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JK184,HedgehogAntagonist
品牌:Xcessbio
貨號(hào):M60087-5s
規(guī)格:5mg solid
貨期:
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JK184,HedgehogAntagonist

商品詳情 參考文獻(xiàn) 相關(guān)資料
Product Information
Molecular Weight: 350.44
Formula: C19H18N4OS
Purity: ≥ 98%
CAS#: 315703-52-7
Solubility: DMSO up to 100mM
Chemical Name: N-(4-Ethoxyphenyl)-4-(2-methylimidazo[1,2-a]pyridin-3-yl)-2-thiazolamine
Storage: Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year.

Biological Activity:?

JK184 is a potent and cell-permeable inhibitor of hedgehog (Hh) signaling downstream of Smo, identified by a cell-based Hh pathway reporter screening. JK184 was found to inhibit Adh7 (IC50?~210 nM), the class IV alcohol dehydrogenase as well as act as a microtubule depolymerizing agent in vitro. JK184 inhibits Hh agonit-induced Gli transcriptional activity (IC50?~30 nM) as well as Gli1 and Ptc1 mRNA expression in a dose-dependent manner in 10T1/2 cells. It shows antiproliferative activity in a range of cancer cell lines (IC50?~ 3 - 21 nM), and inhibits the growth of two xenografted tumors in mice in vivo.

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How to Use:?

  • In vitro:?JK184 was suggested to use at 1-5 μM concentration in vitro and in the cellular assays.
  • In vivo:?JK184 was dosed orally 0.2 mg/mouse once per day. ?

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Reference:

  • 1. Lee J, et al. A small-molecule antagonist of the hedgehog signaling pathway. (2007)?Chembiochem????? 8(16):1916-9.
  • 2. Cupido T, et al. The imidazopyridine derivative JK184 reveals dual roles for microtubules in Hedgehog signaling. (2009)Angew Chem Int Ed Engl.????? 48(13):2321-4.

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Products are for research use only. Not for human use.

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