LDN193189 Tetrahydrochloride,2

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LDN193189 Tetrahydrochloride

CAS No. : 2310134-98-4

MCE 国际站：LDN193189 Tetrahydrochloride

产品活性：LDN193189 Tetrahydrochloride 是一种选择性的 BMP I 型受体抑制剂，抑制 ALK2 和 ALK3 的 IC₅₀ 分别为 5 nM 和 30 nM。对 ALK4，ALK5 和 ALK7 的作用效果弱 (IC₅₀≥500 nM)。

研究领域：TGF-beta/Smad

作用靶点：TGF-β Receptor

In Vitro: 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).
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.
LDN193189 blocks the transcriptional activity induced by either constitutively active ALK2^R206H or ALK2^Q207D mutant proteins.
LDN193189 inhibits the induction of alkaline phosphatase activity in C2C12 cells by BMP4 even when administered 12 h after BMP stimulation.

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.
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.
LDN193189 reduces the ectopic bone volume and bone density.
LDN193189 completely inhibited the anti-proliferation and up-regulation of the bone morphogenetic protein (BMPR2) and Cx40 expression co-incubation with UK-92480.

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