LDN-193189 2HCl

SKU: orb1694659

Description

LDN-193189 2HCl is a potent and selective BMP type I receptor (ALK1, ALK2, ALK3, ALK6) inhibitor, demonstrating low nanomolar IC50 values in kinase and cellular assays. It is over 200-fold selective for BMP over TGF-β signaling. This inhibitor is widely used in research to study bone morphogenetic protein pathways in both in vitro and in vivo models of osteogenesis, hematopoiesis, and fibrodysplasia ossificans progressiva.

Research Area

Cardiovascular Research, Signal Transduction, Stem Cell & Developmental Biology

Images & Validation

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Key Properties

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CAS Number	1435934-00-1
MW	479.4
Purity	99.87% (May vary between batches)
Formula	C₂₅H₂₄Cl₂N₆
SMILES	C1(C2=C3N=CC(C4=CC=C(N5CCNCC5)C=C4)=CN3N=C2)=C6C=CC=CC6=NC=C1.Cl.Cl
Target	TGF-beta/Smad,ALK
Solubility	H2O:45 mg/mL (93.87 mM);DMSO:8.77 mg/mL (18.29 mM)

Bioactivity

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Target IC50	ALK2 (cell-free assay):0.8 nM\|ALK1 (cell-free assay):0.8 nM\|ALK3 (cell-free assay):5.3 nM\|ALK6 (cell-free assay):16.7 nM
In Vivo	LDN-193189 (3 mg/kg, intraperitoneal injection; birth in conditional caALK2) caused weak calcification of the left tibia and fibula, which was visible on day 13 and blocked on day 15 without causing weight loss or growth retardation, spontaneous fractures, decreased bone density, or abnormal behavior. LDN193189 forms curved Zebrafish embryos by inhibiting the signal pathway induced by bone morphogenetic protein (BMP) 6 and has no effect on vascular development. In mice with PCa-118b tumors, LDN-193189 treatment slowed down tumor growth and reduced bone formation in the tumor. In LDLR -/- mice, LDN-193189 inhibited the development of arterial atherosclerosis. In addition, LDN-193189 has inhibitory effects on vascular inflammation, osteogenic activity, and calcification. Read more...
In Vitro	LDN193189 can effectively inhibit BMP4-mediated activation of Smad1, Smad5, and Smad8, with IC50 of 5 nM. It can also effectively inhibit the transcriptional activity of BMP type I receptors ALK2 and ALK3, with IC50 of 5 nM and 30 nM, respectively. LDN193189 also has an inhibitory effect on transcriptional activation induced by persistently activated ALK2R206H or ALK2Q207D mutant proteins. A recent study showed that LDN-193189 blocks the production of oxidative free radicals induced by oxidized LDL in human arterial endothelial cells. Read more...

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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LDN193189, LDN-193189, LDN-193189 2HCl, LDN 193189, DM 3189, DM3189, DM-3189, DM-3189 2HCl, bone morphogenetic protein (BMP), ALK1, ALK6, ALK3, ALK2, TGFb, TGF-b/Smad, TGFβ, TGFbeta/Smad, TGF-β/Smad, TGFbeta, TGF-beta, Smad

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Compound Identifiers

PubChem CID

91900717 ↗

Key Properties

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No computed properties available.

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LDN-193189 2HCl (orb1694659)

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Purity:	>98% (HPLC)
CAS Number:	1435934-00-1
MW:	479.4
Formula:	C₂₅H₂₄Cl₂N₆

LDN-193189 2HCl

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Key Properties

Bioactivity

Storage & Handling

Alternative Names

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