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Stock availabilitIn Stock
In Stock
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CAS number
108068-98-0
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Description
PKA kinase inhibitor
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Molecular weight
537,6 g/mol
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Primary research fields
Cell Signaling, Cancer, Apoptosis, Cancer Growth Inhibitors, Tyrosine Kinase Inhibitors
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Other name
(9S,10S,12R)-2,3,9,10,11,12-Hexahydro-10-hydroxy-9-methyl-1-oxo-9,12-epoxy-1H-diindolo[1,2,3-fg:3′,2′,1′-kl]pyrrolo[3,4-i][1,6]benzodiazocine-10-carboxylic acid hexyl ester
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Product category
Small Molecules
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Product type
Inhibitor
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Chemical formula
C32H31N3O5
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Origin
Synthetic
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Purity pourcentage
≥98% (TLC)
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Soluble in
Soluble in methanol: clear colorless solution at 5 mg/ml
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Physical appearance
White powder
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Storage recommendations
-20ºC
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Shipping recommendations
Shipped Ambient
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Safety information
Classification: Specific target organ toxicity-single exposure (Category 1), H370 Safety Phrases: S22 - Do not breathe dust. S24/25 - Avoid contact with skin and eyes. S36/37/39 - Wear suitable protective clothing, gloves and eye/face protection. Hazard statements: H370 Causes damage to organs. Precautionary statements: P260 Do not breathe dust/ fume/ gas/ mist/ vapours/ spray. P264 Wash skin thoroughly after handling. P270 Do not eat, drink or smoke when using this product. P307 + P311 IF exposed: Call a POISON CENTER or doctor/ physician. P321 Specific treatment (see supplemental first aid instructions on this label). P405 Store locked up. P501 Dispose of contents/ container to an approved waste disposal plant
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PubChem number
3844
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Scientific context
KT5720 is a potent and selective inhibitor of protein kinase A (PKA). This compound blocks PKA signaling through competitive inhibition. It causes no significant effect on protein kinase C (PKC), protein kinase G (PKG) or myosin light chain kinase (mlCK). KT5720 has been shown to reversibly arrests human skin fibroblasts in the G1 phase. It is cell permeable.
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Bibliography
1. Kase H., et al. (1987) Biochem. Biophys. Res. Comm. 142(2): 436–440. 2. Gadbois D.M., Crissman H.A., Tobey R.A., & Bradbury E.M. (1992) Pro. Na. Aca. Sci. USA. 89(18): 8626–8630.
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Release date
1-Oct-2014
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PubMed number
Refer to PubMed
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Tested applications
To be tested
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Tested reactivity
To be tested
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Representative figure legend
Chemical structure of KT5720 (SIH-457), a PKA kinase inhibitor. CAS #: 108068-98-0. Molecular Formula: C32H31N3O5. Molecular Weight: 537.6 g/mol. Chemical structure of KT5720, a PKA kinase inhibitor (SIH-457). CAS # 108068-98-0. Molecular Formula: C32H31N3O5.
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Warning information
Non-hazardous
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Country of production
Canada
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Total weight kg
0.25
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Net weight g
0.0001
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Additional description
Tissue, pathway, proteinase, peptidase, protease ,acrosin, lipoprotein, activator, caspase, trypsin, papain, esterase inhibitors are proteins or receptor ligands or receptor antagonists that bind to an enzyme receptor and decreases its activity. Since blocking an enzyme's activity can kill a pathogen or correct a metabolic imbalance, many drugs are enzyme inhibitors. Not all receptor antagonist that bind to enzymes are inhibitors; enzyme activator ligands or agonists bind to enzymes and increase their enzymatic activity, while enzyme substrates bind and are converted to products in the normal catalytic cycle of the enzyme.
