Biological Activity
Selective inhibitor of protein kinase G (Ki values are 0.23, 4 and > 10 μM for inhibition of PKG, PKC and PKA respectively). Inhibits SNP-stimulated PKG activity with an IC50 of 60 nM in dispersed smooth muscle cells and has little effect on PKA activity at concentrations of up to 10 μM.
Technical Data
| M. Wt | 495.53 |
| Formula | C29H25N3O5 |
| Storage | Desiccate at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 126643-37-6 |
| PubChem ID | 108152 |
| InChI Key | QTYMDECKVKSGSM-YMUMJAELSA-N |
| Smiles | [H][C@]18O[C@](N6C4=C3N1C2=CC=CC=C2C3=C7C(CN(C7=O)C)=C4C5=CC=CC=C56)([C@]([C@@](OC)=O)(OC)C8)C |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 24.78 | 50 |
Preparing Stock Solutions
The following data is based on the product molecular weight 495.53. Batch specific molecular weights may vary from batch to batch due to solvent 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 | 2.02 mL | 10.09 mL | 20.18 mL |
| 5 mM | 0.4 mL | 2.02 mL | 4.04 mL |
| 10 mM | 0.2 mL | 1.01 mL | 2.02 mL |
| 50 mM | 0.04 mL | 0.2 mL | 0.4 mL |
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References
References are publications that support the products' biological activity.
Gadbois et al (1992) Multiple kinase arrest points in the G1 phase of nontransformed mammalian cells are absent in transformed cells. Proc.Natl.Acad.Sci.U.S.A. 89 8626 PMID: 1528872
Murthy and Makhlouf (1995) Interaction of cA-kinase and cG-kinase in mediating relaxation of dispersed smooth muscle cells. Am.J.Physiol. 268 C171 PMID: 7840145
Smolenski et al (1998) Functional analysis of cGMP-dependent protein kinases I and II as mediators of NO/cGMP effects. Naunyn Schmiedebergs Arch.Pharmacol. 358 134 PMID: 9721015
Keywords: KT 5823, supplier, Selective, protein, kinases, G, inhibitors, inhibits, PKG, cGMP, KT5823, Protein, Kinase, G, Protein, Kinase, G, Tocris Bioscience
