LDN-214117

Name: LDN-214117
Brand: Selleck Chemicals
SKU: S7627
Rating: 5 (2 reviews)

For research use only.

Catalog No.S7627

2 publications

CAS No. 1627503-67-6

LDN-214117 is a potent and selective BMP type I receptor kinase ALK2 inhibitor with IC50 of 24 nM.

Selleck's LDN-214117 has been cited by 2 publications

FASEB J, 2021, 35(3):e21263

PubMed: 33570811 ( click the link to review the publication )

Stem Cells Int, 2019, 2019:5026793

PubMed: 31885612 ( click the link to review the publication )

Purity & Quality Control

Choose Selective TGF-beta/Smad Inhibitors

Biological Activity

Description

LDN-214117 is a potent and selective BMP type I receptor kinase ALK2 inhibitor with IC50 of 24 nM.

Targets

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. LDN-214117 demonstrates selective inhibition of ALK2 and ALK1 in preference to ALK3 kinase activity. LDN-214117 exhibits relatively selective inhibition of BMP6 versus BMP2 or BMP4. In a cell-based assay, LDN-214117 exhibits a selective inhibition on BMP6 with IC50 of approximately 100 nM, and 164-fold selectivity for BMP6 versus TGF-β1. ^[1]

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	Formulation	Activity Description	PMID
HEK293T cells	NISyPXRHfW6ldHnvckBie3OjeR?=		MU[zNEBucW6\|		NX\5OXk5UW6qaXLpeIlwdiCxZjDBUGsyKCi3bnvuc5dvKG:{aXfpckkh\XiycnXzd4VlKGmwIFjFT\|I6O1RiY3XscJMh[W[2ZYKgN\|AhdWmwczDifUBtfWOrZnXyZZNmKHKncH;yeIVzKGenbnWgZZN{[XluIFnDOVA:OC5yMkeg{txO	NWCyTYlGOjVzMEG5NVE>
C2C12 cells	MXfGeY5kfGmxbjDhd5NigQ>?		MmHzN\|AhdWmwcx?=		MmLGTY5pcWKrdHnvckBw\iCETWC2MYlv\HWlZXSgRm1RKHKnY3XweI9zKHS7cHWgNUBCVEt{IHnuJI1wfXOnIFOyR\|EzKGOnbHzzJIFnfGW{IEOwJI1qdnNiYomgcJVkcW[ncnHz[UBz\XCxcoTldkBo\W6nIHHzd4F6NCCLQ{WwQVAvOSEQvF2=	Ml3VNlUyODF7MUG=

... Click to View More Cell Line Experimental Data

Protocol

Kinase Assay:^[1]

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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 inhibitor compounds, 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.

Cell Research:^[1]

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Cell lines: HepG2 hepatocarcinoma cells
Concentrations: 100 μM
Incubation Time: 24 h
Method: Cells are seeded at 25000 cells per well in 96-well plates and incubated for 2 h at 37℃ and 5% CO₂. Compounds of LDN-214117 or DMSO are diluted in DMEM and added at ﬁnal compound concentrations of 1, 10, and 100 μM. Cells are incubated for 4 and 24 h, after which the media is discarded. Cells are lysed by adding 30 μL of passive lysis buﬀer and shaken at RT for 15 min. Cell viability is determined by quantifying the ATP present in each well by adding 10 μL of Cell Titer Glo per well and measuring the light output by Spectramax L luminometer. Data is normalized to 100% viability for cells receiving only DMSO.
(Only for Reference)

References

[1] Mohedas AH, et al. J Med Chem. 2014, 57(19), 7900-7915.

Solubility (25°C)

In vitro	DMSO	83 mg/mL (197.84 mM)
	Ethanol	83 mg/mL (197.84 mM)
	Water	Insoluble
In vivo	Add solvents to the product individually and in order(Data is from Selleck tests instead of citations): 2% DMSO+30% PEG 300+2% Tween 80+ddH2O For best results, use promptly after mixing.	3mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information Download LDN-214117 SDF

Molecular Weight	419.52
Formula	C₂₅H₂₉N₃O₃
CAS No.	1627503-67-6
Storage	3 years-20°C powder 2 years-80°C in solvent
Synonyms	N/A
Smiles	CC1=C(C=C(C=N1)C2=CC=C(C=C2)N3CCNCC3)C4=CC(=C(C(=C4)OC)OC)OC

In vivo Formulation Calculator (Clear solution)

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

Dosage

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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

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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.

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.

Bio Calculators

Molarity Calculator

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This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

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The Serial Dilution Calculator Equation

Serial Dilutions
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Computed Result

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
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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

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

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LDN-214117