KT5720
Sign in to saveAlso known as KT 5720, KT-5720
KT5720 is a kinase inhibitor with specificity towards protein kinase A. It is a semi-synthetic derivative of K252a and analog of staurosporine.
Chemical data
- Formula
- C32H31N3O5
- Molecular weight
- 537.6 g/mol
- IUPAC name
- hexyl (15R,16S,18S)-16-hydroxy-15-methyl-3-oxo-28-oxa-4,14,19-triazaoctacyclo[12.11.2.115,18.02,6.07,27.08,13.019,26.020,25]octacosa-1,6,8,10,12,20,22,24,26-nonaene-16-carboxylate
via PubChem
Drug data · ChEMBL
- Molecule type
- Small molecule
via ChEMBL · EBI
Research
980 papers- The Protein Kinase A Inhibitor KT5720 Prevents Endothelial Dysfunctions Induced by High-Dose Irradiation.International journal of molecular sciences · 2024
- KT5720 and U-98017 inhibit MAPK and alter the cytoskeleton and cell morphology.Journal of cellular physiology · 1998
- K252a, KT5720, KT5926, and U98017 support paclitaxel (taxol)-dependent cells and synergize with paclitaxel.
~2 min read
Article
4 sectionsContents
- Physiological Effects
- Protein kinase A
- Non-PKA Targets
- References
KT5720 is a kinase inhibitor with specificity towards protein kinase A. It is a semi-synthetic derivative of K252a and analog of staurosporine.
== Physiological Effects == === Protein kinase A === KT5720 is an antagonist of protein kinase A. Protein kinase A (PKA) is a group of kinases that are cAMP-dependent that primarily phosphorylate serine or threonine residues in target proteins. PKA is a tetramer consisting of two catalytic subunits and two regulatory subunits, with the later holding the catalytic subunits in an inactive state. The binding of two cAMP molecules to each regulatory subunit causes an allosteric change that detaches the regulatory subunits from the catalytic subunits. This exposes the ATP-binding site of the kinase. KT5720 binds competitively to the ATP-binding site of the catalytic subunit of PKA and its effects are dependent on the cellular concentration of ATP.