Appearance:Solid powderPurity: > 98%
ML347(DN193719) is a highly selective ALK1/ALK2 inhibitor with IC50s of 46/32 nM; shows >300-fold selectivity for ALK2 vs. ALK3.
ML347 has IC50’s of 46 and 32 nM, respectively, against ALK1 and ALK2; however, the IC50 against ALK3 is 10,800 nM, >300-fold selective over ALK3. ML347 is completely inactive against all
the other kinases tested (with weak activity against ALK6, 9830 nM and KDR (VEGFR2)19,700 nM). ML347 is potent in the BMP4 cell assay (152 nM).
1:Bioorg Med Chem Lett. 2013 Jun 1;23(11):3248-52. doi: 10.1016/j.bmcl.2013.03.113. Epub 2013 Apr 11. Synthesis and structure-activity relationships of a novel and selective bone morphogenetic protein receptor (BMP) inhibitor derived from the pyrazolo[1.5-a]pyrimidine scaffold of dorsomorphin: the discovery of ML347 as an ALK2 versus ALK3 selective MLPCN probe.Engers DW,Frist AY,Lindsley CW,Hong CC,Hopkins CR, PMID: 23639540 PMCID: PMC3677712 DOI: 10.1016/j.bmcl.2013.03.113 Abstract: A structure-activity relationship of the 3- and 6-positions of the pyrazolo[1,5-a]pyrimidine scaffold of the known BMP inhibitors dorsomorphin, 1, LDN-193189, 2, and DMH1, 3, led to the identification of a potent and selective compound for ALK2 versus ALK3. The potency contributions of several 3-position substituents were evaluated with subtle structural changes leading to significant changes in potency. From these studies, a novel 5-quinoline molecule was identified and designated an MLPCN probe molecule, ML347, which shows >300-fold selectivity for ALK2 and presents the community with a selective molecular probe for further biological evaluation.Copyright © 2013 Elsevier Ltd. All rights reserved.