509882 Sigma-AldrichBMP Inhibitor IV, LDN-193189 - CAS 1062368-62-0 - Calbiochem

This product has been discontinued.

A cell-permeable pyrazoloquinoline analog of Dorsomorphin (AMPK Inhibitor, Compound C, Cat. No. 480066) that potently inhibits the transcriptional activity of BMP type 1 receptors ALK 2 and 3 (IC₅₀ = 5 and 30 nM, respectively) with minimal effect on activin and the TGF-β type 1 receptors ALK4, 5, and 7 (IC₅₀ ~500 nM). Also reported to block the activity of RIPK2 (IC₅₀ = 25 nM) and germinal central kinase (GCK; IC₅₀ = 80 nM). At higher concentration, it inhibits the activity of ALK6 (IC₅₀ = 150 nM). Also reported to block BMP-4- induced phosphorylation of SMAD 1, 5, and 8 (IC₅₀ ~ 5 nM) in murine pulmonary artery smooth muscle cells. Shown to be about 200-fold more potent when compared to Dorsomorphin. Exhibits desirable pharmacokinetic properties with a half life of 1.6 h, low clearance in liver microsomes (CL_int = 16.9 ml/min/mg protein), and a satisfactory exposure following a single intraperitoneal dose of 3 mg/kg in mice (AUC_∞ = 1000 ng . h/ml). Directs differentiation of pluripotent stem cells toward a specified lineage.

Please note that the molecular weight for this compound is batch-specific due to variable water content.