LDN-214117
Based on 2 publication(s) in Google Scholar
LDN-214117 is an orally active ALK2 inhibitor with well-tolerated and good brain penetration. LDN-214117 has a high selectivity and low cytotoxicity for ALK2 with an IC50 value of 24 nM. LDN-214117 also is a specific bone morphogenetic proteins (BMPs) signaling inhibitor and has relatively selective inhibition for BMP6 with an IC50 value of 100 nM. LDN-214117 can be used for the research of fibrodysplasia ossificans progressiva (FOP), diffuse intrinsic pontine glioma (DIPG) .
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.54%
- CAS 番号: 1627503-67-6
- 分子式: C25H29N3O3
- 分子量:419.52
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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MedChemExpress（MCE）の使用を引用している文献 LDN-214117
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Flow Cytometry
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Cell Proliferation/Viability Assay
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Cell Proliferation/Viability Assay
生物活性
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ACVR1 24 nM (IC50) |
ALK1 27 nM (IC50) |
BMPR1A 1171 nM (IC50) |
ALK5 3000 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| C2C12 | IC50 |
100 nM
Compound: 10, LDN-214117
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Inhibition of BMP6-induced BMP receptor type 1 ALK2 in mouse C2C12 cells after 30 mins by luciferase reporter gene assay
Inhibition of BMP6-induced BMP receptor type 1 ALK2 in mouse C2C12 cells after 30 mins by luciferase reporter gene assay
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[PMID: 25101911] |
| C2C12 | IC50 |
1022 nM
Compound: 10, LDN-214117
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Inhibition of BMP4-induced BMP receptor in mouse C2C12 cells after 30 mins by luciferase reporter gene assay
Inhibition of BMP4-induced BMP receptor in mouse C2C12 cells after 30 mins by luciferase reporter gene assay
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[PMID: 25101911] |
| C2C12 | IC50 |
960 nM
Compound: 10, LDN-214117
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Inhibition of BMP2-induced BMP receptor type 1 ALK2 in mouse C2C12 cells after 30 mins by luciferase reporter gene assay
Inhibition of BMP2-induced BMP receptor type 1 ALK2 in mouse C2C12 cells after 30 mins by luciferase reporter gene assay
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[PMID: 25101911] |
| HEK-293T | IC50 |
1171 nM
Compound: 10, LDN-214117
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Inhibition of ALK3 (unknown origin) expressed in HEK293T cells after 30 mins by luciferase reporter gene assay
Inhibition of ALK3 (unknown origin) expressed in HEK293T cells after 30 mins by luciferase reporter gene assay
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[PMID: 25101911] |
| HEK-293T | IC50 |
27 nM
Compound: 10, LDN-214117
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Inhibition of ALK1 (unknown origin) expressed in HEK293T cells after 30 mins by luciferase reporter gene assay
Inhibition of ALK1 (unknown origin) expressed in HEK293T cells after 30 mins by luciferase reporter gene assay
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[PMID: 25101911] |
| HEK-293T | IC50 |
27 nM
Compound: 10, LDN-214117
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Inhibition of ALK2 (unknown origin) expressed in HEK293T cells after 30 mins by luciferase reporter gene assay
Inhibition of ALK2 (unknown origin) expressed in HEK293T cells after 30 mins by luciferase reporter gene assay
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[PMID: 25101911] |
| HEK-293T | IC50 |
16 μM
Compound: 10, LDN-214117
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Inhibition of TGFbeta1-induced TGFbeta type 1 ALK5 in HEK293T cells after 30 mins by luciferase reporter gene assay
Inhibition of TGFbeta1-induced TGFbeta type 1 ALK5 in HEK293T cells after 30 mins by luciferase reporter gene assay
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[PMID: 25101911] |
| Sf9 | IC50 |
24 nM
Compound: LDN-214117
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Inhibition of human N-terminal His-tagged TEV protease site linked ALK2 Q207D mutant (201 to 499 residues) expressed in baculovirus infected Sf9 insect cells
Inhibition of human N-terminal His-tagged TEV protease site linked ALK2 Q207D mutant (201 to 499 residues) expressed in baculovirus infected Sf9 insect cells
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[PMID: 32369358] |
LDN-214117 has high inhibition and selectivity for ALK2 kinase proteins with an IC50 value of 24 nM[1].
LDN-214117 has kinase activity for ALK1, ALK3 and ALK5 with IC50 values of 27 nM, 1,171 nM and 3,000 nM, respectively[1].
LDN-214117 exhibits relatively selective inhibition for BMP6, BMP2 and BMP4 with IC50 values of 100 nM, 1,022 nM and 960 nM, respectively[1].
LDN-214117 has inhibition of TGF-β1-induced transcriptional activity with an IC50 values of 16,000 nM[1].
LDN-214117 (5 μM, 30 min, 3 h and 24 h) has time-dependent effect activity on gene regulation level and/ or a BMP signaling pathway other than SMAD-dependent that is responsible for ID1 targeting[2].
LDN-214117 (5 μM, 24-120 h) reduces viability, proliferation and causes apoptosis of lung carcinoma cells LCLC-103H[2].
LDN-214117 (5 μM, 0-48 h) suppresses wound healing and chemotactic potential of LCLC-103H cells[2].
LDN-214117 (5 μM, 48 h) hinders growth of multicellular LCLC-103H spheroids[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:LCLC-103H cells
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Concentration:5 μM
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Incubation Time:24 h, 48 h, 72 h and 96 h
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Result:Decreased markedly with time, counting approximately 60% of the vehicle control level at the 96-h measurement point.
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Cell Line:LCLC-103H cells
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Concentration:5 μM
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Incubation Time:30 min, 3 h and 24 h
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Result:Diminished the increase of ID1 protein.
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Cell Line:LCLC-103H cells
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Concentration:5 μM
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Incubation Time:24 h, 48 h, 72 h and 96 h
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Result:Induced considerable death of LCLC-103H cells.
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Cell Line:LCLC-103H cells
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Concentration:5 μM
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Incubation Time:24 h, 48 h and 72 h
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Result:Induced distinct gene expression patterns for the two EMTTFs.
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Cell Line:LCLC-103H cells
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Concentration:5 μM
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Incubation Time:0 h, 24 h and 48 h
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Result:Significantly hindered the migration of LCLC-103H cells into the wound area by Inhibiting of BMP signaling.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NOD.SCID mice[3]
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Dosage:25 mg/kg
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Administration:p.o., daily, for 14 days
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Result:Showed good-tolerated in mice.
化学情報
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CAS 番号 1627503-67-6
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性状 Solid
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分子量 419.52
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分子式 C25H29N3O3
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Color Off-white to yellow
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SMILES
CC(C(C1=CC(OC)=C(OC)C(OC)=C1)=C2)=NC=C2C3=CC=C(N4CCNCC4)C=C3
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (2)
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Journal Impact Factor
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Most Recent
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Nat Commun
Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. [Abstract]2026 Feb 12;17(1):1214. PMID: 41680175 -
Adv Sci (Weinh)
2024 Mar;11(12):e2306499. PMID: 38229201
LDN-214117 purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2024 Mar;11(12):e2306499. [Abstract]
Cell apoptosis in WSU-DLCL2 cells treated with LDN-214117 (0.1-1 µM) and/or MAK683 (5 µM) for 9 days, determined by sub G1-content from PI staining and FACS (mean ± s.d., n = 4). LDN-214 antagonized the apoptosis-inducing effects of MAK683.
LDN-214117 purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2024 Mar;11(12):e2306499. [Abstract]
Proliferation of SU-DHL-4 cells treated with LDN-214117 (0.1-1 µM; 18 days) and/or MAK683 (1.2 µM). Viable cells were counted every 3 days (mean ± s.d., n = 2).
LDN-214117 purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2024 Mar;11(12):e2306499. [Abstract]
Cell cycle analysis of SU-DHL-4 cells treated with MAK683 (5 μM) and/or LDN-214117 (0.1 μM-1 μM) at the indicated concentrations for 5 days (mean ± s.d., n=4). LDN‐214117 antagonized the cell cycle arrest inducing effects of MAK683.
溶剤 & 溶解度
DMSO : 20 mg/mL (47.67 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2 mg/mL (4.77 mM); Clear solution
This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2 mg/mL (4.77 mM); Clear solution
This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
純度とドキュメンテーション
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データシート (279 KB)
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SDS (393 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Agustin H Mohedas, et al. Structure-activity relationship of 3,5-diaryl-2-aminopyridine ALK2 inhibitors reveals unaltered binding affinity for fibrodysplasia ossificans progressiva causing mutants. J Med Chem. 2014 Oct 9;57(19):7900-15. [Content Brief]
[2]. Jelena Mihajlović, et al. Inhibition of bone morphogenetic protein signaling reduces viability, growth and migratory potential of non-small cell lung carcinoma cells. J Cancer Res Clin Oncol. 2019 Nov;145(11):2675-2687. [Content Brief]
[3]. Diana Carvalho, et al. ALK2 inhibitors display beneficial effects in preclinical models of ACVR1 mutant diffuse intrinsic pontine glioma. Commun Biol. 2019 May 9;2:156. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| 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 | |
| 15 mM | 0.1589 mL | 0.7946 mL | 1.5891 mL | 3.9728 mL | |
| 20 mM | 0.1192 mL | 0.5959 mL | 1.1918 mL | 2.9796 mL | |
| 25 mM | 0.0953 mL | 0.4767 mL | 0.9535 mL | 2.3837 mL | |
| 30 mM | 0.0795 mL | 0.3973 mL | 0.7946 mL | 1.9864 mL | |
| 40 mM | 0.0596 mL | 0.2980 mL | 0.5959 mL | 1.4898 mL |
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