PKI 14-22 amide, myristoylated

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Cat.No. 2546 - PKI 14-22 amide, myristoylated | Myr-Gly-Arg-Thr-Gly-Arg-Arg-Asn-Ala-Ile-NH2 | CAS No. 201422-03-9
Description: Cell-permeable protein kinase A inhibitor
Alternative Names: Protein kinase inhibitor-(14-22)-amide, myristoylated
Datasheet
Citations (9)
Literature

Biological Activity

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

M. Wt 1209.5
Formula C53H100N20O12
Sequence GRTGRRNAI

(Modifications: Gly-1 = Myr-Gly, Ile-9 = C-terminal amide)

Storage Desiccate at -20°C
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.

All Tocris products are intended for laboratory research use only.

Solubility Data

SolubilitySoluble to 1 mg/ml in 30% acetonitrile / water

Preparing Stock Solutions

The following data is based on the product molecular weight 1209.5. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 0.83 mL 4.13 mL 8.27 mL
5 mM 0.17 mL 0.83 mL 1.65 mL
10 mM 0.08 mL 0.41 mL 0.83 mL
50 mM 0.02 mL 0.08 mL 0.17 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the products' biological activity.

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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Keywords: Cell-permeable protein kinases A inhibitors inhibits Cell permeable PKA PKI14-22 amide myristoylated Protein kinase inhibitor-(14-22)-amide, myristoylated Protein Kinase A

9 Citations for PKI 14-22 amide, myristoylated

Citations are publications that use Tocris products. Selected citations for PKI 14-22 amide, myristoylated include:

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

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

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

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

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


Do you know of a great paper that uses PKI 14-22 amide, myristoylated from Tocris? If so please let us know.

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