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Submit ReviewPKI 14-22 amide, myristoylated
Description: Cell-permeable protein kinase A inhibitor
Alternative Names: Protein kinase inhibitor-(14-22)-amide,myristoylated
Purity: ≥95% (HPLC)
Biological Activity for PKI 14-22 amide, myristoylated
PKI 14-22 amide, myristoylated is a cell-permeable version of protein kinase inhibitor PKI (14-22) amide. The non-myristoylated version inhibits protein kinase A (Ki = 36 nM), inhibits cell growth and induces apoptosis in human pancreatic cancer cells (PANC-1).
Technical Data for PKI 14-22 amide, myristoylated
| M. Wt | 1209.5 |
| Formula | C53H100N20O12 |
| Sequence |
GRTGRRNAI (Modifications: Gly-1 = Myr-Gly, Ile-9 = C-terminal amide) |
| Storage | Store at -20°C |
| Purity | ≥95% (HPLC) |
| CAS Number | 201422-03-9 |
| PubChem ID | 71312213 |
| InChI Key | GQPQKQWUUHDDIS-JDLJUXOTSA-N |
| Smiles | [H]N(CC(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H]([C@@H](C)O)C(=O)NCC(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H]([C@@H](C)CC)C(N)=O)C(=O)CCCCCCCCCCCCC |
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 PKI 14-22 amide, myristoylated
| Solubility | Soluble to 1 mg/ml in DMSO |
Product Datasheets for PKI 14-22 amide, myristoylated
References for PKI 14-22 amide, myristoylated
References are publications that support the biological activity of the product.
Glass et al (1989) Primary structural determinants essential for potent inhibition of cAMP-dependent protein kinase by inhibitory peptides corresponding to the active portion of the heat-stable inhibitory protein. J.Biol.Chem. 264 8802 PMID: 2722799
Zheng et al (2000) Activation of apolipoprotein AI gene expression by protein kinase A and kinase C through transcription factor, Sp1. J.Biol.Chem. 275 31747 PMID: 10829013
Farrow et al (2003) Inhibition of pancreatic cancer cell growth and induction of apoptosis with novel therapies directed against protein kinase A. Surgery 134 197 PMID: 12947318
If you know of a relevant reference for PKI 14-22 amide, myristoylated, please let us know.
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16 Citations for PKI 14-22 amide, myristoylated
Citations are publications that use Tocris products. Selected citations for PKI 14-22 amide, myristoylated include:
Hamnett et al (2019) Vasoactive intestinal peptide controls the suprachiasmatic circadian clock network via ERK1/2 and DUSP4 signalling. Nat Commun 10 542 PMID: 30710088
Hashimotodani et al (2017) LTP at Hilar Mossy Cell-Dentate Granule Cell Synapses Modulates Dentate Gyrus Output by Increasing Excitation/Inhibition Balance. Neuron 95 928 PMID: 28817805
Maddugoda et al (2011) cAMP signaling by anthrax edema toxin induces transendothelial cell tunnels, which are resealed by MIM via Arp2/3-driven actin polymerization. Cell Host Microbe 10 464 PMID: 22100162
Meitzen et al (2011) β1-Adrenergic receptors activate two distinct signaling pathways in striatal neurons. J Neurochem 116 984 PMID: 21143600
Jantarajit et al (2017) CFTR-mediated anion secretion across intestinal epithelium-like Caco-2 monolayer under PTH stimulation is dependent on intermediate conductance K+ channels. Am J Physiol Cell Physiol 313 C118 PMID: 28490422
Jakobsen et al (2019) Soluble adenylyl cyclase-mediated cAMP signaling and the putative role of PKA and EPAC in cerebral mitochondrial function. J Neurosci Res 97 1018 PMID: 31172581
Liu et al (2008) Restoration of lysosomal pH in RPE cells from cultured human and ABCA4(-/-) mice: pharmacologic approaches and functional recovery. Invest Ophthalmol Vis Sci 49 772 PMID: 18235027
Al-Amily et al (2019) The functional impact of G protein-coupled receptor 142 (Gpr142) on pancreatic β-cell in rodent. Pflugers Arch 471 633 PMID: 30767071
Caiati et al (2013) PrPC controls via protein kinase A the direction of synaptic plasticity in the immature hippocampus. J Neurosci 33 2973 PMID: 23407955
Stival et al (2018) Disruption of protein kinase A localization induces acrosomal exocytosis in capacitated mouse sperm. J Biol Chem 293 9435 PMID: 29700114
Muñoz-Llancao et al (2015) Exchange Protein Directly Activated by cAMP (EPAC) Regulates Neuronal Polarization through Rap1B. J Exp Med 35 11315 PMID: 26269639
Watson et al (2015) Endothelial CD99 signals through soluble adenylyl cyclase and PKA to regulate leukocyte transendothelial migration. J Biol Chem 212 1021 PMID: 26101266
Singh et al (2015) The Orphan G Protein-Coupled Receptor Gpr175 (TPRA40) Enhances Hedgehog Signaling by Modulating cAMP Levels. J Biol Chem NULL PMID: 26451044
Tseng et al (2010) PKA-induced receptor activator of NF-κB ligand (RANKL) expression in vascular cells mediates osteoclastogenesis but not matrix calcification. Autophagy 285 29925 PMID: 20663885
Okumura et al (2014) Phospholipase C-Related Catalytically Inactive Protein (PRIP) Regulates Lipolysis in Adipose Tissue by Modulating the Phosphorylation of Hormone-Sensitive Lipase. PLoS One 9 e100559 PMID: 24945349
Adelfinger et al (2014) GABAB receptor phosphorylation regulates KCTD12-induced K+ current desensitization. Biochem Pharmacol 91 369 PMID: 25065880
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Cyclic AMP Pathway-related studies.
By
MARINA KOUTSIOUMPA on 10/13/2022
Assay Type: In Vitro
Species: Human
PKI 14-22 amide, myristoylated was used in studies exploring the role of PKA in mediating drug-induced activation of the cyclic AMP pathway.