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Formula | C25H29N3O3 |
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Molecular Weight | 419.52 | CAS No. | 1627503-67-6 | ||||
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) |
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* <1 mg/ml means slightly soluble or insoluble. * 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. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
Description | LDN-214117 is a potent and selective BMP type I receptor kinase ALK2 inhibitor with IC50 of 24 nM. | ||
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Targets |
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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] |
Kinase Assay:[1] |
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Cell Assay:[1] |
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Live-Cell Invasive Phenotyping Uncovers ALK2 as a Therapeutic Target in LKB1-Mutant Lung Cancer [ Cancer Res, 2024, 10.1158/0008-5472.CAN-23-2631] | PubMed: 39207369 |
Live-cell invasive phenotyping uncovers the ALK2/BMP6 iron homeostasis pathway as a therapeutic vulnerability in LKB1-mutant lung cancer [ bioRxiv, 2023, 2023.06.14.544941] | PubMed: 37398244 |
Fluid shear stress generates a unique signaling response by activating multiple TGFβ family type I receptors in osteocytes [ FASEB J, 2021, 35(3):e21263] | PubMed: 33570811 |
Dual Inhibition of BMP and WNT Signals Promotes Pancreatic Differentiation from Human Pluripotent Stem Cells. [ Stem Cells Int, 2019, 2019:5026793] | PubMed: 31885612 |
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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.
NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.