For research use only. Not for therapeutic Use.
LDN193189 Tetrahydrochloride is a selective BMP type I receptor inhibitor, which efficiently inhibits ALK2 and ALK3 (IC50=5 nM and 30 nM, respectively), with weaker effects on ALK4, ALK5 and ALK7 (IC50≥500 nM)[1].
LDN193189 inhibits BMP4-mediated Smad1, Smad5 and Smad8 activation with great potency (IC50=5 nM) while retaining 200-fold selectivity for BMP signaling versus TGF-β signaling (IC50 for TGF-β ≥1,000 nM)[1].
LDN193189 efficiently inhibits transcriptional activity of the BMP type I receptors ALK2 and ALK3 (IC50=5 nM and 30 nM, respectively), and the TGF-β type I receptors ALK4, ALK5 and ALK7 (IC50≥500 nM) and increases selectivity for BMP signaling versus AMP-activated protein kinase, PDGFR and MAPK signaling pathways as compared to the parent compound[1].
LDN193189 blocks the transcriptional activity induced by either constitutively active ALK2R206H or ALK2Q207D mutant proteins[1].
LDN193189 inhibits the induction of alkaline phosphatase activity in C2C12 cells by BMP4 even when administered 12 h after BMP stimulation[1].
LDN193189 (Tetrahydrochloride) (i.p.;3 mg/kg;twice a day) shows the growth rates between the control vehicle- and LDN193189-treated mice are not significantly different after the first 5 weeks, but differences in the growth rates are detected after 6 and 7 weeks post-treatment[2].
LDN193189 (s.c;5 days) shows significantly the difference of tumor size at 6 and 7 weeks post-treatment and the tumor weights also show significant differences at the termination of the study at week 7[2].
LDN193189 reduces the ectopic bone volume and bone density[2].
LDN193189 completely inhibited the anti-proliferation and up-regulation of the bone morphogenetic protein (BMPR2) and Cx40 expression co-incubation with UK-92480[3].
| Catalog Number | I020708 |
| CAS Number | 2310134-98-4 |
| Synonyms | 4-[6-(4-piperazin-1-ylphenyl)pyrazolo[1,5-a]pyrimidin-3-yl]quinoline;tetrahydrochloride |
| Molecular Formula | C25H26Cl4N6 |
| Purity | ≥95% |
| InChI | InChI=1S/C25H22N6.4ClH/c1-2-4-24-22(3-1)21(9-10-27-24)23-16-29-31-17-19(15-28-25(23)31)18-5-7-20(8-6-18)30-13-11-26-12-14-30;;;;/h1-10,15-17,26H,11-14H2;4*1H |
| InChIKey | NYHXPFHFIMRKDS-UHFFFAOYSA-N |
| SMILES | C1CN(CCN1)C2=CC=C(C=C2)C3=CN4C(=C(C=N4)C5=CC=NC6=CC=CC=C56)N=C3.Cl.Cl.Cl.Cl |
| Reference | [1]. Yu PB, et al. BMP type I receptor inhibition reduces heterotopic [corrected] ossification. Nat Med, 2008, 14(12), 1363-1369. [2]. Lee YC, et al. BMP4 promotes prostate tumor growth in bone through osteogenesis. Cancer Res, 2011, 71(15), 5194-5203. [3]. 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. |
