MedChemExpress - Model LDN-214117 - 1627503-67-6

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].

LDN-214117

MCE China：LDN-214117

Brand：MedChemExpress (MCE)

Cat. No.HY-16712

CAS：1627503-67-6

Purity：99.92%

Storage：Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year

Shipping：Room temperature in continental US; may vary elsewhere.

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) [2]

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].

IC50 & Target：IC50: 24 nM (ALK2); 27 nM (ALK1); 1,171 nM (ALK3); 3,000 nM (ALK5); 1,022 nM (BMP6); 27 nM (BMP2); 960 nM (BMP4); 16,000 nM (TGF-β1)[1] Cellular Effect Cell Line Type Value Description References

References：

[1]. Agustin H Mohedas, et al. Structure-activity relationship of 3,5-diaryl-2-aminopyridine ALK2 inhibitors reveals unaltered binding affinity for fibrodysplasia ossificans progressiva causing mutants. J Med Chem. 2014 Oct 9;57(19):7900-15. [Content Brief]

[2]. Jelena Mihajlović, et al. Inhibition of bone morphogenetic protein signaling reduces viability, growth and migratory potential of non-small cell lung carcinoma cells. J Cancer Res Clin Oncol. 2019 Nov;145(11):2675-2687. [Content Brief]

[3]. Diana Carvalho, et al. ALK2 inhibitors display beneficial effects in preclinical models of ACVR1 mutant diffuse intrinsic pontine glioma. Commun Biol. 2019 May 9;2:156. [Content Brief]

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