616459
TGF-β RI Kinase Inhibitor VIII
6-(2-tert-Butyl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-4-yl)-quinoxaline, Transforming Growth Factor-β Type I Receptor Kinase Inhibitor VIII, SB-525334, ALK5 Inhibitor VIII
Wenn Sie allgemeine Fragen haben, wenden Sie sich bitte an unseren Kundenservice:
Merck KGaA
Frankfurter Str. 250
64293 Darmstadt
Germany
Telefon: +49 6151 72-0
Fax: +49 6151 72 2000
15 Februar 2012
wird geladen
A cell-permeable quinoxaline compound that acts as a potent, highly selective, ATP-competitive inhibitor against type I TGF-β receptor TβR-I/ALK5 (IC50 = 14.3 nM), while exhibiting 4-fold less potency toward ALK4 (IC50 = 58.5 nM) and little or no activity against ALK2/3/6 and a panel of 26 other commonly studied kinases (≤29% inhibition at 10 µM). Effectively blocks (by >95%) TGF-β1-induced Smad2/3 activation (2 µM in ELT-3 cultures) and nuclear localization (1 µM in RPTE cultures), as well as TGF-β1-dependent p3TP- and ARE-luciferase transcription (0.1 µM in HaCat cultures). SB-525334 is orally available and is shown to attenuate Bleomycin- and Puromycin-induced tissue fibrosis in mice and rats in vivo.
| Produktinformationen | |||
|---|---|---|---|
| Form | Yellow solid | ||
| Protect from Light | Ja | ||
| Packaged under inert gas | Ja | ||
| Purity | ≥97% by HPLC | ||
| Chemische Formel | C21H21N5 | ||
| CAS-Nummer | 356559-20-1 | ||
| Lager- und Versandinformationen | |||
|---|---|---|---|
|
Hazardous Materials Attention: Due to the nature of the Hazardous Materials in this shipment, additional shipping chargesmay be applied to your order. Certain sizes may be exempt from the additional hazardous materials shipping charges. Please contact your local sales office for more information regarding these charges. |
|||
| Lagerkategorie | +2°C to +8°C | ||
| Ship |
Ambient Temperature Only
Harmful |
||
| Sicherheitshinweise | |||
|---|---|---|---|
| S-Satz |
S: 26 |
||
| R-Satz |
R: 22-36/37/38 |
||
