Small Molecules for Stem Cell Research
LDN193189 (HCl) is a highly-potent inhibitor of BMP signaling, specifically blocking ALK1 (IC50 of 0.8 nM), ALK2 (IC50 of 0.8 nM), ALK3 (IC50 of 5.3 nM), and ALK6 (IC50 of 16.7 nM), and in turn affecting Smad1/5/8 expression (Galvin-Burgess, et al.). LDN193189 (HCl) has been shown to contribute to the differentiation of pluripotent stem cells (PSCs) into functional pancreatic beta cells when combined with CHIR99021, SANT-1, Y27632, Compound E, RepSox, Triiodothyronine Salt along with other growth factors (Pagliuca, et al.). LDN193189 has also been utilized in the derivation of neural progenitor cells (Edri, et al.), and cortical neurons (Qi, et al.) from PSCs.
|Molecular Name||LDN193189 (4HCl)|
|Alternative Names||LDN193189 tetrahydrochloride, LDN-193189, 1062368-62-0|
|Chemical Name||Quinoline, 4-[6-[4-(1-piperazinyl)phenyl]pyrazolo[1,5-a]pyrimidin-3-yl]-, tetrahydrochloride|
|Purity||Greater than 95% by LCMS|
|Physical Appearance||Light yellow to yellow (Solid)|
|Shelf-Life||≥ 2 years (powder)|
|Storage||Store at -20°C|
|Quality Statement||This product is for Research Use Only and is not intended for therapeutic or diagnostic use.|
References and Publications
Qi, et al. 2017. Combined small-molecule inhibition accelerations the derivation of functional cortical neurons from human pluripotent stem cells. Nature Biotechnology 35(2): 154-163.
Pagliuca, et al. 2014. Generation of functional human pancreatic β cells in vitro. Cell 159: 428-439.
Yang L, et al. UK-92480 increases connexin 40 in smooth muscle cells through activation of BMP pathways in pulmonary arterial hypertension. Int J Clin Exp Pathol. 2014 Jul 15;7(8):4674-84.
Galvin-Burgess, et al. 2012. TGF-β-superfamily signaling regulates embryonic stem cell heterogeneity: Self-renewal as a dynamic and regulated equilibrium. Stem Cells. 31(1): 45-58.
Lee YC, et al. BMP4 promotes prostate tumor growth in bone through osteogenesis. Cancer Res, 2011, 71(15), 5194-5203.
Cuny, G.D., Yu, P.B., Laha, J.K., et al. Structure-activity relationship study of bone morphogenetic protein (BMP) signaling inhibitors. Bioorganic & Medicinal Chemistry Letters 18(15), 4388-4392 (2008).
Yu PB, et al. BMP type I receptor inhibition reduces heterotopic [corrected] ossification. Nat Med, 2008, 14(12), 1363-1369.