LDN-214117

製品コードS7627 バッチS762701

印刷

化学情報

Synonyms

N/A

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₂₅H₂₉N₃O₃

分子量

419.52

CAS No.

1627503-67-6

Solubility (25°C)*

体外

DMSO

83 mg/mL (197.84 mM)

Ethanol

83 mg/mL (197.84 mM)

Water

Insoluble

体内（毎回新しく調製した物を用意してください）

Clear solution

2%DMSO 1 30%PEG300 2 2%Tween80 3 66%ddH2O

3.0mg/ml

Taking the 1 mL working solution as an example, add 20 μL of 150 mg/ml clarified DMSO stock solution to 300 μL of PEG300, mix evenly to clarify it; add 20 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 660 μL of ddH2O to adjust the volume to 1 mL. 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-214117 is a potent and selective BMP type I receptor kinase ALK2 inhibitor with IC50 of 24 nM.
in vitro	The kinase most highly inhibited by LDN-214117 is ALK2 (IC50, 24 nM), followed by TNIK, RIPK2, and ABL1. LDN-214117 demonstrates selective inhibition of ALK2 and ALK1 in preference to ALK3 kinase activity. LDN-214117 exhibits relatively selective inhibition of BMP6 versus BMP2 or BMP4. In a cell-based assay, LDN-214117 exhibits a selective inhibition on BMP6 with IC50 of approximately 100 nM, and 164-fold selectivity for BMP6 versus TGF-β1. ^[1]

製品説明

LDN-214117 is a potent and selective BMP type I receptor kinase ALK2 inhibitor with IC50 of 24 nM.

in vitro

The kinase most highly inhibited by LDN-214117 is ALK2 (IC50, 24 nM), followed by TNIK, RIPK2, and ABL1. LDN-214117 demonstrates selective inhibition of ALK2 and ALK1 in preference to ALK3 kinase activity. LDN-214117 exhibits relatively selective inhibition of BMP6 versus BMP2 or BMP4. In a cell-based assay, LDN-214117 exhibits a selective inhibition on BMP6 with IC50 of approximately 100 nM, and 164-fold selectivity for BMP6 versus TGF-β1. ^[1]

プロトコル(参考用のみ)

キナーゼアッセイ	ALK2 kinase assay
キナーゼアッセイ	Puriﬁed recombinant ALK2 proteins, ATP, ATP[γ-³²P], and dephosphorylated casein at ﬁnal concentrations of 2.5 nM, 6 μM, 0.05 μCi/μL , and 0.5 mg/mL, respectively, are aliquoted in kinase buﬀer 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 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 are dried at RT for 1 h, sealed, and assayed with Microscint 20 scintillation ﬂuid using a Spectramax L luminometer. Data is normalized to positive controls at 100% enzyme activity, with negative controls being subtracted as background.
細胞アッセイ	細胞株	HepG2 hepatocarcinoma cells
	濃度	100 μM
	反応時間	24 h
	実験の流れ	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 ﬁnal 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 buﬀer 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.

参考

[1] Mohedas AH, et al. J Med Chem. 2014, 57(19), 7900-7915.

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：

Live-cell invasive phenotyping uncovers the ALK2/BMP6 iron homeostasis pathway as a therapeutic vulnerability in LKB1-mutant lung cancer [ bioRxiv, 2023, 2023.06.14.544941]	PubMed: 37398244
Fluid shear stress generates a unique signaling response by activating multiple TGFβ family type I receptors in osteocytes [ FASEB J, 2021, 35(3):e21263]	PubMed: 33570811
Dual Inhibition of BMP and WNT Signals Promotes Pancreatic Differentiation from Human Pluripotent Stem Cells. [ Stem Cells Int, 2019, 2019:5026793]	PubMed: 31885612

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。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。