LDN-214117

LDN-214117

Application

LDN-214117 has been used in structure-activity relationship (SAR) study to evaluate its potency on selective inhibition of activin receptor-like kinase-2 (ALK2) through the kinome-wide selectivity of (LDN-214117) via enzymatic kinase profiling.

Biochem/physiol Actions

LDN-214117 is a selective inhibitor of the bone morphogenetic protein (BMP) type I receptor kinases with high selectivity for BMP versus TGF-β signaling, and low cytotoxicity. LDN-214117 inhibited ALK2 most, with a biochemical IC50 of 24 nM, followed by TNIK, RIPK2, and ABL1. LDN-214117 has a cell-based IC50 for BMP6 of approximately 100 nM and 164-fold selectivity for BMP6 versus TGF-β1. Fibrodysplasia ossificans progressiva (FOP) is a debilitating and progressive heterotopic ossification disease caused by activating mutations of ACVR1 encoding the BMP type I receptor kinase ALK2. LDN-214117 had nearly identical binding affinity for wild-type ALK2 and each of the FOP-causing mutants tested.

Packaging

5, 25 mg in glass bottle

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Code Description Colour Quality Level InChI key InChI Manufacturer Solubility Form Assay Price Quantity
3574498 LDN-214117 white to beige 100 BHUXVRVMMYAXKN-UHFFFAOYSA-N 1S/C25H29N3O3/c1-17-22(19-14-23(29-2)25(31-4)24(15-19)30-3)13-20(16-27-17)18-5-7-21(8-6-18)28-11-9-26-10-12-28/h5-8,13-16,26H,9-12H2,1-4H3
£686.68 (exc VAT) per 25MG
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3574499 LDN-214117 white to beige 100 BHUXVRVMMYAXKN-UHFFFAOYSA-N 1S/C25H29N3O3/c1-17-22(19-14-23(29-2)25(31-4)24(15-19)30-3)13-20(16-27-17)18-5-7-21(8-6-18)28-11-9-26-10-12-28/h5-8,13-16,26H,9-12H2,1-4H3
£218.68 (exc VAT) per 5MG
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