373385
Hh Signaling Antagonist VII, JK184
The Hh Signaling Antagonist VII, JK184, also referenced under CAS 315703-52-7, controls the biological activity of Hh pathway. This small molecule/inhibitor is primarily used for Cell Signaling applications.
别名:
Hh Signaling Antagonist VII, JK184, N-(4-Ethoxyphenyl)-4-(2-methylimidazo[1,2-a]pyridin-3-yl)thiazol-2-amine
InChI key
ROYXIPOUVGDTAO-UHFFFAOYSA-N
InChI
1S/C19H18N4OS/c1-3-24-15-9-7-14(8-10-15)21-19-22-16(12-25-19)18-13(2)20-17-6-4-5-11-23(17)18/h4-12H,3H2,1-2H3,(H,21,22)
assay
≥98% (HPLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
color
pink
solubility
methanol: 10 mg/mL, DMSO: 40 mg/mL
shipped in
wet ice
storage temp.
−20°C
Quality Level
General description
A cell-permeable imidazopyridine compound that acts as downstream Hedgehog (Hh) pathway blocker by directly targeting the enzymatic activity of Adh7 (IC50 = 210 nM), the class IV alcohol dehydrogenase. Inhibits Hg-Ag-induced Gli-transcription activity (IC50 = 30 nM) as well as Gli1 and Ptc1 mRNA expression in a dose-dependent manner in H3H10T1/2 cells. Shown to exhibit ≥100-fold greater cytotoxicity towards five Hh activated tumor cells (GI50 ≤21 nM vs. 1.6 µM for the non-Hh activated H3H10T1/2 cells) in vitro and inhibit the growth of two xenografted tumors in mice (30-50% inhibition, 0.2 mg/mouse/day by p.o.) in vivo. Also acts as a microtubule-depolymerizing agent.
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution aliquot and freeze (-70°C). Stock solutions are stable for up to 2 weeks at -70°C.
Other Notes
Cupido, T., et al. 2009. Angew Chem.48, in press.
Lee, J., et al. 2007. ChemBioChem.8, 1916.
Lee, J., et al. 2007. ChemBioChem.8, 1916.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
存储类别
11 - Combustible Solids
wgk
WGK 3
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