Product Details
| Product Name:
JK184 |
CAS No.:
315703-52-7 |
| Purity:
99.89% |
Supply Ability:
10g |
| Release date:
2024/11/06 |
Product Introduction
Bioactivity
| 名稱 | JK184 |
| 描述 | JK184, a potent Hedgehog (Hh) pathway inhibitor. |
| 細(xì)胞實(shí)驗(yàn) | 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]. |
| 體外活性 | 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]. |
| 體內(nèi)活性 | JK184 (5 mg/kg, injected intravenously) demonstrates strong anti-proliferative activity in subcutaneous Panc-1 and BxPC-3 tumor models, making it a promising candidate as an antitumor drug targeting Hh signaling. Histological analysis revealed that JK184 enhances anti-tumor activity by inducing apoptosis, decreasing microvessel density, and reducing CD31, Ki67, and VEGF expression in tumor tissues. However, JK184 exhibits a poor pharmacokinetic profile and bioavailability[1]. |
| 存儲(chǔ)條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | DMSO : 3.5 mg/mL (10 mM), Sonication is recommended.
|
| 關(guān)鍵字 | inhibit | JK184 | Inhibitor | JK-184 | Hedgehog | JK 184 |
| 相關(guān)產(chǎn)品 | Itraconazole | Naftifine hydrochloride | GANT 61 | ALLO-2 | Ellagic acid | Triparanol | Vismodegib | BMS-833923 | Ciliobrevin A | Tolnaftate | SAG | SMO-IN-2 |
| 相關(guān)庫(kù) | 表型篩選靶點(diǎn)鑒定庫(kù) | 經(jīng)典已知活性庫(kù) | 膜蛋白靶向化合物庫(kù) | 抗肥胖化合物庫(kù) | 抑制劑庫(kù) | NO PAINS 化合物庫(kù) | 已知活性化合物庫(kù) | GPCR靶點(diǎn)分子庫(kù) | 抗癌化合物庫(kù) | 神經(jīng)元分化化合物庫(kù) |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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Recommended supplier
| Product name |
Price |
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Suppliers |
Update time |
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$1.00/1KG |
VIP5Y
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Career Henan Chemical Co
|
2019-12-25 |
United States