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| 规格： | 10 mM * 1 mL | 产品价格： | ￥495.0 |
|---|---|---|---|
| 规格： | 5 mg | 产品价格： | ￥450.0 |
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JK184
CAS No. : 315703-52-7
MCE 国际站：JK184
产品活性：JK184 是一种有效的 Hedgehog (Hh) 抑制剂，在哺乳动物细胞中，IC50 为 30 nM。
研究领域：Stem Cell/Wnt
作用靶点：Hedgehog
In Vitro: JK184 is designed to antagonize Hh signaling by inhibiting glioma (Gli)-dependent transcriptional activity in a dose dependent manner. JK184 significantly inhibitts proliferation of HUVECs with IC50 of 6.3 μg/mL after three days incubation. To evaluate anti-tumor effect of JK184, MTT assay is conducted in Panc-1 and BxPC-3 cells after administration with indicated concentrations of compounds, half maximal inhibitory concentration (IC50) of JK184 (23.7 ng/mL in anc-1 and 34.3 ng/mL in BxPC-3). Claudin-low cell lines are more sensitive to JK184 treatment than are MCF10a, MTSV1-7, or HMLE-shGFP and HMLE-pBP cells, and JK184 induced a dose-dependent decrease in glioma-associated oncogene homolog 1 (GLI1) transcript and protein levels in these cells. Treatment with the IC50 dose of JK184 enhances the proportion of HMLE-shEcad cells that stained with Annexin-V, but are negative for propidium iodide (PI) (P<0.0001, t test).
In Vivo: JK184 (5 mg/kg, injected intravenously) exhibits good anti-proliferative activity in subcutaneous Panc-1 and BxPC-3 tumor models, and is a good candidate as antitumor drug targeted Hh signaling. However, JK184 has a poor pharmacokinetic profile and bioavailability.
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Oxidative Stress and Beta Cell Dysfunction
Endocrinol Metabol 52:146–155, 2008; Pietropaolo M et al., Pediatr Diabetes 6:184–192, 2005).
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