KT5720 Struktur

KT5720

Bezeichnung:KT5720

CAS-Nr108068-98-0

Englisch Name:KT5720

CBNumberCB6665746

SummenformelC32H31N3O5

Molgewicht537.61

MOL-Datei108068-98-0.mol

KT5720 physikalisch-chemischer Eigenschaften

Siedepunkt	715.0±60.0 °C(Predicted)
Dichte	1.49±0.1 g/cm3(Predicted)
storage temp.	−20°C
Löslichkeit	methanol: 5 mg/mL
Aggregatzustand	powder
pka	11.96±0.40(Predicted)
Farbe	white
Stabilität	Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 3 months.

Sicherheit

Kennzeichnung gefährlicher	Xi
R-Sätze:	36/38
S-Sätze:	26-36
WGK Germany	-
F	10
HS Code	29419090

Gefahreninformationscode (GHS)

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 IC₅₀ 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™ .
Biochem/physiol Actions
Cell permeable: yes
Lager
-20°C (desiccate)
Einzelnachweise
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

KT5720 Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

108068-98-0, KT5720 Verwandte Suche:

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