DMH1

DMH1 is a potent and highly selective small molecule inhibitor of Bone Morphogenetic Protein (BMP) type I receptors, specifically targeting Activin receptor-like kinase 1 (ALK1), Activin A receptor type 1 (ACVR1/ALK2), and Bone morphogenetic protein receptor type 1A (BMPR1A/ALK3). Developed as a more selective derivative of dorsomorphin (Compound C), DMH1 is designed to avoid the off-target inhibition of VEGF and AMPK pathways. Its mechanism of action involves binding to the intracellular kinase domain of BMP type I receptors, thereby blocking the phosphorylation of SMAD1/5/8 proteins and the subsequent transcription of downstream target genes such as ID1 and ID3. In preclinical research, DMH1 has shown significant efficacy in suppressing tumor cell viability and proliferation in various malignancies, including endometrial cancer, where BMP signaling is frequently overactivated by ACVR1 mutations or ligand overexpression. It is also a critical tool in studying the pathophysiology of fibrodysplasia ossificans progressiva (FOP).

Other names

4-[6-(4-Isopropoxyphenyl)pyrazolo[1,5-a]pyrimidin-3-yl]quinolineDMH-1DMH1DMH 1