Home TGF-beta/Smad TGF-beta/Smad inhibitor LDN-212854 For research use only.

LDN-212854

Synonyms: BMP Inhibitor III

LDN-212854 (BMP Inhibitor III) is a potent and selective BMP receptor inhibitor with IC50 of 1.3 nM for ALK2, about 2-, 66-, 1641-, and 7135-fold selectivity over ALK1, ALK3, ALK4, and ALK5, respectively.

LDN-212854 Chemical Structure

LDN-212854 Chemical Structure

CAS No. 1432597-26-6

Purity & Quality Control

Batch: S714701 DMSO]81 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 100.0%
100.0

LDN-212854 Related Products

Signaling Pathway

TGF-beta/Smad Signaling Pathways

TGF-beta/Smad Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
mouse C2C12BRA cells Function assay 14 h Inhibition of BMP4 in mouse C2C12BRA cells after 14 hrs by luciferase reporter gene assay, IC50=0.117 μM 23639540
Click to View More Cell Line Experimental Data

Biological Activity

Description LDN-212854 (BMP Inhibitor III) is a potent and selective BMP receptor inhibitor with IC50 of 1.3 nM for ALK2, about 2-, 66-, 1641-, and 7135-fold selectivity over ALK1, ALK3, ALK4, and ALK5, respectively.
Targets
ALK2 [1]
(Cell-free assay)		 ALK1 [1]
(Cell-free assay)		 ALK3 [1]
(Cell-free assay)		 ALK4 [1]
(Cell-free assay)		 ALK5 [1]
(Cell-free assay)
1.3 nM 2.4 nM 85.8 nM 2133 nM 9276 nM
In vitro
In vitro In myofibroblast C2C12 cells, LDN-212854 exhibits greater selectivity for BMP6- versus BMP4-induced osteogenic differentiation. [1]
Experimental Result Images Methods Biomarkers Images PMID
Western blot pSMAD1/5/9 TGF-β1 / pSMAD2 / SMAD1 23547776
In Vivo
In vivo LDN-212854 (6 mg/kg, i.p.) effectively neutralize ALK2 signaling in vivo, and potently inhibits heterotopic ossification in an inducible transgenic mutant ALK2 mouse model of fibrodysplasia ossificans progressiva. [1]
Animal Research Animal Models Murine inducible transgenic ALK2Q207D model of heterotopic ossification.
Dosages 6 mg/kg, twice daily
Administration i.p.

Chemical Information & Solubility

Molecular Weight 406.48 Formula

C25 H22 N6
CAS No. 1432597-26-6 SDF Download LDN-212854 SDF
Smiles C1CN(CCN1)C2=CC=C(C=C2)C3=CN4C(=C(C=N4)C5=C6C=CC=NC6=CC=C5)N=C3
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 81 mg/mL ( (199.27 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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In vivo Formulation Calculator

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In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Frequently Asked Questions

Question 1:
Can you suggest me the formulation of LDN-212854 for use in vivo?

Answer:
There is an IP formula for S7147, which is "2% DMSO+35% PEG 300+2% Tween 80+ddH2O" concentration can up to 2mg/ml.

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