PD 169316 Struktur

PD 169316

Bezeichnung:PD 169316

CAS-Nr152121-53-4

Englisch Name:PD 169316

CBNumberCB7497465

SummenformelC20H13FN4O2

Molgewicht360.34

MOL-Datei152121-53-4.mol

PD 169316 physikalisch-chemischer Eigenschaften

Siedepunkt	583.1±50.0 °C(Predicted)
Dichte	1.354±0.06 g/cm3(Predicted)
storage temp.	2-8°C
Löslichkeit	DMSO: >10mg/mL
pka	9.09±0.10(Predicted)
Aggregatzustand	solid
Farbe	light orange

Sicherheit

Kennzeichnung gefährlicher	Xn
R-Sätze:	22-37/38-41
S-Sätze:	26-39
RIDADR	UN 2811 6.1/PG 3
WGK Germany	3
HS Code	2933399990

Gefahreninformationscode (GHS)

PD 169316 Chemische Eigenschaften,Einsatz,Produktion Methoden

R-Sätze Betriebsanweisung:
R22:Gesundheitsschädlich beim Verschlucken.
R37/38:Reizt die Atmungsorgane und die Haut.
R41:Gefahr ernster Augenschäden.
S-Sätze Betriebsanweisung:
S26:Bei Berührung mit den Augen sofort gründlich mit Wasser abspülen und Arzt konsultieren.
S39:Schutzbrille/Gesichtsschutz tragen.
Beschreibung
p38 is a member of the mitogen-activated protein kinase (MAPK) superfamily of enzymes that play an important role in signal transduction. PD 169316 is a selective inhibitor of p38 MAPK. It inhibits p38 MAPK with an IC₅₀ of 89 nM, whereas the IC₅₀s are >100-fold higher for extracellular signal-regulated kinase (ERK) and >1,000-fold higher for protein kinase A (PKA) and PKCα. PD 169316 inhibits apoptosis of neuronal and non-neuronal cells deprived of specific trophic factors such as potassium or nerve growth factor.
Verwenden
PD 169316 is a highly selective, potent inhibitor of p38 MAP kinase. PD 169316 inhibits transforming growth factor β-induced Smad signaling in human ovarian cancer cells. PD 169316 acts as an an endogenous suppressor of apoptosis by mimicking CD9, a membrane tetraspanin. Studies show that PD 169316 reduces myocardial ischemia/reperfusion induced voltage-dependent anion channel(VDAC) phosphorylation
Verwenden
PD 169316 has been used for the inhibition of p38 enzyme in human hepatocytes. It has been used in culture media to promote embryoid bodies differentiation.
Definition
ChEBI: 4-[4-(4-fluorophenyl)-2-(4-nitrophenyl)-1H-imidazol-5-yl]pyridine is a member of imidazoles.
Allgemeine Beschreibung
PD 169316 is a pyridinyl imidazole compound. It is a potential inhibitor of p38 mitogen-activated protein kinases. It also inhibits signalling transforming growth factor β (TGFβ), particularly in human ovarian cancer cells.
Biochem/physiol Actions
Potent, cell-permeable and selective p38 MAP kinase inhibitor (IC50 = 89 nM).
in vitro
it was reported that pretreatment of caov3 cells with 10 m pd169316 caused a significant decrease in smad2 and smad3 phosphorylation which was mediated by tgf-β. the inhibitory effect of pd 169316 was proved to act in a dose-dependent manner. study also demonstrated that pd169316 at 5 m or higher dose directly suppressed tgf-β signaling activity. [1]
in vivo
based on an amyloid β (aβ) rat model of alzheimer's disease, the effect of pd 169316 on apoptosis induced by amyloid beta was examined. it was demonstrated that caspase-3 and bax/bcl-2 ratio, two marks of apoptosis, were significantly decreased in the rats pre-treated with pd169316 intracerebroventricularly. this study suggested the potential neuroprotective role of pd 169316 against the neuronal toxicity induced by aβ. [2]
IC 50
a potent, selective and cell-permeable suppressor of p38 map kinase, with the ic50 value of 89 nm.
Einzelnachweise
[1]fu yx, o’connor lm, shepherd tg and nachtigal mw. the p38 mapk inhibitor, pd169316, inhibits transforming growth factor β-induced smad signaling in human ovarian cancer cells. biochem bioph res co. 2003. 310: 3917.
[2]ashabi g, alamdary sz, ramin m and khodagholi f. reduction of hippocampal apoptosis by intracerebroventricular administration of extracellular signal-regulated protein kinase and/or p38 inhibitors in amyloid beta rat model of alzheimer’s disease: involvement of nuclear-related factor-2 and nuclear factor-κb. basic clin. pharmacol. toxicol. 2013 aug. 112: 145–55.

PD 169316 Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

152121-53-4, PD 169316 Verwandte Suche:

Send Inquriy