2. TGF-beta/Smad
  3. TGF-β Receptor
  4. LDN-214117

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) [2]

For research use only. We do not sell to patients.

LDN-214117 Chemical Structure

LDN-214117 Chemical Structure

CAS No. : 1627503-67-6

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 73 In-stock
Solution
10 mM * 1 mL in DMSO USD 73 In-stock
Solid
1 mg USD 26 In-stock
5 mg USD 66 In-stock
10 mg USD 121 In-stock
25 mg USD 242 In-stock
50 mg USD 418 In-stock
100 mg USD 649 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

LDN-214117 Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE LDN-214117

View All TGF-β Receptor Isoform Specific Products:

View All Isoforms
ALK1 ALK2 ALK3 ALK4 ALK5 ALK6 ALK7 TGFβR2 ACVR2A ACVR2B

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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) [1][2]

IC50 & Target

IC50: 24 nM (ALK2); 27 nM (ALK1); 1,171 nM (ALK3); 3,000 nM (ALK5); 1,022 nM (BMP6); 27 nM (BMP2); 960 nM (BMP4); 16,000 nM (TGF-β1)[1]
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.

LDN-214117 Related Antibodies

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.
Molecular Weight

419.52

Formula

C25H29N3O3
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3837 mL 11.9184 mL 23.8368 mL
5 mM 0.4767 mL 2.3837 mL 4.7674 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
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Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

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V2

In Vivo:

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.

  • 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.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • 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.

    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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

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g

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(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Purity & Documentation

Purity: 99.92%

COA (247 KB) LCMS (94 KB)

Handling Instructions (2659 KB)
References

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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LDN-214117 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

LDN-2141171627503-67-6LDN214117LDN 214117TGF-β ReceptorTransforming growth factor beta receptorsoralbone morphogenetic proteins (BMPs)type I receptor kinasesALK1ALK2ALK3ALK5BMP6BMP2BMP4transforming growth factor-beta (TGF-β)fibrodysplasia ossificans progressiva (FOP)diffuse intrinsic pontine glioma (DIPG)Inhibitorinhibitorinhibit

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