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.
CAS Number: 315703-52-7
Molecular Weight: 350.44
Chemical Name: N-(4-Ethoxyphenyl)-4-(2-methylimidazo[1,2-a]pyridin-3-yl)-2-thiazolamine
Appearance: Solid Power.
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO up to 100mM
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined.
HS Tariff Code: 382200
How to use
JK184 was suggested to use at 1-5 µM concentration in vitro and in the cellular assays.
JK184 was dosed orally 0.2 mg/mouse once per day.
- Lee J, et al. A small-molecule antagonist of the hedgehog signaling pathway. (2007) Chembiochem 8(16):1916-9.
- 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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