Home TGF-beta/Smad TGF-beta/Smad inhibitor LDN-214117

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LDN-214117 TGF-beta/Smad inhibitor

Cat.No.S7627

LDN-214117 is a potent and selective BMP type I receptor kinase ALK2 inhibitor with IC50 of 24 nM.
LDN-214117 TGF-beta/Smad inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 419.52

Jump to Mechanism of Action Cell Culture & Working Concentration Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Cell Culture, Treatment & Working Concentration

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HEK293T cells Function assay 30 mins Inhibition of ALK1 (unknown origin) expressed in HEK293T cells after 30 mins by luciferase reporter gene assay, IC50=0.027 μM
C2C12 cells Function assay 30 mins Inhibition of BMP6-induced BMP receptor type 1 ALK2 in mouse C2C12 cells after 30 mins by luciferase reporter gene assay, IC50=0.1 μM
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Chemical Information, Storage & Stability

Molecular Weight 419.52 Formula

C25H29N3O3

 Storage (From the date of receipt)
CAS No. 1627503-67-6 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles CC1=C(C=C(C=N1)C2=CC=C(C=C2)N3CCNCC3)C4=CC(=C(C(=C4)OC)OC)OC

Solubility

In vitro
Batch:

DMSO : 83 mg/mL (197.84 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 83 mg/mL

Water : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
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In vivo Formulation Calculator (Clear solution)

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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.

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Mechanism of Action

Targets/IC50/Ki
ALK2 [1]
(Cell-free assay)
24 nM
In vitro
The kinase most highly inhibited by LDN-214117 is ALK2 (IC50, 24 nM), followed by TNIK, RIPK2, and ABL1. This compound demonstrates selective inhibition of ALK2 and ALK1 in preference to ALK3 kinase activity. It exhibits relatively selective inhibition of BMP6 versus BMP2 or BMP4. In a cell-based assay, this chemical exhibits a selective inhibition on BMP6 with IC50 of approximately 100 nM, and 164-fold selectivity for BMP6 versus TGF-β1. [1]
Kinase Assay
ALK2 kinase assay
Purified recombinant ALK2 proteins, ATP, ATP[γ-32P], and dephosphorylated casein at final concentrations of 2.5 nM, 6 μM, 0.05 μCi/μL , and 0.5 mg/mL, respectively, are aliquoted in kinase buffer containing 0.2% BSA supplemented with 10 mM MnCl2 into 96-microwell plates, in combination with inhibitor compounds diluted at varying concentrations (0.01 nM to 100 μM). Positive control samples lacking this compound, and negative controls lacking recombinant kinase, are also measured. The mixture is reacted at RT for 45 min, quenched with a final concentration of 2% phosphoric acid. The reaction mixture is transferred to 96-well P81 phosphocellulose filter plates and bound for 5 min. The plates are washed 20 times with 150 μL of 1% phosphoric acid solution per well by vacuum manifold. Plates are dried at RT for 1 h, sealed, and assayed with Microscint 20 scintillation fluid using a Spectramax L luminometer. Data is normalized to positive controls at 100% enzyme activity, with negative controls being subtracted as background.
References

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