LDN-193189
Catalog No.: GC16580Purity:>99.00%Synonyms: LDN 193189;LDN193189
Inhibidor de ALK, potente y selectivo.
Los productos son exclusivamente para uso en investigación. No aptos para uso humano. No vendemos a pacientes.
Cas No.: 1062368-24-4
5mgIn Stock
$63.00
1
10mgIn Stock
$108.00
1
50mgIn Stock
$446.00
1
| Pack Size | Price | Availability | Quantity | Action |
|---|---|---|---|---|
| 5mg | $63.00 | In Stock | 1 | |
| 10mg | $108.00 | In Stock | 1 | |
| 50mg | $446.00 | In Stock | 1 |
Tel: (909) 407-4943 / (909) 689-7124Email: sales@glpbio.com
Citas (Citations)
3 publicationsPublicaciones de investigadores que utilizan este productoDescripción (Description)
LDN193189 is a selective transcriptional activity morphogenetic protein (BMP) type I receptors inhibitor. It inhibits activin receptor-like kinase-2 (ALK2) and ALK3 with IC50 values of 5 nM and 30 nM, respectively [1].
LDN193189 has been showed to inhibit BMP induced phosphorylation of Smad signaling (Smad1/5/8) and non-Smad signaling including p38 and Akt in C2C12 cells [2].
Pharmacological inhibition of BMP by LDN193189 has shown to prevent down-regulation of E-cadherin in response to BMP2 both in bronchial epithelial (Beas2B) cells and in C57BL/6 mice. LDN193189 also inhibits the BMP-induced reduction of epithelial permeability at cellular level [3].
References:
[1] Yu PB, Deng DY, Lai CS, Hong CC, Cuny GD, Bouxsein ML, Hong DW, McManus PM, Katagiri T, Sachidanandan C, Kamiya N, Fukuda T, Mishina Y, Peterson RT, Bloch KD. BMP type I receptor inhibition reduces heterotopic [corrected] ossification. Nat Med. 2008 Dec;14(12):1363-9.
[2] Boergermann JH1, Kopf J, Yu PB, Knaus P. Dorsomorphin and LDN-193189 inhibit BMP-mediated Smad, p38 and Akt signalling in C2C12 cells. Int J Biochem Cell Biol. 2010 Nov;42(11):1802-7.
[3] Helbing T1, Herold EM, Hornstein A, Wintrich S, Heinke J, Grundmann S, Patterson C, Bode C, Moser M. Inhibition of BMP activity protects epithelial barrier function in lung injury. J Pathol. 2013 Sep;231(1):105-16. doi: 10.1002/path.4215. Epub 2013 Jul 10.
Protocolo (Protocol)
| Cell experiment [1]: | |
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Cell lines |
C2C12 myofibroblast cells; bronchial epithelial (Beas2B) cells |
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Preparation method |
This compound is limited soluble in DMSO. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
|
Reacting condition |
0.005-5 μM. 30-60 min |
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Applications |
LDN-193189 inhibited both BMP induced Smad1/5/8 phosphorylation and BMP-mediated induction of the p38 MAPK, Erk1/2 and Akt pathway in C2C12 cells. LDN-193189 dose-dependently inhibited the activation of Smad1/5/8, p38 and Akt. LDN-193189 induced a strong increase in phosphorylated p38 MAPK levels and a slight increase in p-Akt in C2C12 cells. LDN (10 μM, 60 min) induced p38 and Akt phosphorylation. LDN (0.5 μM, 30 min) inhibited BMP-mediated Smad1/5/8, p38, ATF2 and CREB phosphorylation. |
| Animal experiment [2]: | |
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Animal models |
C57BL/6 mice |
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Dosage form |
Intraperitoneal injection; 3 mg/kg every 12 h |
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Application |
In Ad.Cre-injected, caALK2-expressing mice, treatment with LDN-193189 prevented radiographic lesions at P15. LDN-193189–treated mice appeared to preserve knee and ankle joints at P30 and P60. LDN-193189-treated mice showed no ectopic bone at P15 but did show enhanced cartilage formation in surrounding soft tissues. LDN-193189–treated mice showed mildly impaired range of motion even in the absence of radiographically visible disease at P30. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1]. Yu PB, Deng DY, Lai CS, Hong CC, Cuny GD, Bouxsein ML, Hong DW, McManus PM, Katagiri T, Sachidanandan C, Kamiya N, Fukuda T, Mishina Y, Peterson RT, Bloch KD. BMP type I receptor inhibition reduces heterotopic [corrected] ossification. Nat Med. 2008 Dec;14(12):1363-9. [2]. Yu PB, Deng DY, Lai CS, Hong CC, Cuny GD, Bouxsein ML, Hong DW, McManus PM, Katagiri T, Sachidanandan C, Kamiya N, Fukuda T, Mishina Y, Peterson RT, Bloch KD. BMP type I receptor inhibition reduces heterotopic [corrected] ossification. Nat Med. 2008 Dec;14(12):1363-9. | |
Documentos del producto (Product Documents)
Purity:>99.00%Appearance:A solid
Datos biológicos (Biological Data)
1 / 1
Propiedades químicas (Chemical Properties)
N.º CAS
1062368-24-4
Sinónimos
LDN 193189;LDN193189
Nombre químico
4-[6-(4-piperazin-1-ylphenyl)pyrazolo[1,5-a]pyrimidin-3-yl]quinoline
SMILES
C1CN(CCN1)C2=CC=C(C=C2)C3=CN4C(=C(C=N4)C5=CC=NC6=CC=CC=C56)N=C3
Fórmula molecular
C25H22N6
Peso molecular
406.48
Solubilidad
<0.81mg/mL in DMSO
Almacenamiento
Store at -20°C
Consejos generales
Seleccione un disolvente adecuado según los datos de solubilidad del producto. Una vez preparada, divida la solución madre en alícuotas para evitar ciclos repetidos de congelación y descongelación.
Utilice las soluciones madre en un plazo de 6 meses si se conservan a -80°C, o de 1 mes si se conservan a -20°C.
Para mejorar la solubilidad, caliente el tubo a 37°C y soníquelo durante un periodo adecuado.
Utilice las soluciones madre en un plazo de 6 meses si se conservan a -80°C, o de 1 mes si se conservan a -20°C.
Para mejorar la solubilidad, caliente el tubo a 37°C y soníquelo durante un periodo adecuado.
Condiciones de envío
Las muestras de evaluación se envían con acumuladores de frío. Los demás tamaños se envían a temperatura ambiente o, previa solicitud, con acumuladores de frío.
Calculadoras (Calculators)Molaridad / Dilución / Peso molecular / Conversión de unidades / Formulación in vivo / Solubilidad
g/mol
Reviews
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