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.

• Synonym(s): Hh Signaling Antagonist VII, JK184, N-(4-Ethoxyphenyl)-4-(2-methylimidazo[1,2-a]pyridin-3-yl)thiazol-2-amine
• Empirical Formula (Hill Notation): C₁₉H₁₈N₄OS
• CAS Number: 315703-52-7
• Molecular Weight: 350.44
• UNSPSC Code: 12352200

Properties

• Quality Level: 100
• 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
• 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)
• InChI key: ROYXIPOUVGDTAO-UHFFFAOYSA-N

Description

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

Warning

Toxicity: Standard Handling (A)

Reconstitution

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.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Safety Information

• Storage Class: 11 - Combustible Solids
• wgk_germany: WGK 3