373385
Hh Signaling Antagonist VII, JK184
N-(4-Ethoxyphenyl)-4-(2-methylimidazo[1,2-a]pyridin-3-yl)thiazol-2-amine
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EMD Chemicals, Inc.
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13 February 2012
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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.
| Product information | |||
|---|---|---|---|
| Form | Pink solid | ||
| Molar mass | 350.4 | ||
| Protect from Light | Yes | ||
| Packaged under inert gas | Yes | ||
| Purity | ≥98% by HPLC | ||
| Solubility | DMSO or MeOH | ||
| Chemical formula | C19H18N4OS | ||
| CAS number | 315703-52-7 | ||
| Store and ship information | |||
|---|---|---|---|
| Storage | -20°C | ||
| Ship |
Shipped with Blue Ice or with Dry Ice
Standard Handling |
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