A cell-permeable dihydroquinoline compound that potently and specifically inhibits cellular JAK1/JAK2/TYK2/STAT3 activation (IC50 against U266 constitutive STAT3 Y705 phosphorylation =170 nM) as well as the transcription of STAT3 target genes, while exhibiting little effects against pathways involved in Akt/mTOR, Erk1/2, or STAT5 activation. Since the inhibitor does not affect JAK1/2/3 kinase activity, its cellular target(s) appears to be upstream of JAKs.
Packaging
Packaged under inert gas
Warning
Toxicity: Standard Handling (A)
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Xu, J., et al. 2008. J. Med. Chem.51, 4115.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Storage Class Code
11 - Combustible Solids
WGK
WGK 3
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
Certificates of Analysis (COA)
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Aberrant RON signaling is present in numerous cancers including breast cancer. Evidence suggests that the ligand, hepatocyte growth factor-like (HGFL), is also overexpressed in breast cancer. RON (MST1R) and HGFL (MST1) genes are located on human chromosome 3 and mouse
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