KT 5720 |
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Catalog No.GC14648
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protein kinase A inhibitor, potent and selective
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 108068-98-0
Sample solution is provided at 25 µL, 10mM.
Protein kinase A (PKA) regulates multiple signal transduction events via protein phosphorylation and is integral to all cellular responses involving the cyclic AMP second messenger system. KT 5720 is one of a family of compounds synthesized by the fungus Nocardiopsis sp. It blocks PKA signaling through competitive inhibition of ATP with a Ki value of 60 nM.[1] Reported IC50 values vary widely depending upon ATP concentration tested and can range from 56 nM (low ATP) to 3 µM (physiologic ATP).[2],[3] Non-specific effects of KT 5720 include inhibition of phosphorylase kinase, PDK1, MEK, MSK1, PKBα, and GSK3β at concentrations as effective as or more potent than that for inhibition of PKA.[2],[3]
Reference:
[1]. Kase, H., Iwahashi, K., Nakanishi, S., et al. K-252 compounds, novel and potent inhibitors of protein kinase C and cyclic nucleotide-dependent protein kinases. Biochemical and Biophysical Research Communications 142(2), 436-440 (1987).
[2]. Davies, S.P., Reddy, H., Caivano, M., et al. Specificity and mechanism of action of some commonly used protein kinase inhibitors. Biochem. J. 351(1), 95-105 (2000).
[3]. Murray, A.J. Pharmacological PKA inhibition: All may not be what it seems. Science Signaling 1(22), (2008).
| Cas No. | 108068-98-0 | SDF | |
| Chemical Name | (5S,6S,8R)-hexyl 6,13-dihydroxy-5-methyl-6,7,8,15-tetrahydro-5H-16-oxa-4b,8a,14-triaza-5,8-methanodibenzo[b,h]cycloocta[jkl]cyclopenta[e]-as-indacene-6-carboxylate | ||
| Canonical SMILES | CCCCCCOC([C@]([C@@]12C)(O)C[C@](O2)([H])N3C4=CC=CC=C4C5=C6C(CN=C6O)=C7C8=CC=CC=C8N1C7=C53)=O | ||
| Formula | C32H31N3O5 | M.Wt | 537.61 |
| Solubility | DMSO: 1 mg/ml; Methanol: 5 mg/ml | Storage | Store 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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.8601 mL | 9.3004 mL | 18.6008 mL |
| 5 mM | 372 μL | 1.8601 mL | 3.7202 mL |
| 10 mM | 186 μL | 930 μL | 1.8601 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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 saline, 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% Appearance: A clear film
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 14 reference(s) in Google Scholar.)