JK184, Hedgehog Antagonist


Catalog No. size PriceQuantity
M60087-5S 5mg solid $79
M60087-10S 10mg solid $328

Description

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.

 

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.  

 

 

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.

 

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

 

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