SKI II

Bezeichnung:SKI II

CAS-Nr312636-16-1

Englisch Name:SKI II

CBNumberCB1498400

SummenformelC15H11ClN2OS

Molgewicht302.78

MOL-Datei312636-16-1.mol

SKI II physikalisch-chemischer Eigenschaften

Siedepunkt	507.1±60.0 °C(Predicted)
Dichte	1.415±0.06 g/cm3(Predicted)
RTECS-Nr.	SK5900000
storage temp.	2-8°C
Löslichkeit	DMSO: ≥20 mg/mL
Aggregatzustand	solid
pka	10.17±0.26(Predicted)
Farbe	off-white
Sensitive	Air & Light Sensitive
CAS Datenbank	312636-16-1

Sicherheit

WGK Germany

Gefahreninformationscode (GHS)

SKI II Chemische Eigenschaften,Einsatz,Produktion Methoden

Verwenden
SKI II is a nonlipid inhibitor of sphingosine kinase. SKI II s orally bioavailable and has shown significant inhibition of tumor growth in mice.
Definition
ChEBI: 4-[[4-(4-chlorophenyl)-2-thiazolyl]amino]phenol is a substituted aniline.
Biologische Aktivität
Selective non-lipid inhibitor of sphingosine kinase (IC 50 = 0.5 μ M); does not act at ATP-binding site. Displays no inhibition of ERK2, PI 3-kinase, or PKC α at concentrations up to 60 μ M. Reduces levels of sphingosine-1-phosphate in MDA-MB-231 breast cancer cells. Induces apoptosis and inhibits proliferation in several other tumor cell lines in vitro (IC 50 = 0.9-4.6 μ M).
Biochem/physiol Actions
Sphingosine kinase (SK) plays a pivotal role in regulating tumor growth and SK can act as an oncogene. Expression of SK RNA is significantly elevated in a variety of solid tumors, compared with normal tissue from the same patient. A number of novel inhibitors of human SK were identified, and several representative compounds were characterized in detail. These compounds demonstrated activity at sub- to micromolar concentrations, making them more potent than any other reported SK inhibitor, and were selective toward SK compared with a panel of human lipid and protein kinases. Kinetic studies revealed that the compounds were not competitive inhibitors of the ATP-binding site of SK. 4-[4-(4-chloro-phenyl)-thiazol-2-ylamino]-phenol (SKI-II) inhibitor is orally bioavailable, detected in the blood for at least 8 h, and showed a significant inhibition of tumor growth in mice with IC50 = 0.5 μM; SKI II does not act at ATP-binding site. Displays no inhibition of ERK2, PI 3-kinase, or PKCa at concentrations up to 60 μM.SKI II induces apoptosis and inhibits proliferation in several other tumor cell lines in vitro (IC50 = 0.9-4.6 μM).
Lager
Store at -20°C
Einzelnachweise
[1] french kj, schrecengost rs, lee bd, zhuang y, smith sn, eberly jl, yun jk, smith cd. discovery and evaluation of inhibitors of human sphingosine kinase. cancer res. 2003 sep 15;63(18):5962-9.

SKI II Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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