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Submit ReviewPKA inhibitor fragment (6-22) amide is a potent inhibitor of cAMP-dependent protein kinase (PKA) (Ki = 2.5 nM); derived from the active portion of the heat-stable PKA inhibitor protein PKI.
分子量 | 1868.08 |
公式 | C80H130N28O24 |
序列 |
TYADFIASGRTGRRNAI (Modifications: Ile-17 = C-terminal amide) |
储存 | Store at -20°C |
纯度 | ≥95% (HPLC) |
CAS Number | 121932-06-7 |
PubChem ID | 16155227 |
InChI Key | VAKHFAFLRUNHLQ-PEBJKXEYSA-N |
Smiles | [H]N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CC1=CC=C(O)C=C1)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](CC1=CC=CC=C1)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)NCC(=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 |
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。
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溶解性 | Soluble to 1 mg/ml in water |
参考文献是支持产品生物活性的出版物。
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 inhibitor protein. J.Biol.Chem. 264 8802 PMID: 2722799
Glass et al (1989) Protein kinase inhibitor-(6-22)-amide peptide analogs with standard and nonstandard amino acid substitutions for phenylalanine 10. J.Biol.Chem. 264 14579 PMID: 2760075
Otmakhova et al (2000) Inhibition of the cAMP pathway decreases early long-term potentiation at CA1 hippocampal synapses. J.Neurosci. 20 4446 PMID: 10844013
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关键词: PKA Inhibitor Fragment (6-22) amide, PKA Inhibitor Fragment (6-22) amide supplier, Potent, protein, kinases, A, inhibitors, inhibits, PKA, Protein, kinase, inhibitor-(6-22)-amide, PKI-(6-22)-amide, Kinase, 1904, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 PKA inhibitor fragment (6-22) amide 的部分引用包括:
Costa et al (2018) Activation of Serotonin 5-HT7 Receptors Modulates Hippocampal Synaptic Plasticity by Stimulation of Adenylate Cyclases and Rescues Learning and Behavior in a Mouse Model of Fragile X Syndrome. Front Mol Neurosci 11 353 PMID: 30333723
Pleil et al (2015) NPY signaling inhibits extended amygdala CRF neurons to suppress binge alcohol drinking. Nat Neurosci 18 545 PMID: 25751534
Tumati et al (2009) Sustained mor. treatment augments capsaicin-evoked calcitonin gene-related peptide release from primary sensory neurons in a protein kinase A- and Raf-1-dependent manner. J Neurosci 330 810 PMID: 19491327
Cui et al (2016) Endocannabinoid dynamics gate spike-timing dependent depression and potentiation. Elife 5 e13185 PMID: 26920222
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
O'Neill & Sylantyev (2018) Selective modulation of tonically active GABAA receptor functional subgroups by G-proteins and protein kinase C. Exp Biol Med (Maywood) 243 1046 PMID: 30205722
Hopf et al (2005) Atypical protein kinase C is a novel mediator of DA-enhanced firing in nucleus accumbens neurons. FASEB J 25 985 PMID: 15673680
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PKA inhibitor fragment (PKI) was used to compare effects of PKA and G-protein signalling on root mean square noise (RMS) produced by GABA-A receptors in electrophysiological recording. We found that after block of PKA with PKI GABA-A receptor antagonists SR 95531 and Picrotoxin generate stronger impact on RMS noise than after block of G-protein signalling with pertussis toxin.