N-[3-[[5-Iodo-4-[[3-[(2-thienylcarbonyl)amino]propyl]amino]-2-pyrimidinyl]amino]phenyl]-1-pyrrolidinecarboxamide Chemische Eigenschaften,Einsatz,Produktion Methoden
Beschreibung
3-
Phosphoinositide-
dependent protein kinase 1 (PDK1) is a serine-
threonine kinase that phosphorylates and activates a range of other kinases, including PKB, PKA, and certain isoforms of PKC. BX-
795 is a potent, ATP-
competitive inhibitor of PDK1
in vitro (IC
50 = 11 nM) and in cells (IC
50 = 300 nM). At comparable concentrations, BX-
795 also inhibits ERK8, MAPK-
interacting kinase 2, Aurora B, Aurora C, MAP/microtubule affinity-
regulating kinases 1-
4, TNF receptor associated factor-
associated NF-
κB activator-
binding kinase 1, IκB kinase ε, and additional kinases.
Verwenden
BX-795 hydrochloride has been used to study the effect of kinase inhibition on human endogenous retroviruses (HERVs) transcription activation.
Biochem/physiol Actions
BX-795 competes for the ATP (adenosine triphosphate) binding pocket of 3-phosphoinositide-dependent kinase-1 (PDK1) with its substrate ATP. In vitro assays reveal that BX-795 might inhibit Unc-51 (serine/threonine-protein kinase)-like autophagy activating kinase (ULK1).
N-[3-[[5-Iodo-4-[[3-[(2-thienylcarbonyl)amino]propyl]amino]-2-pyrimidinyl]amino]phenyl]-1-pyrrolidinecarboxamide Upstream-Materialien And Downstream Produkte
Upstream-Materialien
Downstream Produkte