LDN-212854 TGF-beta/Smad inhibitor

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Quality Control

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

Cited in Nature Medicine for its top-tier quality
COA
NMR
HPLC
SDS
Datasheet

100.0

Related Targets	PKC ROCK Bcr-Abl
Other TGF-beta/Smad Inhibitors	SB431542 RepSox (E-616452) Vactosertib (TEW-7197) LDN-193189 A-83-01 LDN-193189 Dihydrochloride Galunisertib (LY2157299) SRI-011381 (C381) LY2109761 SIS3 Hydrochloride

Cell Culture, Treatment & Working Concentration

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

Chemical Information, Storage & Stability

Molecular Weight	406.48	Formula	C₂₅ H₂₂ N₆	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	1432597-26-6	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	BMP Inhibitor III			Smiles	C1CN(CCN1)C2=CC=C(C=C2)C3=CN4C(=C(C=N4)C5=C6C=CC=NC6=CC=C5)N=C3

Solubility

In vitro
Batch:

DMSO : 81 mg/mL (199.27 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.500mg/ml (1.23mM)	Taking the 1 mL working solution as an example, add 50 μL of 10 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.500mg/ml (1.23mM)	Taking the 1 mL working solution as an example, add 50 μL of 10 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

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.

Mechanism of Action

Targets/IC₅₀/Ki	ALK2 (Cell-free assay) 1.3 nM ALK1 (Cell-free assay) 2.4 nM ALK3 (Cell-free assay) 85.8 nM ALK4 (Cell-free assay) 2133 nM ALK5 (Cell-free assay) 9276 nM
In vitro	In myofibroblast C2C12 cells, LDN-212854 exhibits greater selectivity for BMP6- versus BMP4-induced osteogenic differentiation.
In vivo	LDN-212854 (6 mg/kg, i.p.) effectively neutralises ALK2 signalling in vivo, and potently inhibits heterotopic ossification in an inducible transgenic mutant ALK2 mouse model of fibrodysplasia ossificans progressiva.
References	[1] https://pubmed.ncbi.nlm.nih.gov/23547776/

Applications

Methods	Biomarkers	Images	PMID
Western blot	pSMAD1/5/9 TGF-β1 / pSMAD2 / SMAD1		23547776

Tech Support

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

Frequently Asked Questions

Question 1:
Can you suggest me the formulation for it for use in vivo?

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

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Chemical Structure

Molecular Weight: 406.48