616459
TGF-β RI Kinase Inhibitor VIII
SB-525334, 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, ALK5 Inhibitor VIII
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.
| Product information | |||
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| Form | Yellow solid | ||
| Molar mass | 343.4 | ||
| Protect from Light | Yes | ||
| Packaged under inert gas | Yes | ||
| Purity | ≥97% by HPLC | ||
| Solubility | DMSO | ||
| Chemical formula | C21H21N5 | ||
| CAS number | 356559-20-1 | ||
| Store and ship information | |||
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<b>Hazardous Materials Attention:</b> Due to the nature of the Hazardous Materials in this shipment, additional shipping charges <i>may</i> 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. |
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| Storage | +2°C to +8°C | ||
| Ship |
Ambient Temperature Only
Harmful |
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| Safety information | |||
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| S Phrase |
S: 26 In case of contact with eyes, rinse immediately with plenty of water and seek medical advice. |
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| R Phrase |
R: 22-36/37/38 Harmful if swallowed. |
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