2. TGF-beta/Smad
  3. TGF-β Receptor
  4. LDN-212854

LDN-212854 is a bone morphogenetic protein (BMP) inhibitor that potently inhibits ALK2 (IC50: 1.3 nM). LDN-212854 also inhibits ALK1 (IC50: 2.40 nM). LDN-212854 can be used in the research of fibrodysplasia ossificans progressive and cancers, such as hepatocellular carcinoma (HCC).

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

LDN-212854 Chemical Structure

LDN-212854 Chemical Structure

CAS No. : 1432597-26-6

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10 mM * 1 mL in DMSO
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Customer Review

Based on 1 publication(s) in Google Scholar

LDN-212854 Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE LDN-212854

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-212854 is a bone morphogenetic protein (BMP) inhibitor that potently inhibits ALK2 (IC50: 1.3 nM). LDN-212854 also inhibits ALK1 (IC50: 2.40 nM). LDN-212854 can be used in the research of fibrodysplasia ossificans progressive and cancers, such as hepatocellular carcinoma (HCC)[1][2].

IC50 & Target[1]

ACVR1

1.3 nM (IC50)

ALK1

2.4 nM (IC50)

BMPR1A

85.8 nM (IC50)

ALK4

2133 nM (IC50)

ALK5

9276 nM (IC50)

In Vitro

LDN-212854 (0-3.815 μM) blocks the phosphorylation of SMAD1/5/8 induced by BMP7 in BMPR2−/− cells[1].
LDN-212854 (2.5 μM, 5 days ) inhibits cell proliferation in Huh7 and MT cells[2].
LDN-212854 (0.5 μM, 48 h ) suppresses ID1 and EpCAM expression in Huh7 and MT cells[2].

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

LDN-212854 Related Antibodies

Western Blot Analysis[1]

Cell Line: BMPR2-deficient pulmonary vascular smooth muscle cells
Concentration: 0, 1, 3, 6, 16, 39, 98, 244, 610, 1530, 3815 nM
Incubation Time:
Result: Inhibited the phosphorylation of SMAD1/5/8 induced by BMP7 with an IC50 value of 37 nM.
In Vivo

LDN-212854 (intraperitoneal injection, 6 mg/kg, twice daily for 4 weeks) potently inhibits heterotopic ossification in an inducible transgenic mutant ALK2 mouse model of fibrodysplasia ossificans progressiva[1].
LDN-212854 (intraperitoneal injection, 6 mg/kg, twice daily for 10-14 days) suppresses HCC tumor progression through repression of ID1 in HCC xenografts model[2].

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

Animal Model: Murine inducible transgenic ALK2Q207D model of heterotopic ossification[1]
Dosage: 6 mg/kg
Administration: Intraperitoneal injection , twice daily for 4 weeks
Result: Prevented the formation of heterotopic bone and preserved limb range of motion with minimal or no impairment in the majority of mice.
Animal Model: HCC xenografts (Huh7 or MT cell)[1]
Dosage: 6 mg/kg
Administration: Intraperitoneal injection, twice daily for 10-14 days.
Result: Inhibited tumor growth and showed less spheroid/colony formation ability than PBS-treated tumor cells.
Molecular Weight

406.48

Formula

C25H22N6
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

C12=C(C3=C4N=CC(C5=CC=C(N6CCNCC6)C=C5)=CN4N=C3)C=CC=C1N=CC=C2
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 : ≥ 30 mg/mL (73.80 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4601 mL 12.3007 mL 24.6015 mL
5 mM 0.4920 mL 2.4601 mL 4.9203 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

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

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: 2.5 mg/mL (6.15 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: 2.5 mg/mL (6.15 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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

Animal weight
(per animal)

g

Dosing volume
(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: 99.70%

SDS (420 KB)

COA (254 KB) LCMS (266 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 2.4601 mL 12.3007 mL 24.6015 mL 61.5036 mL
5 mM 0.4920 mL 2.4601 mL 4.9203 mL 12.3007 mL
10 mM 0.2460 mL 1.2301 mL 2.4601 mL 6.1504 mL
15 mM 0.1640 mL 0.8200 mL 1.6401 mL 4.1002 mL
20 mM 0.1230 mL 0.6150 mL 1.2301 mL 3.0752 mL
25 mM 0.0984 mL 0.4920 mL 0.9841 mL 2.4601 mL
30 mM 0.0820 mL 0.4100 mL 0.8200 mL 2.0501 mL
40 mM 0.0615 mL 0.3075 mL 0.6150 mL 1.5376 mL
50 mM 0.0492 mL 0.2460 mL 0.4920 mL 1.2301 mL
60 mM 0.0410 mL 0.2050 mL 0.4100 mL 1.0251 mL
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LDN-212854 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-2128541432597-26-6LDN212854LDN 212854TGF-β ReceptorTransforming growth factor beta receptorsBMPFOP modelBMPR2 cellheterotopic ossificationHCCHuh7MT cellEpCAMBMP9-ID1 signalingInhibitorinhibitorinhibit

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