KT 5720

Pricing Availability   Qty
Cat.No. 1288 - KT 5720 | C32H31N3O5 | CAS No. 108068-98-0
Description: Selective protein kinase A inhibitor
Chemical Name: (9R,10S,12S)-2,3,9,10,11,12-Hexahydro-10-hydroxy-9-methyl-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, hexyl ester
Purity: ≥98% (HPLC)
Datasheet
Citations (24)
Reviews
Literature

Biological Activity

Potent, selective inhibitor of protein kinase A (Ki = 60 nM). Has no effect on PKG or PKC (Ki > 2 μM). Reversibly arrests human skin fibroblasts in the G1 phase.

Technical Data

M. Wt 537.61
Formula C32H31N3O5
Storage Desiccate at -20°C
Purity ≥98% (HPLC)
CAS Number 108068-98-0
PubChem ID 9850141
InChI Key ZHEHVZXPFVXKEY-MWOZDUBJSA-N
Smiles O[C@@]1(C(OCCCCCC)=O)C[C@@H]2O[C@]1(N3C4=CC=CC=C4C5=C3C6=C(C7=C5CNC7=O)C8=CC=CC=C8N26)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

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 26.88 50

Preparing Stock Solutions

The following data is based on the product molecular weight 537.61. 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 3.72 mL 18.6 mL 37.2 mL
2.5 mM 0.74 mL 3.72 mL 7.44 mL
5 mM 0.37 mL 1.86 mL 3.72 mL
25 mM 0.07 mL 0.37 mL 0.74 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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References

References are publications that support the biological activity of the product.

Cabell et al (1993) Effects of selective inhibition of protein kinase C, cyclic AMP-dependent protein kinase, and Ca(2+)-calmodulin-dependent protein kinase on neurite development in cultured rat hippocampal neurons. Int.J.Dev. Neurosci. 11 357 PMID: 7689287

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

Kase et al (1987) K-252 compounds, novel and potent inhibitors of protein kinase C and cyclic nucleotide-dependent protein kinases. Biochem.Biophys.Res.Commun. 142 436 PMID: 3028414


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Keywords: KT 5720, KT 5720 supplier, Selective, protein, kinases, A, inhibitors, inhibits, PKA, cAMP, KT5720, Protein, Kinase, 1288, Tocris Bioscience

24 Citations for KT 5720

Citations are publications that use Tocris products. Selected citations for KT 5720 include:

Dai et al (2008) A crucial role for cAMP and protein kinase A in D1 DA receptor regulated intracellular calcium transients. Neurosignals 16 112 PMID: 18253052

Hook et al (2012) DArgic modulation of ganglion-cell photoreceptors in rat. Biochim Biophys Acta 35 507 PMID: 22304466

Kravtsov et al (2007) Altered Ca(2+) handling by ryanodine receptor and Na(+)-Ca(2+) exchange in the heart from ovariectomized rats: role of protein kinase A. Am J Physiol Cell Physiol 292 C1625 PMID: 17166940

Weng et al (2016) Potentiation of Schaffer-Collateral CA1 Synaptic Transmission by eEF2K and p38 MAPK Mediated Mechanisms. Front Cell Neurosci 10 247 PMID: 27826228

O'Riordan et al (2006) Regulation of nuclear factor κB in the hippocampus by group I metabotropic glutamate receptors. PLoS One 26 4870 PMID: 16672661

Cornelison et al (2016) Elevated levels of calcitonin gene-related peptide in upper spinal cord promotes sensitization of primary trigeminal nociceptive neurons Neuroscience 339 491 PMID: 27746346

Merino et al (2015) Glucagon Increases Beating Rate but Not Contractility in Rat Right Atrium. Comparison with isoprote. Br J Pharmacol 10 e0132884 PMID: 26222156

Parnell et al (2015) Phosphorylation of ezrin on Thr567 is required for the synergistic activation of cell spreading by EPAC1 and protein kinase A in HEK293T cells. Invest Ophthalmol Vis Sci 1853 1749 PMID: 25913012

Thakran et al (2015) Pioglitazone restores IGFBP-3 levels through DNA PK in retinal endothelial cells cultured in hyperglycemic conditions. PLoS One 56 177 PMID: 25525174

Smith et al (2015) The Effects of the Endocannabinoids Anandamide and 2-Arachidonoylglycerol on Human Osteoblast Proliferation and Differentiation. PLoS One 10 e0136546 PMID: 26414859

Brignell et al (2015) Steady-state modulation of voltage-gated K+ channels in rat arterial smooth muscle by cyclic AMP-dependent protein kinase and protein phosphatase 2B. J Neurosci 10 e0121285 PMID: 25793374

Campos et al (2014) Central vagal afferent endings mediate reduction of food intake by melanocortin-3/4 receptor agonist. J Neurosci 34 12636 PMID: 25232103

Liu and Zhuo (2014) Loss of long-term depression in the insular cortex after tail amputation in adult mice. Mol Pain 10 1 PMID: 24398034

Lee et al (2012) The calcium-sensing receptor regulates the NLRP3 inflammasome through Ca2+ and cAMP. Nature 492 123 PMID: 23143333

Guo and Feng (2012) OX2R activation induces PKC-mediated ERK and CREB phosphorylation. Exp Cell Res 318 2004 PMID: 22652455

Nakao et al (2012) The role of mislocalized phototransduction in photoreceptor cell death of retinitis pigmentosa. PLoS One 7 e32472 PMID: 22485131

Sowa et al (2010) Prostatic acid phosphatase reduces thermal sensitivity and chronic pain sensitization by depleting phosphatidylinositol 4,5-bisphosphate. J Neurosci 30 10282 PMID: 20685973

Xu et al (2018) Enriched environment enhances β-adrenergic signaling to prevent microglia inflammation by amyloid-β. EMBO Mol Med 10 PMID: 30093491

Patra et al (2018) Mutant GNAS drives pancreatic tumourigenesis by inducing PKA-mediated SIK suppression and reprogramming lipid metabolism. Nat Cell Biol 20 811 PMID: 29941929

Cui et al (2016) Endocannabinoid dynamics gate spike-timing dependent depression and potentiation. Elife 5 e13185 PMID: 26920222

Li et al (2016) Progesterone receptor membrane component-1 regulates hepcidin biosynthesis. J Clin Invest 126 389 PMID: 26657863

Chang et al (2015) Protection against β-amyloid-induced synaptic and memory impairments via altering β-amyloid assembly by bis(heptyl)-cognitin. Sci Rep 5 10256 PMID: 26194093

Agopyan et al (2004) TRPV1 receptors mediate particulate matter-induced apoptosis. Am J Physiol Lung Cell Mol Physiol 286 L563 PMID: 14633515

Meitzen et al (2011) β1-Adrenergic receptors activate two distinct signaling pathways in striatal neurons. J Neurochem 116 984 PMID: 21143600


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