616459
TGF-β RI Kinase Inhibitor VIII
The TGF-β RI Kinase Inhibitor VIII, also referenced under CAS 356559-20-1, controls the biological activity of TGF-β RI Kinase. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.
别名:
TGF-β RI Kinase Inhibitor VIII, ALK5 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
InChI
1S/C21H21N5/c1-13-6-5-7-16(24-13)19-18(25-20(26-19)21(2,3)4)14-8-9-15-17(12-14)23-11-10-22-15/h5-12H,1-4H3,(H,25,26)
InChI key
DKPQHFZUICCZHF-UHFFFAOYSA-N
assay
≥97% (HPLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
color
yellow
solubility
DMSO: 10 mg/mL
shipped in
ambient
Quality Level
General description
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.
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-20°:C). Stock solution is stable for up to 3 months at -20°C.
Other Notes
Due to the nature of the Hazardous Materials in this shipment, additional shipping charges may 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.
Higashiyama, H., et al. 2007. Exp. Mol. Pathol.83, 39.
Grygielko, E.T., et al. 2005. J. Pharmacol. Exp. Ther.313, 943.
Grygielko, E.T., et al. 2005. J. Pharmacol. Exp. Ther.313, 943.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Harmful (C)
存储类别
11 - Combustible Solids
wgk
WGK 3
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