K-252A Chemische Eigenschaften,Einsatz,Produktion Methoden
S-S?tze Betriebsanweisung:
S22:Staub nicht einatmen.
S24/25:Berührung mit den Augen und der Haut vermeiden.
Beschreibung
K252a is a staurosporine analog isolated from
Nocardiopsis sp. soil fungi that inhibits protein kinase (PK) C, PKA, Ca
2+/calmodulin-
dependent kinase type II, and phosphorylase kinase with IC
50 values of 470, 140, 270, and 1.7 nM, respectively. Because it inhibits neurotrophin receptor tyrosine kinases, K252a at 100-
500 nM has been used to suppress trophoblast proliferation and increase apoptosis associated with the disruption of mitochondrial functions in cultured choriocarcinoma cells. Recently, K252a has been shown to inhibit PRK1 (IC
50 = 3.2 nM
in vitro), a PKC-
related kinase that phosphorylates histone H3 at threonine 11 and is involved in androgen-
dependent gene expression.
Verwenden
K-252a is used to inhibit protein kinases involved in cell signaling processes, including CaM kinase; phosphorylase kinase, serine/threonine kinases, Trk. It is used to inhibit the actions of nerve growth factor (NGF) on PC1 2 cells and to inhibit smooth muscle myosin light chain kinase .
Definition
ChEBI: A organic heterooctacyclic compound that is a potent inhibitor of protein kinase C and is isolated from Nocardiopsis sp K-252a
Biologische Aktivit?t
Non-selective protein kinase inhibitor; analog of staurosporine. Inhibits PKC (IC 50 = 32.9 nM), Ca 2+ /calmodulin-stimulated phosphodiesterases (IC 50 = 1.3-2.9 μ M), MLCK (K i = 20 nM) and receptor tyrosine kinases. Inhibits the oncogenic properties of MET; prevents autophosphorylation and activation of downstream effectors (MAPK, Akt).
K-252A Upstream-Materialien And Downstream Produkte
Upstream-Materialien
Downstream Produkte
