LDN-214117

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