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Submit ReviewKT 5720
说明： Selective protein kinase A inhibitor
化学名： (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
纯度： ≥97% (HPLC)
生物活性 for KT 5720
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.
技术数据 for KT 5720
| 分子量 | 537.61 |
| 公式 | C32H31N3O5 |
| 储存 | Store at -20°C |
| 纯度 | ≥97% (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 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for KT 5720
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 26.88 | 50 |
制备储备液 for KT 5720
以下数据基于产品分子量 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.
| 浓度/溶剂体积/质量 | 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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产品说明书 for KT 5720
参考文献 for KT 5720
参考文献是支持产品生物活性的出版物。
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
If you know of a relevant reference for KT 5720, please let us know.
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关键词: KT 5720, KT 5720 supplier, Selective, protein, kinases, A, inhibitors, inhibits, PKA, cAMP, KT5720, Protein, Kinase, 1288, Tocris Bioscience
28 篇 KT 5720 的引用文献
引用文献是使用了 Tocris 产品的出版物。 KT 5720 的部分引用包括：
Cruz et al (2018) Protein kinase A activation inhibits DUX4 gene expression in myotubes from patients with facioscapulohumeral muscular dystrophy. J Biol Chem 293 11837 PMID: 29899111
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
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
Hook et al (2012) DArgic modulation of ganglion-cell photoreceptors in rat. Biochim Biophys Acta 35 507 PMID: 22304466
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
Meitzen et al (2011) β1-Adrenergic receptors activate two distinct signaling pathways in striatal neurons. J Neurochem 116 984 PMID: 21143600
Salinar et al (2020) Imiquimod suppresses respiratory syncytial virus (RSV) replication via PKA pathway and reduces RSV induced-inflammation and viral load in mice lungs Antiviral Res 179 PMID: 32387475
Yuede et al (2021) Pimavanserin, a 5HT 2A receptor inverse agonist, rapidly suppresses Aβ production and related pathology in a mouse model of Alzheimer's disease. J.Neurochem. 156 658 PMID: 33278025
Vaden et al (2019) The readily-releasable pool dynamically regulates multivesicular release. Elife 8 PMID: 31364987
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
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
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
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
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
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
Agopyan et al (2004) TRPV1 receptors mediate particulate matter-induced apoptosis. Am J Physiol Lung Cell Mol Physiol 286 L563 PMID: 14633515
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KT 5720 的评论
平均评分: 5 (基于 2 条评论。)
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Pancreatic cancer signaling testing.
By
MARINA KOUTSIOUMPA on 12/26/2023
分析类型： In Vitro
种属： Human
Pancreatic cancer cells were pretreated for 2 hours with KT 5720, triethylammonium salt followed by conventional chemotherapeutics. Selective Inhibition of Protein Kinase A mediated the signal transduction pathways triggered by the chemotherapeutics.
Excellent PKA inhibitor.
By
Gaurang Trivedi on 09/28/2019
分析类型： In Vitro
种属： Mouse
细胞系/组织： Stem Cells
It is an excellent inhibitor for PKA.