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> LDN-214117 [1627503-67-6]

LDN-214117 [1627503-67-6]

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Referência HY-16712-5mg

Tamanho : 5mg

Marca : MedChemExpress

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Description

LDN-214117 is an orally active ALK2 inhibitor with well-tolerated and good brain penetration. LDN-214117 has a high selectivity and low cytotoxicity for ALK2 with an IC50 value of 24 nM. LDN-214117 also is a specific bone morphogenetic proteins (BMPs) signaling inhibitor and has relatively selective inhibition for BMP6 with an IC50 value of 100 nM. LDN-214117 can be used for the research of fibrodysplasia ossificans progressiva (FOP), diffuse intrinsic pontine glioma (DIPG) [1][2].

IC50 & Target[1]

ACVR1

24 nM (IC50)

ALK1

27 nM (IC50)

BMPR1A

1171 nM (IC50)

ALK5

3000 nM (IC50)

Cellular Effect
Cell Line Type Value Description References
C2C12 IC50
100 nM
Compound: 10, LDN-214117
Inhibition of BMP6-induced BMP receptor type 1 ALK2 in mouse C2C12 cells after 30 mins by luciferase reporter gene assay
Inhibition of BMP6-induced BMP receptor type 1 ALK2 in mouse C2C12 cells after 30 mins by luciferase reporter gene assay
[PMID: 25101911]
C2C12 IC50
1022 nM
Compound: 10, LDN-214117
Inhibition of BMP4-induced BMP receptor in mouse C2C12 cells after 30 mins by luciferase reporter gene assay
Inhibition of BMP4-induced BMP receptor in mouse C2C12 cells after 30 mins by luciferase reporter gene assay
[PMID: 25101911]
C2C12 IC50
960 nM
Compound: 10, LDN-214117
Inhibition of BMP2-induced BMP receptor type 1 ALK2 in mouse C2C12 cells after 30 mins by luciferase reporter gene assay
Inhibition of BMP2-induced BMP receptor type 1 ALK2 in mouse C2C12 cells after 30 mins by luciferase reporter gene assay
[PMID: 25101911]
HEK-293T IC50
1171 nM
Compound: 10, LDN-214117
Inhibition of ALK3 (unknown origin) expressed in HEK293T cells after 30 mins by luciferase reporter gene assay
Inhibition of ALK3 (unknown origin) expressed in HEK293T cells after 30 mins by luciferase reporter gene assay
[PMID: 25101911]
HEK-293T IC50
16 μM
Compound: 10, LDN-214117
Inhibition of TGFbeta1-induced TGFbeta type 1 ALK5 in HEK293T cells after 30 mins by luciferase reporter gene assay
Inhibition of TGFbeta1-induced TGFbeta type 1 ALK5 in HEK293T cells after 30 mins by luciferase reporter gene assay
[PMID: 25101911]
HEK-293T IC50
16000 nM
Compound: 10, LDN-214117
Inhibition of TGFbeta1-induced TGFbeta type 1 ALK5 in HEK293T cells after 30 mins by luciferase reporter gene assay
Inhibition of TGFbeta1-induced TGFbeta type 1 ALK5 in HEK293T cells after 30 mins by luciferase reporter gene assay
[PMID: 25101911]
HEK-293T IC50
27 nM
Compound: 10, LDN-214117
Inhibition of ALK1 (unknown origin) expressed in HEK293T cells after 30 mins by luciferase reporter gene assay
Inhibition of ALK1 (unknown origin) expressed in HEK293T cells after 30 mins by luciferase reporter gene assay
[PMID: 25101911]
HEK-293T IC50
27 nM
Compound: 10, LDN-214117
Inhibition of ALK2 (unknown origin) expressed in HEK293T cells after 30 mins by luciferase reporter gene assay
Inhibition of ALK2 (unknown origin) expressed in HEK293T cells after 30 mins by luciferase reporter gene assay
[PMID: 25101911]
Sf9 IC50
24 nM
Compound: LDN-214117
Inhibition of human N-terminal His-tagged TEV protease site linked ALK2 Q207D mutant (201 to 499 residues) expressed in baculovirus infected Sf9 insect cells
Inhibition of human N-terminal His-tagged TEV protease site linked ALK2 Q207D mutant (201 to 499 residues) expressed in baculovirus infected Sf9 insect cells
[PMID: 32369358]
In Vitro

LDN-214117 has high inhibition and selectivity for ALK2 kinase proteins with an IC50 value of 24 nM[1].
LDN-214117 has kinase activity for ALK1, ALK3 and ALK5 with IC50 values of 27 nM, 1,171 nM and 3,000 nM, respectively[1].
LDN-214117 exhibits relatively selective inhibition for BMP6, BMP2 and BMP4 with IC50 values of 100 nM, 1,022 nM and 960 nM, respectively[1].
LDN-214117 has inhibition of TGF-β1-induced transcriptional activity with an IC50 values of 16,000 nM[1].
LDN-214117 (5 μM, 30 min, 3 h and 24 h) has time-dependent effect activity on gene regulation level and/ or a BMP signaling pathway other than SMAD-dependent that is responsible for ID1 targeting[2].
LDN-214117 (5 μM, 24-120 h) reduces viability, proliferation and causes apoptosis of lung carcinoma cells LCLC-103H[2].
LDN-214117 (5 μM, 0-48 h) suppresses wound healing and chemotactic potential of LCLC-103H cells[2].
LDN-214117 (5 μM, 48 h) hinders growth of multicellular LCLC-103H spheroids[2].

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

LDN-214117 Related Antibodies

Cell Viability Assay[2]

Cell Line: LCLC-103H cells
Concentration: 5 μM
Incubation Time: 24 h, 48 h, 72 h and 96 h
Result: Decreased markedly with time, counting approximately 60% of the vehicle control level at the 96-h measurement point.

Western Blot Analysis[2]

Cell Line: LCLC-103H cells
Concentration: 5 μM
Incubation Time: 30 min, 3 h and 24 h
Result: Diminished the increase of ID1 protein.

Apoptosis Analysis[2]

Cell Line: LCLC-103H cells
Concentration: 5 μM
Incubation Time: 24 h, 48 h, 72 h and 96 h
Result: Induced considerable death of LCLC-103H cells.

RT-PCR[2]

Cell Line: LCLC-103H cells
Concentration: 5 μM
Incubation Time: 24 h, 48 h and 72 h
Result: Induced distinct gene expression patterns for the two EMTTFs.

Cell Migration Assay [2]

Cell Line: LCLC-103H cells
Concentration: 5 μM
Incubation Time: 0 h, 24 h and 48 h
Result: Significantly hindered the migration of LCLC-103H cells into the wound area by Inhibiting of BMP signaling.
In Vivo

LDN-214117 (p.o., 25 mg/kg, daily, for 14 days) has well-tolerated in mice[3].

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

Animal Model: NOD.SCID mice[3]
Dosage: 25 mg/kg
Administration: p.o., daily, for 14 days
Result: Showed good-tolerated in mice.
Masse moléculaire

419.52

Formule

C25H29N3O3
CAS No.
Appearance

Solid

Color

Off-white to yellow

SMILES

CC(C(C1=CC(OC)=C(OC)C(OC)=C1)=C2)=NC=C2C3=CC=C(N4CCNCC4)C=C3
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvant et solubilité
In Vitro: 

DMSO : 20 mg/mL (47.67 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3837 mL 11.9184 mL 23.8368 mL
5 mM 0.4767 mL 2.3837 mL 4.7674 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.

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 mg/mL (4.77 mM); Clear solution

    This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 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 mg/mL (4.77 mM); Clear solution

    This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 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.
Pureté et documentation
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