LDN-193189 HCl

SKU: orb1301025

Description

LDN-193189 HCl is a potent and selective small molecule inhibitor of BMP type I receptor kinases (ALK2/3/6). It is widely used in research to study BMP signaling pathways in vitro and has been applied in vivo to investigate bone formation, stem cell differentiation, and embryonic development.

Research Area

Cardiovascular Research, Signal Transduction

Images & Validation

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Key Properties

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CAS Number	1062368-62-0
MW	442.94
Purity	>99.99% (May vary between batches)
Formula	C₂₅H₂₂N₆·HCl
SMILES	Cl.C1CN(CCN1)c1ccc(cc1)-c1cnc2c(cnn2c1)-c1ccnc2ccccc12
Target	ALK
Solubility	DMSO:7.29 mg/mL (16.46 mM)

Bioactivity

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Target IC50	ALK3:5.3nM\|ALK6:16.7 nM\|ALK1:0.8 nM\|ALK2:0.8nM
In Vivo	In conditional caALK2-transgenic mice with Ad.Cre on on postnatal day 7 (P7), LDN-193189 (3 mg/kg i.p) leads to mild calcifications surrounding the left tibia and fibula first visible at P13, and prevents radiographic lesions at P15 without causing weight loss or growth retardation, spontaneous fractures, decreased bone density or behavioral abnormalities. LDN193189 dorsalizes zebrafish embryos by inhibiting signaling pathways induced by bone morphogenetic protein (BMP)6 without effect on vascular development. In PCa-118b tumor-bearing mice, LDN-193189 treatment attenuates tumor growth and reduces bone formation in the tumors. In LDL receptor-deficient (LDLR-/-) mice, LDN-193189 potently inhibits development of atheroma. Moreover, LDN-193189 also exhibits the inhibitory effects on associated vascular inflammation, osteogenic activity, and calcification. Read more...
In Vitro	LDN193189 potently inhibits BMP4-mediated Smad1, Smad5 and Smad8 activation with IC50 of 5 nM, and efficiently inhibits transcriptional activity of the BMP type I receptors ALK2 and ALK3 with IC50 of 5 nM and 30 nM, respectively. Furthermore, LDN193189 also shows the inhibitory effect on the transcriptional activity induced by either constitutively active ALK2R206H or ALK2Q207D mutant proteins. A recent study shows that LDN-193189 blocks the production of reactive oxygen species induced by oxidized LDL during atherogenesis in human aortic endothelial cells. Read more...
Cell Research	Concentrations: 3 μM

Storage & Handling

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Storage	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice/Shipping at ambient temperature.
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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ALK2, ALK3, LDN 193189 HCl, LDN 193189 Hydrochloride, LDN193189 HCl, LDN-193189 HCl, LDN193189 Hydrochloride, LDN-193189 Hydrochloride

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Compound Identifiers

PubChem CID

54613581 ↗

Key Properties

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No computed properties available.

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LDN-193189 HCl (orb1301025)

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LDN-193189 HCl

Description

Research Area

Images & Validation

Key Properties

Bioactivity

Storage & Handling

Alternative Names

Quality Guarantee

Compound Identifiers

Key Properties

Documents Download

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Protocol Information

LDN-193189 HCl (orb1301025)

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