化合物JK184 T3588
品牌 | 厂商性质 | 产地 | 货期 |
---|---|---|---|
TargetMol | 生产商 | 美国 | 现货 |
性能特点
生化试剂,可用于动物细胞实验
规格 | CAS号 | 价格 | 操作 |
---|---|---|---|
25 mg | 315703-52-7 | ¥1,190.00 | 询底价 |
100 mg | 315703-52-7 | ¥3,270.00 | 询底价 |
50 mg | 315703-52-7 | ¥1,980.00 | 询底价 |
10 mg | 315703-52-7 | ¥619.00 | 询底价 |
1 mg | 315703-52-7 | ¥169.00 | 询底价 |
500 mg | 315703-52-7 | ¥7,190.00 | 询底价 |
5 mg | 315703-52-7 | ¥372.00 | 询底价 |
1 mL | 315703-52-7 | ¥397.00 | 询底价 |
Product Introduction
Bioactivity
英文名: JK184
描述: JK184 是 Hedgehog 抑制剂,在哺乳动物细胞中的IC50值为 30 nM。
细胞实验: 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].
体外活性: JK184 is designed to antagonize Hh signaling by inhibiting glioma (Gli)-dependent transcriptional activity in a dose dependent manner. JK184 significantly inhibits the proliferation of HUVECs with IC50 of 6.3 μg/mL after three days incubation. 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) to evaluate anti-tumor effect of JK184[1]. 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)[2].
体内活性: 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].
存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year
溶解度: DMSO : 3.5 mg/mL (10 mM)
关键字: inhibit | JK184 | Inhibitor | JK-184 | Hedgehog | JK 184
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注:该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案,不可用于临床诊断或治疗等相关用途