| Identification | Back Directory | [Name]
LDN193189 Tetrahydrochloride | [CAS]
2310134-98-4 | [Synonyms]
LDN193189 Tetrahydrochloride | [Molecular Formula]
C??H??Cl?N? | [MDL Number]
MFCD30207834 | [MOL File]
2310134-98-4.mol | [Molecular Weight]
442.95 |
| Chemical Properties | Back Directory | [storage temp. ]
Store at -20°C | [solubility ]
Water: 33.33 mg/mL (60.34 mM); DMSO: 4.17 mg/mL (7.55 mM) | [form ]
Solid | [color ]
Light yellow to yellow |
| Hazard Information | Back Directory | [Uses]
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]. | [in vivo]
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]. | [IC 50]
ACVR1: 5 nM (IC50); BMPR1A: 30 nM (IC50) | [References]
[1] Yu PB, et al. BMP type I receptor inhibition reduces heterotopic [corrected] ossification. Nat Med, 2008, 14(12), 1363-1369. DOI:10.1038/nm.1888
[2] Lee YC, et al. BMP4 promotes prostate tumor growth in bone through osteogenesis. Cancer Res, 2011, 71(15), 5194-5203. DOI:10.1158/0008-5472.CAN-10-4374
[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. PMID:25197339 |
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