LDN-214117,1627503-67-6

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LDN-214117

CAS No. : 1627503-67-6

MCE 国际站：LDN-214117

产品活性：LDN-214117 是一种 ALK2 抑制剂，具有口服活性，耐受性好，脑穿透性好。LDN-214117 对 ALK2 具有较高的选择性和较低的细胞毒性，其 IC₅₀ 值为 24 nM。LDN-214117 也是一种特异性的骨形态发生蛋白 (BMPs) 信号抑制剂，对 BMP6 具有相对选择的抑制作用，其 IC₅₀ 值为 100 nM。LDN-214117 可用于进行性骨化性纤维发育不良 (FOP) 和弥漫性内源性桥脑胶质瘤 (DIPG) 的研究。

研究领域：TGF-beta/Smad

作用靶点：TGF-β Receptor

In Vitro: LDN-214117 has high inhibition and selectivity for ALK2 kinase proteins with an IC₅₀ value of 24 nM.
LDN-214117 has kinase activity for ALK1, ALK3 and ALK5 with IC₅₀ values of 27 nM, 1,171 nM and 3,000 nM, respectively.
LDN-214117 exhibits relatively selective inhibition for BMP6, BMP2 and BMP4 with IC₅₀ values of 100 nM, 1,022 nM and 960 nM, respectively.
LDN-214117 has inhibition of TGF-β1-induced transcriptional activity with an IC₅₀ values of 16,000 nM.
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.
LDN-214117 (5 μM, 24-120 h) reduces viability, proliferation and causes apoptosis of lung carcinoma cells LCLC-103H.
LDN-214117 (5 μM, 0-48 h) suppresses wound healing and chemotactic potential of LCLC-103H cells.
LDN-214117 (5 μM, 48 h) hinders growth of multicellular LCLC-103H spheroids.

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

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