KT 5720
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: ≥97%
Biological Activity
KT 5720 is a 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
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.
Background References
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Protein kinase A activation inhibits DUX4 gene expression in myotubes from patients with facioscapulohumeral muscular dystrophy
JM Cruz, N Hupper, LS Wilson, JB Concannon, Y Wang, B Oberhauser, K Patora-Kom, Y Zhang, DJ Glass, AU Trendelenb, BA Clarke
J. Biol. Chem., 2018;0(0):. -
The calcium-sensing receptor regulates the NLRP3 inflammasome through Ca2+ and cAMP.
Lee G, Subramanian N, Kim A, Aksentijevich I, Goldbach-Mansky R, Sacks D, Germain R, Kastner D, Chae J
Nature, 2012;492(7427):123-7. -
The role of mislocalized phototransduction in photoreceptor cell death of retinitis pigmentosa.
Nakao T, Tsujikawa M, Notomi S
PLoS ONE, 2012;7(4):e32472. -
Inversion of Sonic hedgehog action on its canonical pathway by electrical activity.
Belgacem Y, Borodinsky L
Proc Natl Acad Sci U S A, 2015;112(13):4140-5. -
Apelin inhibits adipogenesis and lipolysis through distinct molecular pathways.
Than A, Cheng Y, Foh L, Leow M, Lim S, Chuah Y, Kang Y, Chen P
Mol Cell Endocrinol, 2012;362(1):227-41. -
CR1-mediated ATP release by human red blood cells promotes CR1 clustering and modulates the immune transfer process.
Melhorn M, Brodsky A, Estanislau J, Khoory J, Illigens B, Hamachi I, Kurishita Y, Fraser A, Nicholson-Weller A, Dolmatova E, Duffy H, Ghiran I
J Biol Chem, 2013;288(43):31139-53. -
Phosphorylation of mouse melanopsin by protein kinase a.
Blasic, Joseph R, Brown, R Lane, Robinson, Phyllis
PLoS ONE, 2012;7(9):e45387. -
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.
Cabell et al.
Int.J.Dev. Neurosci., 1993;11:357 -
Multiple kinase arrest points in the G1 phase of nontransformed mammalian cells are absent in transformed cells.
Gadbois et al.
Proc.Natl.Acad.Sci.U.S.A., 1992;89:8626 -
K-252 compounds, novel and potent inhibitors of protein kinase C and cyclic nucleotide-dependent protein kinases.
Kase et al.
Biochem.Biophys.Res.Commun., 1987;142:436
Product Datasheets
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Citations for KT 5720
The citations listed below are publications that use Tocris products. Selected citations for KT 5720 include:
28 Citations: Showing 1 - 10
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Pimavanserin, a 5HT 2A receptor inverse agonist, rapidly suppresses Aβ production and related pathology in a mouse model of Alzheimer's disease.
Authors: Yuede Et al.
J.Neurochem. 2021;156:658
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Imiquimod suppresses respiratory syncytial virus (RSV) replication via PKA pathway and reduces RSV induced-inflammation and viral load in mice lungs
Authors: Salinar Et al.
Antiviral Res 2020;179
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The readily-releasable pool dynamically regulates multivesicular release.
Authors: Vaden Et al.
Elife 2019;8
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Protein kinase A activation inhibits DUX4 gene expression in myotubes from patients with facioscapulohumeral muscular dystrophy.
Authors: Cruz Et al.
J Biol Chem 2018;293:11837
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Mutant GNAS drives pancreatic tumourigenesis by inducing PKA-mediated SIK suppression and reprogramming lipid metabolism.
Authors: Patra Et al.
Nat Cell Biol 2018;20:811
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Enriched environment enhances β-adrenergic signaling to prevent microglia inflammation by amyloid-β.
Authors: Xu Et al.
EMBO Mol Med 2018;10
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Endocannabinoid dynamics gate spike-timing dependent depression and potentiation.
Authors: Cui Et al.
Elife 2016;5:e13185
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Elevated levels of calcitonin gene-related peptide in upper spinal cord promotes sensitization of primary trigeminal nociceptive neurons
Authors: Cornelison Et al.
Neuroscience 2016;339:491
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Progesterone receptor membrane component-1 regulates hepcidin biosynthesis.
Authors: Li Et al.
J Clin Invest 2016;126:389
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Potentiation of Schaffer-Collateral CA1 Synaptic Transmission by eEF2K and p38 MAPK Mediated Mechanisms.
Authors: Weng Et al.
Front Cell Neurosci 2016;10:247
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Protection against β-amyloid-induced synaptic and memory impairments via altering β-amyloid assembly by bis(heptyl)-cognitin.
Authors: Chang Et al.
Sci Rep 2015;5:10256
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Pioglitazone restores IGFBP-3 levels through DNA PK in retinal endothelial cells cultured in hyperglycemic conditions.
Authors: Thakran Et al.
PLoS One 2015;56:177
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Phosphorylation of ezrin on Thr567 is required for the synergistic activation of cell spreading by EPAC1 and protein kinase A in HEK293T cells.
Authors: Parnell Et al.
Invest Ophthalmol Vis Sci 2015;1853:1749
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The Effects of the Endocannabinoids Anandamide and 2-Arachidonoylglycerol on Human Osteoblast Proliferation and Differentiation.
Authors: Smith Et al.
PLoS One 2015;10:e0136546
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Glucagon Increases Beating Rate but Not Contractility in Rat Right Atrium. Comparison with isoprote.
Authors: Merino Et al.
Br J Pharmacol 2015;10:e0132884
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Steady-state modulation of voltage-gated K+ channels in rat arterial smooth muscle by cyclic AMP-dependent protein kinase and protein phosphatase 2B.
Authors: Brignell Et al.
J Neurosci 2015;10:e0121285
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Central vagal afferent endings mediate reduction of food intake by melanocortin-3/4 receptor agonist.
Authors: Campos Et al.
J Neurosci 2014;34:12636
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Loss of long-term depression in the insular cortex after tail amputation in adult mice.
Authors: Liu and Zhuo
Mol Pain 2014;10:1
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The role of mislocalized phototransduction in photoreceptor cell death of retinitis pigmentosa.
Authors: Nakao Et al.
PLoS One 2012;7:e32472
-
The calcium-sensing receptor regulates the NLRP3 inflammasome through Ca2+ and cAMP.
Authors: Lee Et al.
Nature 2012;492:123
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DArgic modulation of ganglion-cell photoreceptors in rat.
Authors: Hook Et al.
Biochim Biophys Acta 2012;35:507
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OX2R activation induces PKC-mediated ERK and CREB phosphorylation.
Authors: Guo and Feng
Exp Cell Res 2012;318:2004
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β1-Adrenergic receptors activate two distinct signaling pathways in striatal neurons.
Authors: Meitzen Et al.
J Neurochem 2011;116:984
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Prostatic acid phosphatase reduces thermal sensitivity and chronic pain sensitization by depleting phosphatidylinositol 4,5-bisphosphate.
Authors: Sowa Et al.
J Neurosci 2010;30:10282
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A crucial role for cAMP and protein kinase A in D1 DA receptor regulated intracellular calcium transients.
Authors: Dai Et al.
Neurosignals 2008;16:112
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Altered Ca(2+) handling by ryanodine receptor and Na(+)-Ca(2+) exchange in the heart from ovariectomized rats: role of protein kinase A.
Authors: Kravtsov Et al.
Am J Physiol Cell Physiol 2007;292:C1625
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Regulation of nuclear factor κB in the hippocampus by group I metabotropic glutamate receptors.
Authors: O'Riordan Et al.
PLoS One 2006;26:4870
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TRPV1 receptors mediate particulate matter-induced apoptosis.
Authors: Agopyan Et al.
Am J Physiol Lung Cell Mol Physiol 2004;286:L563
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