LDN193189 is an optimized molecule synthesized through the modifications of parental molecule dorsomorphin [1], and acts as a highly potent and selective inhibitor of bone morphogenetic protein (BMP) type I receptors ALK2 and ALK3 (IC50 = 5 nM and 30 nM, respectively), but with much weaker effects on activin and TGF-β type I receptor ALK4, ALK5, and ALK7 (IC50≥ 500 nM). It inhibits BMP4-mediated Smad1, Smad5 and Smad8 activation in tissue expressing caALK2 infected by Ad.Cre, and reduces ectopic ossification and functional impairment in a mouse model of fibrodysplasia ossificans progressive (FOP)[2]. Both LDN193189 and Dorsomorphin affect not only the Smad but also the non-Smad signaling pathways induced by either BMP2, BMP6 or GDF5. The activation of p38, ERK1/2 and Akt in C2C12 cells is inhibited by both molecules[3]. LDN-193189 attenuates PCa-118b tumor growth via inhibition of BMP4 secretion and subsequent osteoblast differentiation [4].
Chemical Properties
Cas No.: 1062368-24-4
M. Wt.: 406.48
Formula: C25H22N6
Purity: >99%
Synonym: LDN-193189, DM-3189
Chemical Name: 4-(6-(4-(piperazin-1-yl)phenyl)pyrazolo[1,5-a]pyrimidin-3-yl)quinoline
Appearance: Yellow solid
Solubility: Soluble in water (30 mg/ml). Soluble in DMSO (4 mg/ml) and ethanol (<1 mg/mL).
Storage: Store solid at -20 °C for 2 years, protect from light.