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Description: LDN-212854 (LDN 212854; LDN212854) is a potent and selective inhibitor of BMP (bone morphogenetic protein) receptor with potential antineoplastic activity. It inhibits ALK2 with an IC50 of 1.3 nM. In vivoLDN-212854 potently inhibits heterotopic ossification in an inducible transgenic mutant ALK2 mouse model of fibrodysplasia ossificans progressiva. In vitro, LDN-212854 exhibits some selectivity for ALK2 in preference to other BMP type I receptors, ALK1 and ALK3, which may permit the interrogation of ALK2-mediated signaling, transcriptional activity and function.
References: ACS Chem Biol. 2013; 8(6):1291-302.
Chemical Name: 5-(6-(4-(piperazin-1-yl)phenyl)pyrazolo[1, 5-a]pyrimidin-3-yl)quinoline
InChi Key: BBDGBGOVJPEFBT-UHFFFAOYSA-N
InChi Code: InChI=1S/C25H22N6/c1-3-21(22-4-2-10-27-24(22)5-1)23-16-29-31-17-19(15-28-25(23)31)18-6-8-20(9-7-18)30-13-11-26-12-14-30/h1-10, 15-17, 26H, 11-14H2
SMILES Code: C12=C(C3=C4N=CC(C5=CC=C(N6CCNCC6)C=C5)=CN4N=C3)C=CC=C1N=CC=C2
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