KT5720
Synonym(s):;InSolution KT5720 - CAS 108068-98-0 - Calbiochem;KT5720 - CAS 108068-98-0 - Calbiochem;PKA Inhibitor VII
- CAS NO.:108068-98-0
- Empirical Formula: C32H31N3O5
- Molecular Weight: 537.61
- MDL number: MFCD09878277
- EINECS: 810-587-2
- SAFETY DATA SHEET (SDS)
- Update Date: 2024-10-23 13:36:13
What is KT5720?
Description
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. Reported IC50 values vary widely depending upon ATP concentration tested and can range from 56 nM (low ATP) to 3 μM (physiologic ATP). Non-
Chemical properties
White solid
The Uses of KT5720
KT 5720 is a potent, specific and cell-permeable inhibitor of PKA.
What are the applications of Application
KT 5720 is a potent, specific and cell-permeable inhibitor of PKA, able to block PKA signaling through the competitive inhibition of ATP.
Definition
ChEBI: An organic heterooctacyclic compound that is 1H,1'H-2,2'-biindole in which the nitrogens have undergone formal oxidative coupling to positions 2 and 5 of hexyl (3S)-3-hydroxy-2-methyltetrahydrofuran-3- arboxylate (the 2R,3S,5S product), and in which the 3 and 3' positions of the biindole moiety have also undergone formal oxidative coupling to positions 3 and 4 of 1,5-dihydro-2H-pyrrol- -one.
Biological Activity
Potent, selective inhibitor of protein kinase A (K i = 60 nM). Has no effect on PKG or PKC (K i > 2 μ M). Reversibly arrests human skin fibroblasts in the G 1 phase. Also available as part of the Mixed Kinase Inhibitor Tocriset™ and PKA Tocriset™ .
Biochem/physiol Actions
Cell permeable: yes
storage
-20°C (desiccate)
References
1) Kase et al. (1987), K-252 compounds, novel and potent inhibitors of protein kinase C and cyclic nucleotide-dependent protein kinases; Biochem. Biophys. Res. Commun., 142 436 2) Cabell et al. (1993), Effects of selective inhibition of protein kinase C, cyclic AMP-dependent protein kinase, and Ca(2+)-calmodulin-dependent protein kinase on neurite development in cultured rat hippocampal neurons; Int. J. Dev. Neurosci., 11 357
Properties of KT5720
Boiling point: | 715.0±60.0 °C(Predicted) |
Density | 1.49±0.1 g/cm3(Predicted) |
storage temp. | −20°C |
solubility | methanol: 5 mg/mL |
form | powder |
pka | 11.96±0.40(Predicted) |
color | white |
Stability: | Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 3 months. |
Safety information for KT5720
Signal word | Warning |
Pictogram(s) |
Exclamation Mark Irritant GHS07 |
GHS Hazard Statements |
H315:Skin corrosion/irritation H319:Serious eye damage/eye irritation H335:Specific target organ toxicity, single exposure;Respiratory tract irritation |
Precautionary Statement Codes |
P261:Avoid breathing dust/fume/gas/mist/vapours/spray. P271:Use only outdoors or in a well-ventilated area. P280:Wear protective gloves/protective clothing/eye protection/face protection. |
Computed Descriptors for KT5720
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