| 名称 | LDN-214117 |
| 描述 | LDN-214117 is a potent and selective ALK2 inhibitor. |
| 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) |
| 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. |
| 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。 |
| 存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | Ethanol : 42 mg/mL (100.11 mM), Sonication is recommended.
DMSO : 4.2 mg/mL (10.01 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 1 mg/mL (2.38 mM), Sonication is recommended.
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| 关键字 | type I receptor kinases | Transforming growth factor beta receptors | TGF-β/Smad | TGF-β Receptor | TGFβ | TGFbeta/Smad | TGF-beta | TGFbeta | TGF-b/Smad | TGFb | Smad | oral | LDN-214117 | LDN214117 | LDN 214117 | fibrodysplasia ossificans progressiva (FOP) | diffuse intrinsic pontine glioma(DIPG) | bone morphogenetic proteins (BMPs) | BMP6 | BMP4 | BMP2 | ALK5 | ALK3 | ALK2 | ALK1 |
| 相关产品 | Entrectinib | Pirfenidone | Ceritinib | A 83-01 | Chebulinic acid | Chromenone 1 | LY-364947 | BMP signaling agonist sb4 | Alectinib hydrochloride | Alantolactone | Galunisertib | Hydrochlorothiazide |
| 相关库 | 抑制剂库 | 血管生成库 | 经典已知活性库 | 已知活性化合物库 | 抗结直肠癌化合物库 | 激酶抑制剂库 | HIF-1化合物库 | 癌细胞分化化合物库 | NO PAINS 化合物库 | TGF-β/Smad靶点化合物库 | 膜蛋白靶向化合物库 | 酪氨酸激酶分子库 |