Powder: -20°C for 3 years | In solvent: -80°C for 1 year
JK184 is a potent Hedgehog (Hh) pathway inhibitor.
パッケージサイズ | 在庫状況 | 単価(税別) | |||
---|---|---|---|---|---|
サンプルについてお問い合わせ | |||||
5 mg | 在庫あり | ¥ 11,000 | |||
10 mg | 在庫あり | ¥ 18,000 | |||
25 mg | 在庫あり | ¥ 41,000 | |||
50 mg | 在庫あり | ¥ 71,000 | |||
100 mg | 在庫あり | ¥ 117,500 | |||
500 mg | 在庫あり | ¥ 248,000 | |||
1 mL * 10 mM (in DMSO) | 在庫あり | ¥ 12,500 |
説明 | JK184 is a potent Hedgehog (Hh) pathway inhibitor. |
ターゲット&IC50 | Hedgehog:30 nM |
In vitro | JK184 is specifically designed to counteract Hedgehog (Hh) signaling through the inhibition of glioma-associated oncogene (Gli)-dependent transcriptional activity in a dose-dependent fashion. It effectively reduces the growth of human umbilical vein endothelial cells (HUVECs) with a half maximal inhibitory concentration (IC50) of 6.3 μg/mL following a three-day incubation period. Moreover, MTT assays reveal that JK184 significantly restricts tumor growth in Panc-1 and BxPC-3 cell lines, demonstrating IC50 values of 23.7 ng/mL and 34.3 ng/mL, respectively. Notably, cell lines characterized by lower levels of the tight junction protein claudin show increased sensitivity to JK184, with the compound inducing a dose-dependent reduction in both GLI1 mRNA and protein expressions. Additionally, administering JK184 at the IC50 concentration significantly increases Annexin-V staining in HMLE-shEcad cells while maintaining negativity for propidium iodide (PI) staining, indicating a pronounced pro-apoptotic effect without compromising cell membrane integrity (P<0.0001, t-test)[1][2]. |
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. Histological analysis showed that JK184 improved anti-tumor activity by inducing more apoptosis, decreasing microvessel density, and reducing expression of CD31, Ki67, and VEGF in tumor tissues. However, JK184 has a poor pharmacokinetic profile and bioavailability[1]. |
細胞研究 | JK184 is dissolved in DMSO and stored, and then diluted with appropriate medium before use[1]. The Shh-LIGHT2 cells are seeded in 96-well plates and grown to confluency. The Shh-LIGHT2 cells are treated with various concentrations of JK184 micelles or free JK184 or micelles in DMEM containing 0.5% CS, 0.1 mg/mL streptomycin, 100 U/mL penicillin, 5% Shh-N conditioned medium obtained from Shh-N-producing HEK293 cells. The treated cells are cultured further for 60 h, and firefly and Renilla luciferase activities are measured using a dual luciferase kit. Proliferation assay or apoptosis evaluation of HUVECs is measured using MTT method or FCM analysis, respectively. HUVECs are treated with a series concentration of free JK184, JK184 micelles, or blank MPEG-PCL micelles for 48 h, respectively. The mean percentage of cell inhibition or apoptosis is calculated[1]. |
分子量 | 350.44 |
分子式 | C19H18N4OS |
CAS No. | 315703-52-7 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 3.5 mg/mL (10 mM), Sonication is recommended.
You can also refer to dose conversion for different animals. 詳細
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JK184 315703-52-7 GPCR/G Protein Stem Cells Hedgehog/Smoothened inhibit Inhibitor JK-184 Hedgehog JK 184 inhibitor