PKA inhibitor fragment (6-22) amide (Synonyms: PKI (6-22) amide) |
| Catalog No.GP10075 |
A synthetic peptide inhibitor of PKA
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 121932-06-7
Sample solution is provided at 25 µL, 10mM.
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Ki: 1.6 nM
PKA inhibitor fragment (6-22) amide is a PKA inhibitor.
In?cell biology,?protein kinase A?(PKA) is a family of?enzymes?whose activity is dependent on cellular levels of?cyclic AMP (cAMP). PKA is also regarded as?a cAMP-dependent protein kinase. PKA has various functions in the cell, such as regulation of sugar,?glycogen,?and?lipid?metabolism.
In vitro: Compared with (Ala)Kemptide, PKA inhibitor fragment (6-22) amide was found to have significant difference in inhibitory potency, likely due to the critical role of several of the nonarginine residues to this difference in potency. The minimal length analog of PKA inhibitor fragment (6-22) that inhibited CAMP-dependent protein kinase with high potency was the 17-residue PKI-(6-22)-amide. PKA inhibitor fragment (6-22) interacted at the peptide/protein binding portion of the active site in a competitive manner with a low nanomolar Ki value. To inhibit CAMP-dependent protein kinase, PKA inhibitor fragment (6-22) required both the pseudosubstrate site (residues 14-22) and additional NH2-terminal determinants within residues 6-13. PKA inhibitor fragment (6-22) could clear mimic protein and peptide substrates in interacting with the binding region of the active site particularly in the COOH-terminal pseudosubstrate basic domain. Undoubtedly, the overall affinity of PKA inhibitor fragment (6-22) was due to the number of hydrogen bonds as well as other bonding interactions with the active site of the CAMP-dependent protein kinase [1, 2].
References:
[1] 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.
[2] 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.
| Cas No. | 121932-06-7 | SDF | |
| Synonymes | PKI (6-22) amide | ||
| Formula | C80H130N28O24 | M.Wt | 1868.08 |
| Solubility | ≥186.8mg/mL in DMSO | Storage | Desiccate at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 535.3 μL | 2.6765 mL | 5.3531 mL |
| 5 mM | 107.1 μL | 535.3 μL | 1.0706 mL |
| 10 mM | 53.5 μL | 267.7 μL | 535.3 μL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
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