Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ciliobrevin A (HPI-4) 是Hedgehog(Hh) 信号通路抑制剂,平均抑制浓度 (IC50) 值小于 10 μM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
2 mg | ¥ 279 | 现货 | ||
5 mg | ¥ 438 | 现货 | ||
10 mg | ¥ 591 | 现货 | ||
25 mg | ¥ 1,330 | 现货 | ||
50 mg | ¥ 2,480 | 现货 | ||
100 mg | ¥ 3,970 | 现货 | ||
200 mg | ¥ 5,680 | 现货 | ||
500 mg | ¥ 8,690 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 493 | 现货 |
产品描述 | Ciliobrevin A (HPI-4) is an inhibitor of hedgehog signaling pathway with an IC50 <10 μM. |
靶点活性 | Hh:>10 μM. |
体外活性 | Shh-EGFPFLAG-Gli2 cells cultured with Ciliobrevin A have truncated primary cilia, and this cellular organelle is absent in a significant fraction of Ciliobrevin A-treated cells. Ciliobrevin A perturbs primary cilia formation in the Shh-LIGHT2FLAG-Gli1 cells and promotes accumulation of FLAG-Gli1 at the distal tip of this organelle. Ciliobrevin A significantly inhibits the proliferation of these neuronal progenitors, as measured by histone H3 phosphorylation (pH3) levels, and reduces cellular levels of cyclin D1 protein and Gli1, Gli2, and N-Myc transcripts in the CGNPs. Ciliobrevin A can block the proliferation of SmoM2-expressing CGNPs and should be equally potent against CGNPs lacking Su(fu) function, whereas the Smo inhibitor Cyclopamine is ineffective against either oncogenic lesion. Ciliobrevin A prevents an increase in the FLAG-Gli2 full-length/repressor ratio upon Shh stimulation, but HPI-2 and HPI-3 have no significant effect. Ciliobrevin A increases ciliary levels of FLAG-Gli2 in a manner disproportionate to their effects on total FLAG-Gli2 levels[1]. |
激酶实验 | Smo-binding assays are conducted with BODIPY-cyclopamine and Smo-overexpressing HEK 293T cells, using a CMVpromoter-based SV40 origin-containing expression construct for Smo-Myc3 (murine Smo containing three consecutive Myc epitopes at the C terminus). HEK 293T cells are seeded into eight-well chambered coverslips (80,000 cells/well) and cultured in DMEM containing 10% FBS, 100 U/mL penicillin, and 0.1 mg/mL streptomycin. The cells are cultured until they reached 55 to 65% confluency (14-18 h), after which they are transfected with the Smo-Myc3 expression construct and Transit-LT1. Twenty-four hours after transfection, the cells are washed with PBS and cultured in DMEM containing 0.5% FBS, 5 nM BODIPY-cyclopamine, and various concentrations of either cyclopamine or individual HPIs. After 30 min, 10 μM Hoescht 33342 is added to each well, and the HPIs are incubated with the cells for an additional 30 min. The cells are then washed two times with PBS buffer, once with phenol red-free DMEM containing 0.5% FBS, and immediately imaged using a DMI6000B compound microscope. Images are background-substracted using ImageJ software with a rolling ball size of 75 pixels, and BODIPY-cyclopamine intensity is then determined using Metamorph software. Circular regions with a diameter of 300 pixels are placed over regions containing uniformly confluent cells, and the pixel intensities of approximately 20 regions from four independent images is used to determine the average BODIPY-cyclopamine levels for each experimental condition[1]. |
细胞实验 | Using MTS-8 assay to measure cell proliferation and the toxicity of this drug. 2000 cells were plated in 96-well plates per well. HPI-4 was added to cells at concentrations of 0, 5 and 10 μM in 100 μl DMEM/F12 with 10% FBS and incubated for 0, 1, 3, 6 and 9 days. Then, 10 μl MST-8 was added to the media in each well and incubated in an environment without light for 90 min. The absorbance value was measured using an enzyme microplate reader at 450 nm wavelength. The relative viability of cells was expressed by OD value.(Only for Reference) |
别名 | Hedgehog Pathway Inhibitor 4, HPI-4 |
分子量 | 358.18 |
分子式 | C17H9Cl2N3O2 |
CAS No. | 302803-72-1 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 70 mg/mL (195.43 mM)
Ethanol: 1 mg/mL (2.79 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO / Ethanol | 1 mM | 2.7919 mL | 13.9595 mL | 27.9189 mL | 69.7973 mL |
DMSO | 5 mM | 0.5584 mL | 2.7919 mL | 5.5838 mL | 13.9595 mL |
10 mM | 0.2792 mL | 1.3959 mL | 2.7919 mL | 6.9797 mL | |
20 mM | 0.1396 mL | 0.698 mL | 1.3959 mL | 3.4899 mL | |
50 mM | 0.0558 mL | 0.2792 mL | 0.5584 mL | 1.3959 mL | |
100 mM | 0.0279 mL | 0.1396 mL | 0.2792 mL | 0.698 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Ciliobrevin A 302803-72-1 GPCR/G Protein Stem Cells Hedgehog/Smoothened Hedgehog Pathway Inhibitor 4 Hedgehog HPI 4 HPI-4 HPI4 inhibit Inhibitor inhibitor