In Vitro: LDN-212854 (0-3.815 μM) blocks the phosphorylation of SMAD1/5/8 induced by BMP7 in BMPR2−/− cells. LDN-212854 (2.5 μM, 5 days ) inhibits cell proliferation in Huh7 and MT cells. LDN-212854 (0.5 μM, 48 h ) suppresses ID1 and EpCAM expression in Huh7 and MT cells.
In Vivo: LDN-212854 (intraperitoneal injection, 6 mg/kg, twice daily for 4 weeks) potently inhibits heterotopic ossification in an inducible transgenic mutant ALK2 mouse model of fibrodysplasia ossificans progressiva. LDN-212854 (intraperitoneal injection, 6 mg/kg, twice daily for 10-14 days) suppresses HCC tumor progression through repression of ID1 in HCC xenografts model.