219332
β-Catenin/Tcf Inhibitor III, iCRT3
2-(((2-(4-Ethylphenyl)-5-methyl-1,3-oxazol-4-yl)methyl)sulfanyl)-N-(2-phenylethyl)acetamide, Inhibitor of β-Catenin Responsive Transcription, Wnt Pathway Inhibitor VIII
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メルク株式会社
目黒区下目黒1-8-1
153-8927 東京
Japan
TEL： 0120-189-390
Fax: 0120-189-350
E-mail mj_service@merckgroup.com
31 5月 2012
ローディング
A cell-permeable oxazole compound that acts as a selective CRT (β-catenin responsive transcription) inhibitor (IC50 = 8.2 nM against Wnt3a-dependent SuperTopFlash STF16-luc reporter activity in HEK293 cultures) by interfering with β-cat-TCF4 interaction via direct β-catenin (β-cat) binding, while exhibiting much reduced activity against Hedgehog, Jak/Stat, or Notch signaling pathway-dependent transcription activation. Effectively inhibits cellular expression of CRT target genes, including WISP1, AXN2, and CYCD1, in a dose-dependent manner (25 to 75 µM), and selectively inhibits the proliferation of HCT116 (75 µM), HT29 (75 µM), and several primary human colon cancer cultures (6.25 to 100 µg/ml; average IC50 ~36 µg/ml) that require sustained Wnt/CRT activity for survival.
| 製品情報 | |||
|---|---|---|---|
| Form | Tan powder | ||
| Protect from Light | はい | ||
| Packaged under inert gas | はい | ||
| Purity | ≥95% by HPLC | ||
| 化学式 | C23H26N2O2S | ||
| 保管と送付情報 | |||
|---|---|---|---|
| Storage | -20°C | ||
| Ship |
Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
Standard Handling |
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