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LDN193189 hydrochloride

Chemical Structure : LDN193189 hydrochloride

CAS No.: 1062368-62-0

LDN193189 hydrochloride (LDN 193189 hydrochloride;LDN-193189 hydrochloride)

Catalog No.: PC-42885Not For Human Use, Lab Use Only.

LDN193189 is a potent, selective BMP type I receptor that inhibits BMP4-induced phosphorylation of SMAD1/5/8 with IC50 of 5 nM, displays >200-fold selectivity for BMP signaling over TGF-β signaling (IC50>1,000 nM).

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

LDN193189 hydrochloride is a potent, selective BMP type I receptor that inhibits BMP4-induced phosphorylation of SMAD1/5/8 with IC50 of 5 nM, displays >200-fold selectivity for BMP signaling over TGF-β signaling (IC50>1,000 nM).
LDN193189 efficiently inhibits transcriptional activity of the BMP type I receptors ALK2 and ALK3 (IC50=5 nM and 30 nM, respectively), with weaker effects on activin and the TGF-β type I receptors ALK4, ALK5 and ALK7.
LDN193189 also blocks the transcriptional activity induced by either constitutively active ALK2 R206H or ALK2 Q207D mutant proteins, affects BMP-induced osteoblast differentiation, attenuates ectopic ossification in vivo.

Physicochemical Properties

M.Wt 552.3261
Formula C25H26Cl4N6
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

H2O: 20 mg/mL

Chemical Name/SMILES

Quinoline, 4-[6-[4-(1-piperazinyl)phenyl]pyrazolo[1,5-a]pyrimidin-3-yl]-, hydrochloride (1:1)

References

1. Yu PB, et al. Nat Med. 2008 Dec;14(12):1363-9.

2. Cuny GD, et al. Bioorg Med Chem Lett. 2008 Aug 1;18(15):4388-92.

3. Cannon JE, et al. Br J Pharmacol. 2010 Sep;161(1):140-9.

4. Steinbicker AU, et al. Blood. 2011 May 5;117(18):4915-23.

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