| 名稱(chēng) | LDN-214117 |
| 描述 | LDN-214117 is a potent and selective ALK2 inhibitor. |
| 細(xì)胞實(shí)驗(yàn) | 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) |
| 激酶實(shí)驗(yàn) | 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. |
| 體內(nèi)活性 | LDN-214117對(duì)BMP6比對(duì)BMP2或BMP4表現(xiàn)出相對(duì)的選擇性抑制。在基于細(xì)胞的測(cè)定中,LDN-214117對(duì)BMP6表現(xiàn)出選擇性抑制,IC50約為100 nM,作用于BMP6比作用于TGF-β1選擇性高164倍。LDN-214117高度抑制的激酶為ALK2,IC50為24 nM,其次為T(mén)NIK,RIPK2和ABL1。LDN-214117選擇性抑制ALK2和ALK1激酶活性,抑制作用高于ALK3激酶。 |
| 存儲(chǔ)條件 | 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 : 21.43 mg/mL (51.08 mM), Sonication is recommended.
10% DMSO+90% Saline : 2.14 mg/mL (5.1 mM), Solution.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 1 mg/mL (2.38 mM), Sonication is recommended.
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| 關(guān)鍵字 | 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 |
| 相關(guān)產(chǎn)品 | Trimethylamine N-oxide | Pirfenidone | Crizotinib | Melamine | A 83-01 | SB-431542 | Alectinib | Cetrimonium bromide | Galunisertib | Alantolactone | Brigatinib | Hydrochlorothiazide |
| 相關(guān)庫(kù) | 抑制劑庫(kù) | 經(jīng)典已知活性庫(kù) | 已知活性化合物庫(kù) | 激酶抑制劑庫(kù) | HIF-1化合物庫(kù) | 癌細(xì)胞分化化合物庫(kù) | 干細(xì)胞分化化合物庫(kù) | 抗肺癌化合物庫(kù) | TGF-β/Smad靶點(diǎn)化合物庫(kù) | 膜蛋白靶向化合物庫(kù) | 酪氨酸激酶分子庫(kù) | 神經(jīng)元分化化合物庫(kù) |