Powder: -20°C for 3 years | In solvent: -80°C for 1 year
LDN214117 是一种高效的 ALK2 选择性抑制剂(IC50:22nM),也是一种 BMP6 抑制剂(IC50:100nM),对ALK5抑制力弱100倍。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
2 mg | ¥ 297 | 现货 | ||
5 mg | ¥ 497 | 现货 | ||
10 mg | ¥ 913 | 现货 | ||
25 mg | ¥ 1,830 | 现货 | ||
50 mg | ¥ 3,130 | 现货 | ||
100 mg | ¥ 4,590 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 547 | 现货 |
产品描述 | LDN-214117 is a potent and selective ALK2 inhibitor. |
靶点活性 | ALK2:24 nM |
体内活性 | LDN-214117对BMP6比对BMP2或BMP4表现出相对的选择性抑制。在基于细胞的测定中,LDN-214117对BMP6表现出选择性抑制,IC50约为100 nM,作用于BMP6比作用于TGF-β1选择性高164倍。LDN-214117高度抑制的激酶为ALK2,IC50为24 nM,其次为TNIK,RIPK2和ABL1。LDN-214117选择性抑制ALK2和ALK1激酶活性,抑制作用高于ALK3激酶。 |
激酶实验 | ALK2 kinase assay: Puri?ed recombinant ALK2 proteins, ATP, ATP[γ-32P], and dephosphorylated casein at ?nal concentrations of 2.5 nM, 6 μM, 0.05 μCi/μL , and 0.5 mg/mL, respectively, are aliquoted in kinase bu?er containing 0.2% BSA supplemented with 10 mM MnCl2 into 96-microwell plates, in combination with inhibitor compounds diluted at varying concentrations (0.01 nM to 100 μM). Positive control samples lacking inhibitor compounds, and negative controls lacking recombinant kinase, are also measured. The mixture is reacted at RT for 45 min, quenched with a ?nal concentration of 2% phosphoric acid. The reaction mixture is transferred to 96-well P81 phosphocellulose ?lter plates and bound for 5 min. The plates are washed 20 times with 150 μL of 1% phosphoric acid solution per well by vacuum manifold. Plates are dried at RT for 1 h, sealed, and assayed with Microscint 20 scintillation ?uid using a Spectramax L luminometer. Data is normalized to positive controls at 100% enzyme activity, with negative controls being subtracted as background. |
细胞实验 | Cells are seeded at 25000 cells per well in 96-well plates and incubated for 2 h at 37℃ and 5% CO2. Compounds of LDN-214117 or DMSO are diluted in DMEM and added at ?nal compound concentrations of 1, 10, and 100 μM. Cells are incubated for 4 and 24 h, after which the media is discarded. Cells are lysed by adding 30 μL of passive lysis bu?er and shaken at RT for 15 min. Cell viability is determined by quantifying the ATP present in each well by adding 10 μL of Cell Titer Glo per well and measuring the light output by Spectramax L luminometer. Data is normalized to 100% viability for cells receiving only DMSO.(Only for Reference) |
分子量 | 419.52 |
分子式 | C25H29N3O3 |
CAS No. | 1627503-67-6 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ethanol: 42 mg/mL (100 mM)
DMSO: 42 mg/mL (100 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
Ethanol / DMSO | 1 mM | 2.3837 mL | 11.9184 mL | 23.8368 mL | 59.5919 mL |
5 mM | 0.4767 mL | 2.3837 mL | 4.7674 mL | 11.9184 mL | |
10 mM | 0.2384 mL | 1.1918 mL | 2.3837 mL | 5.9592 mL | |
20 mM | 0.1192 mL | 0.5959 mL | 1.1918 mL | 2.9796 mL | |
50 mM | 0.0477 mL | 0.2384 mL | 0.4767 mL | 1.1918 mL | |
100 mM | 0.0238 mL | 0.1192 mL | 0.2384 mL | 0.5959 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。
LDN-214117 1627503-67-6 Angiogenesis Stem Cells Tyrosine Kinase/Adaptors ALK TGF-beta/Smad ALK2 BMP4 BMP2 Transforming growth factor beta receptors BMP6 TGF-β Receptor diffuse intrinsic pontine glioma(DIPG) oral ALK3 fibrodysplasia ossificans progressiva (FOP) ALK5 type I receptor kinases ALK1 LDN214117 bone morphogenetic proteins (BMPs) LDN 214117 Inhibitor inhibitor inhibit