LDN-212854

製品コードS7147 バッチS714701

印刷

化学情報

Chemical Structure Synonyms BMP Inhibitor III Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C25 H22 N6
分子量 406.48 CAS No. 1432597-26-6
Solubility (25°C)* 体外 DMSO (warmed with 50ºC water bath) 81 mg/mL (199.27 mM)
Water Insoluble
Ethanol Insoluble
体内 （毎回新しく調製した物を用意してください）
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
0.5mg/ml Taking the 1 mL working solution as an example, add 50 μL of 10 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
Clear solution
5% DMSO 95% Corn oil
0.5mg/ml Taking the 1 mL working solution as an example, add 50 μL of 10 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 LDN-212854 (BMP Inhibitor III) is a potent and selective BMP receptor inhibitor with IC50 of 1.3 nM for ALK2, about 2-, 66-, 1641-, and 7135-fold selectivity over ALK1, ALK3, ALK4, and ALK5, respectively.
in vitro In myofibroblast C2C12 cells, LDN-212854 exhibits greater selectivity for BMP6- versus BMP4-induced osteogenic differentiation. [1]
in vivo LDN-212854 (6 mg/kg, i.p.) effectively neutralize ALK2 signaling in vivo, and potently inhibits heterotopic ossification in an inducible transgenic mutant ALK2 mouse model of fibrodysplasia ossificans progressiva. [1]

プロトコル(参考用のみ)

キナーゼアッセイ Kinase assay
Purified recombinant ALK1-5 and other kinase proteins, ATP, ATP [γ-32P] , and dephosphorylated casein at final concentrations of 2.5 nM, 6 μM, 0.05 μCi μL–1, and 0.5 mg/mL, respectively, are aliquoted in kinase buffer containing 0.2% bovine serum albumin supplemented with 10 mM MnCl2 into 96-well plates, in combination with inhibitor compounds diluted at varying concentrations in kinase buffer (0.01 nM to 10 μM) in triplicate. Positive control samples lacking inhibitor compounds and negative controls lacking recombinant kinase are also measured in triplicate. The mixture is reacted at RT for 45 min and quenched with a final concentration of 2% phosphoric acid. The reaction mixture is transferred to 96-well P81 phosphocellulose filter 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 were dried at RT for 1 h, sealed, and assayed with Microscint 20 scintillation fluid using a Spectramax L luminometer using the photon counting setting with an integration time of 1 s per well. Data is normalized to positive controls at 100% enzyme activity with negative controls being subtracted as background. GraphPad is used for graphing and regression analysis by sigmoidal dose-response with variable Hill coefficient.
動物実験 動物モデル Murine inducible transgenic ALK2Q207D model of heterotopic ossification.
投薬量 6 mg/kg, twice daily
投与方法 i.p.

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Transcriptional Profiling Supports the Notochordal Origin of Chordoma and Its Dependence on a TGFΒ1-TBXT Network [ Am J Pathol, 2023, S0002-9440(23)00047-0] PubMed: 36804377
Transcriptional Profiling Supports the Notochordal Origin of Chordoma and Its Dependence on a TGFB1-TBXT Network [ Am J Pathol, 2023, 193(5):532-547] PubMed: 36804377
BMP9-ID1 Signaling Activates HIF-1α and VEGFA Expression to Promote Tumor Angiogenesis in Hepatocellular Carcinoma [ Int J Mol Sci, 2022, 23(3)1475] PubMed: 35163396
Clonal hematopoiesis with JAK2V617F promotes pulmonary hypertension with ALK1 upregulation in lung neutrophils [ Nat Commun, 2021, 12(1):6177] PubMed: 34702814
BMP9-ID1 signaling promotes EpCAM-positive cancer stem cell properties in hepatocellular carcinoma [ Mol Oncol, 2021, 10.1002/1878-0261.12963] PubMed: 33834612
KR‑12‑a6 promotes the osteogenic differentiation of human bone marrow mesenchymal stem cells via BMP/SMAD signaling. [ Mol Med Rep, 2020, 21(1):61-68] PubMed: 31939626
ALK1 Loss Results in Vascular Hyperplasia in Mice and Humans Through PI3K Activation. [ Arterioscler Thromb Vasc Biol, 2018, 38(5):1216-1229] PubMed: 29449337

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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