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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

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

Darren W Engers, Audrey Y Frist, Craig W Lindsley, Charles C Hong, Corey R Hopkins

Bioorg Med Chem Lett. 2013 Jun 1;23(11):3248-52.

PMID: 23639540

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.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP1062368493	ML347		1062368-49-3	Price

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