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
Para preguntas en general por favor contacte a nuestro Servicio de Atención al Cliente:
Merck KGaA
Frankfurter Str. 250
64293 Darmstadt
Germany
Teléfono: +49 6151 72-0
Fax: +49 6151 72 2000
15 febrero 2012
cargando
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.
| Información sobre producto | |||
|---|---|---|---|
| Form | Yellow solid | ||
| Protect from Light | Si | ||
| Packaged under inert gas | Si | ||
| Purity | ≥97% by HPLC | ||
| Fórmula químico | C21H21N5 | ||
| Número CAS | 356559-20-1 | ||
| Almacenar y enviar información | |||
|---|---|---|---|
|
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. |
|||
| Categoría de alamacenamiento | +2°C to +8°C | ||
| Ship |
Ambient Temperature Only
Harmful |
||
| Información de seguridad | |||
|---|---|---|---|
| Frase S |
S: 26 |
||
| Frase R |
R: 22-36/37/38 |
||
