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LDN-214117 is a highly BMP selective compound, significantly biased toward ALK2 and its cognate ligands including BMP6 and also demonstrates a high degree of kinome selectivity and low cytotoxicity. LDN-214117 may be useful as highly selective probes of BMP-mediated cellular physiology that may provide a useful complement to the dorsomorphin class of compounds. Furthermore, this class of BMP inhibitors offers a structurally distinct template for the development of therapeutics for the treatment of BMP signaling-mediated diseases such as FOP.
| Cell Experiment | |
|---|---|
| Cell lines | HepG2 hepatocarcinoma cells |
| Preparation method | Seeding cells at 25000 cells per well in 96-well plates and incubatng for 2 h at 37℃ and 5% CO2. Diluting compounds of LDN-214117 or DMSO are in DMEM and adding at final compound concentrations of 1, 10, and 100 μM.Incubating cells 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. |
| Concentrations | 100 μM |
| Incubation time | 24 h |
| Animal Experiment | |
|---|---|
| Animal models | |
| Formulation | |
| Dosages | |
| Administration | |
| Molecular Weight | 419.52 |
| Formula | C25H29N3O3 |
| CAS Number | 1627503-67-6 |
| Solubility (25°C) | DMSO 10 mM |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related ALK Products |
|---|
| NVL-655 TFA
NVL-655 (ALK-IN-27) TFA is a novel, brain-permeable, selective ALK inhibitor with antitumor activity. For Ba/F3 CLIP1-LTK cells, NVL-655 (ALK-IN-27) TFA has an IC50 of 2.7 nM. It can be used in studies related to ALK-positive non-small cell lung cancer (NSCLC). |
| NVL-655
NVL-655 (ALK-IN-27) is a novel, brain-permeable, selective ALK inhibitor with antitumor activity. For Ba/F3 CLIP1-LTK cells, NVL-655 has an IC50 of 2.7 nM. NVL-655 (ALK-IN-27) can be used in studies related to ALK-positive non-small cell lung cancer (NSCLC). |
| APG-2449
APG-2449 is an orally active, potent ALK/ROS1/FAK inhibitor with anti-tumor activity in a mouse model of non-small cell lung cancer (NSCLC). |
| ALK2-IN-5
ALK2-IN-5, pyrazolopyrimidine compound, is an ALK2 inhibitor. |
| J-1048
J-1048 is an activin receptor-like kinase 5 (ALK5) inhibitor. |
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