KT5720 Chemische Eigenschaften,Einsatz,Produktion Methoden
R-Sätze Betriebsanweisung:
R36/38:Reizt die Augen und die Haut.
S-Sätze Betriebsanweisung:
S26:Bei Berührung mit den Augen sofort gründlich mit Wasser abspülen und Arzt konsultieren.
S36:DE: Bei der Arbeit geeignete Schutzkleidung tragen.
Beschreibung
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 K
i value of 60 nM. Reported IC
50 values vary widely depending upon ATP concentration tested and can range from 56 nM (low ATP) to 3 μM (physiologic ATP). 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.
Chemische Eigenschaften
White solid
Verwenden
KT 5720 is a potent, specific and cell-permeable inhibitor of PKA.
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.
Biologische Aktivität
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™ .
KT5720 Upstream-Materialien And Downstream Produkte
Upstream-Materialien
Downstream Produkte
