated ion channel, thus suitable for distinction between kinase and ion channel mediated effects.
    C 045 5 uM/ ~3 mg, 5 x 5 uM CAS No.: [pending]

    8- (4- Chlorophenylthio)adenosine- 3', 5'- cyclic monophosphate ( 8-CPT-cAMP ), economy grade
       Lipophilic activator of both cAMP- and cGMP- dependent protein kinase and of Epac. Higher activation potential compared to cAMP;
       excellent cell membrane permeability, improved phosphodiesterase stability and high site selectivity preferring site B of cAK type II.
       Geiger et al.: Proc. Natl. Acad. Sci. USA, 89, 1031 - 1035 (1992).Murray et al.: Biochem. Pharmacol., 44, 2303 - 2306 (1992).
    C 010 E 50 mg/ ~102uM, 5 x 50 mg CAS No.: [93882-12-3]

    8- (4- Chlorophenylthio)adenosine- 3', 5'- cyclic monophosphate ( 8-CPT-cAMP ), fluorescence grade
       Lipophilic activator of both cAMP- and cGMP- dependent protein kinase and of Epac. Higher activation potential compared to cAMP;
       excellent cell membrane permeability, improved phosphodiesterase stability and high site selectivity preferring site B of cAK type II.
       Geiger et al.: Proc. Natl. Acad. Sci. USA, 89, 1031 - 1035 (1992).Murray et al.: Biochem. Pharmacol., 44, 2303 - 2306 (1992).
    C 010 100 uM/ ~49 mg, 5 x 100 uM CAS No.: [93882-12-3]

    8- (4- Chlorophenylthio)guanosine- 3', 5'- cyclic monophosphate ( 8-pCPT-cGMP ), economy grade
       Selective activator of both, cGMP-dependent protein kinase type I α and type II, as well as of cGMP-gated ion channels.
       Geiger et al., Proc. Natl. Acad. Sci. USA, 89, 1031 - 1035 (1992).
    C 009 E 10 mg/ ~19 uM, 5 x 10 mg CAS No.: [51239-26-0]

    8- (4- Chlorophenylthio)guanosine- 3', 5'- cyclic monophosphate ( 8-pCPT-cGMP ), fluorescence grade
       Selective activator of both, cGMP-dependent protein kinase type I α and type II, as well as of cGMP-gated ion channels.
       Geiger et al., Proc. Natl. Acad. Sci. USA, 89, 1031 - 1035 (1992).
    C 009 10 uM/ ~5 mg, 5 x 10 uM CAS No.: [51239-26-0]

    7- Deazaguanosine- 3', 5'- cyclic monophosphate ( 7-CH-cGMP )
       Cyclic GMP analogue lacking purine N-7 nitrogen for receptor mapping studies.
       Hebert et al., J. Biol. Chem., 273, 5557 - 5565 (1998); Quynh-Hoa et al., Angew. Chem., 94, 366 (1982).
    D 099 5 uM/ ~1.8 mg, 5 x 5 uM CAS No.: [81611-03-2]

    N2, 2'- O- Dibutyrylguanosine- 3', 5'- cyclic monophosphate ( DB-cGMP )
       Metabolically activatable PKG agonist.
       References
    D 010 50 uM/ ~25 mg, 5 x 50 uM CAS No.: [51116-00-8]

    8- (2- [ DY-547]- aminoethylthio)guanosine- 3', 5'- cyclic monophosphate ( 8-[DY-547]-AET-cGMP )
       Fluorescent cGMP analogue e.g. for research focussed on kinetic studies of CNG ion channels and other cGMP-reponsive binding
       proteins; λexc 557 nm, λem 574 nm.
       Biskup et al., Nature, 446, 440 - 443 (2007).
    D 087 0.1 uM/ ~0.1 mg, 5 x 0.1 uM CAS No.: [pending]

    8- (2- [ Fluoresceinyl]aminoethylthio)guanosine- 3', 5'- cyclic monophosphate ( 8-Fluo-cGMP )
       Fluorescent cGMP analogue λexc 494 nm, λem 517 nm.
       Tanaka et al, Biochemistry 28, 2776 - 2784 (1989); Koutalos et al., Biophys. J., 69, 2163 - 2167 (1995).
    F 001 1 uM/ ~0.8 mg, 5 x 1 uM CAS No.: [pending]

    Guanosine- 3', 5'- cyclic monophosphate ( cGMP )
       Target receptors for the second messenger cyclic GMP include protein kinase G isozymes, cGMP-gated ion channels as well as
       cGMP-responsive phosphodiesterases.
       Poppe, H.; Nature Methods, 5, 277 - 278 (2008), Schweinsberg, S., Proteomics, 8, 1212 - 1220 (2008)
    G 001 100 uM/ ~37 mg, 5 x 100 uM CAS No.: [40732-48-7]

    Inosine- 3', 5'- cyclic monophosphate ( cIMP )Guanosine- 3', 5'- cyclic monophosphate ( cGMP )
       Poteet-Smith et al., J. Biol. Chem., 272, 379 - 388 (1997).
    I 001 50 uM/ ~18 mg, 5 x 50 uM CAS No.: [41092-64-2]

    8- (2- [7- Nitro- 4- benzofurazanyl]aminoethylthio)guanosine- 3', 5'- cyclic monophosphate ( 8-NBD-cGMP )
       Potent membrane-permeant fluorescent activator of both isozymes I a and I ß of cGMP-dependent protein kinase.
       Ruf et al. in Heilmeyer (ed.), Signal Transduction and Protein Phosphorylation, Ser. A, Life Sci., 135, 99 - 104 ( 1987), Plenum Press, NATO ASI.
    N 001 1 uM/ ~0.7 mg, 5 x 1 uM CAS No.: [115993-88-9]

    8- Nitroguanosine- 3', 5'- cyclic monophosphate ( 8-NO2-cGMP )
       The nitrated derivative of cGMP, 8-NO2-cGMP, is considered to play an important role in NO-mediated signal transduction.
       Sawa et al., Nat. Chem. Biol., 3, 727 - 735 (2007).
    N 011   CAS No.: [pending]

    8- [ Pharos-450]- guanosine- 3', 5'- cyclic monophosphate ( 8-[φ-450]-cGMP )
       cyclic GMP connected to the relatively small Pharos 450 fluorophore (λexc 450 nm, λem 534 nm). The fluorophore can be excited e.g.
       by a He/Cd laser. especially suitable for studies with intact cells.
    P 025 0.1 uM/ ~74 ug, 5 x 0.1 uM CAS No.: [pending]

    8- [ Pharos-575]- guanosine- 3', 5'- cyclic monophosphate ( 8-[φ-575]-cGMP )
       cyclic GMP connected to the relatively small Pharos 575 fluorophore (λexc 577 nm, λem 605 nm). The fluorophore can be excited e.g.
       by a Kr/Ar laserby . especially suitable for studies with intact cells.
    P 020 0.1 uM/ ~74 ug, 5 x 0.1 uM CAS No.: [pending]

    β- Phenyl- 1, N²- ethenoguanosine- 3', 5'- cyclic monophosphate ( PET-cGMP )
       Potent membrane-permeant activator of both isozymes I α and I ß of cGMP-dependent protein kinase while only a poor stimulator of
       type II. Common agonists such as 8-Br-cGMP or 8-pCPT-cGMP mainly activate kinase subtypes I α and II.
    P 001 10 uM/ ~4.7 mg, 5 x 10 uM CAS No.: [78080-27-0]