LDN193189Catalog No. A11205

Quick Overview

LDN193189 is a highly potent small molecule BMP inhibitor that inhibits BMP type I receptors ALK2 (IC50: 5 nM), ALK3 (IC50: 30 nM) and ALK6 (TGFβ1/BMP signaling) and subsequent SMAD phosphorylation.
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LDN193189

Product Information
Catalog Num A11205
M. Wt 406.48
Formula C25H22N6
Solubility DMSO
Purity >98%
Storage at -20°C 3 years Powder
CAS No. 1062368-24-4
Synonyms LDN-193189
Chemical Name 4-[6-(4-Piperazin-1-yl-phenyl)-pyrazolo[1,5-a]pyrimidin-3-yl]-quinoline hydrochloride
SMILES Code C1CN(CCN1)C2=CC=C(C=C2)C3=CN4C(=C(C=N4)C5=CC=NC6=CC=CC=C56)N=C3

Biological activity
Introduction
LDN193189 is a highly potent small molecule BMP inhibitor that inhibits BMP type I receptors ALK2 (IC50: 5 nM), ALK3 (IC50: 30 nM) and ALK6 (TGFβ1/BMP signaling) and subsequent SMAD phosphorylation.
Targets
ALK2 (C2C12 cells) ALK3 (C2C12 cells)
5 nM30 nM
Solubility
Solubility (25C) * In vitro DMSO 0.01 mg/mL (<1 mM)
Water 0.01 mg/mL (<1 mM)
Ethanol <1 mg/mL (<1 mM)
In vivo Saline 30 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Adooq tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

LDN-193189 is a cell permeable small molecule inhibitor of bone morphogenetic protein (BMP) type I receptors ALK2 and ALK3 (IC50 = 5 nM and 30 nM respectively). LDN-193189 was derived from structure-activity relationship studies of Dorsomorphin and functions primarily through prevention of Smad1, Smad5, and Smad8 phosphorylation. LDN-193189 only weakly inhibits ALK4, ALK5, and ALK7. BMP signaling coordinates developmental patterning and has essential physiological roles in mature organisms. LDN-193189  has been used to reduce ectopic ossification in a mouse model of fibrodysplasia ossificans progressiva

Reference:

 1.  Cuny GD, et al.  Structure-activity relationship study of bone morphogenetic protein (BMP) signaling inhibitors. (2008), Bioorg Med Chem Lett. 18(15):4388-92.

2.  Paul B Yu, et al. BMP type I receptor inhibition reduces heterotopic ossification. (2008), Nature Med. 14: 1363-1369.

3.  Yu PB, et al.  Dorsomorphin inhibits BMP signals required for embryogenesis and iron metabolism. (2008), Nature Chem Biol. 4: 33-41.

4.  Chambers SM, et al. Highly efficient neural conversion of human ES and iPS cells by dual inhibition of SMAD signaling. (2009), Nature Biotechnology 27, 275-280.

5.  Boergermann JH, et al. Dorsomorphin and LDN-193189 inhibit BMP-mediated Smad, p38 and Akt signalling in C2C12 cells. (2010), Int J Biochem Cell Biol. 42(11):1802-7.

6.  Lee YC, et al. BMP4 promotes prostate tumor growth in bone through osteogenesis.  (2011), Cancer Res 71:5194-5203.

7.  Najm FJ, et al. Rapid and robust generation of functional oligodendrocyte progenitor cells from epiblast stem cells. (2011) Nature Methods 8, 957–962

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High Purity Kinase Inhibitors on Signaling Pathways

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