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LDN-193189 HCl

Catalog No. T6158   CAS 1062368-62-0
Synonyms: LDN193189 Hydrochloride

LDN-193189 HCl (LDN193189 Hydrochloride) is a selective BMP type I receptor kinases inhibitor.

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LDN-193189 HCl Chemical Structure
LDN-193189 HCl, CAS 1062368-62-0
Pack Size Availability Price/USD Quantity
1 mg In stock $ 37.00
2 mg In stock $ 50.00
5 mg In stock $ 72.00
10 mg In stock $ 89.00
25 mg In stock $ 162.00
50 mg In stock $ 282.00
100 mg In stock $ 423.00
1 mL * 10 mM (in DMSO) In stock $ 97.00
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Purity: 100%
Purity: 99.49%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description LDN-193189 HCl (LDN193189 Hydrochloride) is a selective BMP type I receptor kinases inhibitor.
Targets&IC50 ALK6:16.7 nM, ALK1:0.8 nM, ALK3:5.3nM, ALK2:0.8nM
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. [1] 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. [4]
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. [1] LDN193189 dorsalizes zebrafish embryos by inhibiting signaling pathways induced by bone morphogenetic protein (BMP)6 without effect on vascular development. [2] In PCa-118b tumor-bearing mice, LDN-193189 treatment attenuates tumor growth and reduces bone formation in the tumors. [3] 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. [4]
Kinase Assay C2C12 cells are seeded into 96-well plates at 2,000 cells per well in DMEM supplemented with 2% FBS. The wells are treated in quadruplicate with BMP ligands and LDN-193189 or vehicle. The cells are collected after 6 d in culture in 50 μL Tris-buffered saline and 1% Triton X-100. The lysates are added to p-nitro-phenylphosphate reagent in 96-well plates for 1 h and then evaluated alkaline phosphatase activity (absorbance at 405 nm). Cell viability are measured and quantity by Cell Titer Aqueous One (absorbance at 490 nm), using replicate wells treated identically to those used for alkaline phosphatase measurements[1].
Cell Research Concentrations: 3 μM
Synonyms LDN193189 Hydrochloride
Molecular Weight 442.94
Formula C25H22N6·HCl
CAS No. 1062368-62-0

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 10 mg/mL (22.58 mM), Sonification is recommended

TargetMolReferences and Literature

1. Yu PB, et al. Nat Med, 2008, 14(12), 1363-1369. 2. Cannon JE, et al. Br J Pharmacol, 2010, 161(1), 140-149. 3. Lee YC, et al. Cancer Res, 2011, 71(15), 5194-5203. 4. Derwall M, et al. Arterioscler Thromb Vasc Biol, 2012, 32(3), 613-622.

Related compound libraries

This product is contained In the following compound libraries:
Tyrosine Kinase Inhibitor Library Bioactive Compound Library Kinase Inhibitor Library Anti-Cancer Compound Library Angiogenesis related Compound Library Osteogenesis Compound Library Anti-Lung Cancer Compound Library Bioactive Compounds Library Max Inhibitor Library NO PAINS Compound Library

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ALK-IN-5 Belizatinib AZD-3463 EML4-ALK kinase inhibitor 1 A 83-01 KRCA-0008 ALK-IN-1 ALK inhibitor 1

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Keywords

LDN-193189 HCl 1062368-62-0 Angiogenesis Tyrosine Kinase/Adaptors ALK LDN 193189 Hydrochloride LDN 193189 HCl LDN-193189 Hydrochloride LDN193189 HCl LDN193189 Hydrochloride inhibitor inhibit

 

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