Art. -Nr.: HY-16712

LDN-214117

2 Cited Publications

Kundenbewertung

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) .

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Reinheit: 99.54%
CAS. Nr.: 1627503-67-6
Formel: C₂₅H₂₉N₃O₃
Molecular Weight:419.52

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

LDN-214117 Chemical Structure

CAS. Nr.: 1627503-67-6

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (2)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

ACVR1

24 nM (IC₅₀)

ALK1

27 nM (IC₅₀)

BMPR1A

1171 nM (IC₅₀)

ALK5

3000 nM (IC₅₀)

Alle TGF-β Receptor Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
C2C12	IC₅₀	100 nM Compound: 10, LDN-214117	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	[PMID: 25101911]
C2C12	IC₅₀	1022 nM Compound: 10, LDN-214117	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	[PMID: 25101911]
C2C12	IC₅₀	960 nM Compound: 10, LDN-214117	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	[PMID: 25101911]
HEK-293T	IC₅₀	1171 nM Compound: 10, LDN-214117	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	[PMID: 25101911]
HEK-293T	IC₅₀	27 nM Compound: 10, LDN-214117	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	[PMID: 25101911]
HEK-293T	IC₅₀	27 nM Compound: 10, LDN-214117	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	[PMID: 25101911]
HEK-293T	IC₅₀	16 μM Compound: 10, LDN-214117	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	[PMID: 25101911]
Sf9	IC₅₀	24 nM Compound: LDN-214117	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	[PMID: 32369358]

In Vitro

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.

Cell Viability Assay^[2]

Cell Line:

LCLC-103H cells
Concentration:

5 μM
Incubation Time:

24 h, 48 h, 72 h and 96 h
Result:

Decreased markedly with time, counting approximately 60% of the vehicle control level at the 96-h measurement point.

Western Blot Analysis^[2]

Cell Line:

LCLC-103H cells
Concentration:

5 μM
Incubation Time:

30 min, 3 h and 24 h
Result:

Diminished the increase of ID1 protein.

Apoptosis Analysis^[2]

Cell Line:

LCLC-103H cells
Concentration:

5 μM
Incubation Time:

24 h, 48 h, 72 h and 96 h
Result:

Induced considerable death of LCLC-103H cells.

RT-PCR^[2]

Cell Line:

LCLC-103H cells
Concentration:

5 μM
Incubation Time:

24 h, 48 h and 72 h
Result:

Induced distinct gene expression patterns for the two EMTTFs.

Cell Migration Assay ^[2]

Cell Line:

LCLC-103H cells
Concentration:

5 μM
Incubation Time:

0 h, 24 h and 48 h
Result:

Significantly hindered the migration of LCLC-103H cells into the wound area by Inhibiting of BMP signaling.

In Vivo

LDN-214117 (p.o., 25 mg/kg, daily, for 14 days) has well-tolerated in mice^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

NOD.SCID mice^[3]
Dosage:

25 mg/kg
Administration:

p.o., daily, for 14 days
Result:

Showed good-tolerated in mice.

Chemical Information

CAS. Nr. 1627503-67-6
Appearance Solid
Molecular Weight 419.52
Formel C₂₅H₂₉N₃O₃
Color Off-white to yellow
SMILES

CC(C(C1=CC(OC)=C(OC)C(OC)=C1)=C2)=NC=C2C3=CC=C(N4CCNCC4)C=C3
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (2)

All Flow CytometryCell Proliferation/Viability Assay

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Journal Impact Factor

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)

BMP-ACVR1 Axis is Critical for Efficacy of PRC2 Inhibitors in B-Cell Lymphoma. [Abstract]

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.

Lösungsmittel & Löslichkeit

In Vitro:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.3837 mL

11.9184 mL

23.8368 mL

5 mM

0.4767 mL

2.3837 mL

4.7674 mL

10 mM

0.2384 mL

1.1918 mL

2.3837 mL

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

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.

Protocol 2

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2 mg/mL (4.77 mM); Clear solution

This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (279 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

LDN-214117

2 Cited Publications

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LDN-214117

Kinase Inhibitor Library

TGF-beta/Smad Compound Library

Anti-Cancer Compound Library

CNS-Penetrant Compound Library

Reprogramming Compound Library

Orally Active Compound Library

Chemical Probe Library

Anti-Pancreatic Cancer Compound Library

Anti-Obesity Compound Library

Angiogenesis-Related Compound Library

Anti-Colorectal Cancer Compound Library

Anti-Prostate Cancer Compound Library

Anti-Pulmonary Fibrosis Compound Library

Osteogenesis Compound Library

Cancer Stem Cells Compound Library

Heterocyclic Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Cytokine Inhibitors Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Fibrosis Compound Library

Anti-Brain Cancer Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) LDN-214117

Alle TGF-β Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (2)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

LDN-214117

Kinase Inhibitor Library

TGF-beta/Smad Compound Library

Anti-Cancer Compound Library

CNS-Penetrant Compound Library

Reprogramming Compound Library

Orally Active Compound Library

Chemical Probe Library

Anti-Pancreatic Cancer Compound Library

Anti-Obesity Compound Library

Angiogenesis-Related Compound Library

Anti-Colorectal Cancer Compound Library

Anti-Prostate Cancer Compound Library

Anti-Pulmonary Fibrosis Compound Library

Osteogenesis Compound Library

Cancer Stem Cells Compound Library

Heterocyclic Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Cytokine Inhibitors Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Fibrosis Compound Library

Anti-Brain Cancer Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) LDN-214117

Alle TGF-β Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (2)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

LDN-214117 Related Classifications

Art. -Nr.: HY-16712