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Description: Selective protein kinase G inhibitor
Chemical Name: (9S,10R,12R)-2,3,9,10,11,12-Hexahydro-10-methoxy-2,9-dimethyl-1-oxo-9,12-epoxy-1H-diindolo[1,2,3-fg:3',2',1'-kl]pyrrolo[3,4-i][1,6]benzodiazocine-10-carboxylic acid, methyl ester
Purity: ≥95% (HPLC)
Biological Activity for KT 5823
KT 5823 is a 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 for KT 5823
| M. Wt | 495.53 |
| Formula | C29H25N3O5 |
| Storage | Desiccate at -20°C |
| Purity | ≥95% (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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for KT 5823
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 24.78 | 50 |
Preparing Stock Solutions for KT 5823
The following data is based on the product molecular weight 495.53. 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 |
|---|---|---|---|
| 0.5 mM | 4.04 mL | 20.18 mL | 40.36 mL |
| 2.5 mM | 0.81 mL | 4.04 mL | 8.07 mL |
| 5 mM | 0.4 mL | 2.02 mL | 4.04 mL |
| 25 mM | 0.08 mL | 0.4 mL | 0.81 mL |
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Product Datasheets for KT 5823
References for KT 5823
References are publications that support the biological activity of the product.
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
If you know of a relevant reference for KT 5823, please let us know.
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Keywords: KT 5823, KT 5823 supplier, Selective, protein, kinases, G, inhibitors, inhibits, PKG, cGMP, KT5823, Protein, Kinase, 1289, Tocris Bioscience
6 Citations for KT 5823
Citations are publications that use Tocris products. Selected citations for KT 5823 include:
Livingstone et al (2019) Secreted Amyloid Precursor Protein-Alpha Promotes Arc Protein Synthesis in Hippocampal Neurons. Front Mol Neurosci 12 198 PMID: 31474829
Kuo et al (2014) A xanthine-derivative K(+)-channel opener protects against serotonin-induced cardiomyocyte hypertrophy via the modulation of protein kinases. Int J Biol Sci 10 64 PMID: 24391452
Becker et al (2014) Differential activation of natriuretic peptide receptors modulates cardiomyocyte proliferation during development. Development 141 335 PMID: 24353062
Jayabal et al (2023) Nitric oxide suppression by secreted frizzled-related protein 2 drives retinoblastoma Cell Rep 42 112103 PMID: 36773293
Giricz et al (2009) Hyperlipidaemia induced by a high-cholesterol diet leads to the deterioration of guanosine-3',5'-cyclic monophosphate/protein kinase G-dependent cardioprotection in rats. J Neurosci 158 1495 PMID: 19845676
Pulkkinen et al (2012) The bitter taste receptor (TAS2R) agonists denatonium and chloroquine display distinct patterns of relaxation of the guinea pig trachea. Am J Physiol Lung Cell Mol Physiol 303 L956 PMID: 22962016
Do you know of a great paper that uses KT 5823 from Tocris? Please let us know.
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