Selectively inhibits ALK1 (IC50 = 46 nM) and ALK2 (IC50 = 32 nM) with >300-fold selectivity over ALK3

ML-347 – 50 mg

Brand:
Cayman
CAS:
1062368-49-3
Storage:
-20
UN-No:
Non-Hazardous - /

Activation of bone morphogenetic protein (BMP) type I receptors, also known as activin receptor-like kinases (ALK1-7), leads to the assembly of SMAD complexes, which translocate to the nucleus to induce transcriptional activation important for normal development and tissue repair.{9612} ML-347 is a 5-quinoline compound that inhibits ALK1 and ALK2 with IC50 values of 46 and 32 nM, respectively.{28723} It demonstrates >300-fold selectivity for ALK2 over ALK3, ALK6, and VEGF type 2 receptor (IC50s = 10.8, 9.8, and 19.7 µM, respectively) and is inactive at ALK4, ALK5, BMP type 2 receptors, TGF-β type 2 receptor, and AMPK.{28723} In a functional assay, ML-347 was shown to inhibit BMP4 signaling with an IC50 value of 152 nM.{28723}  

 

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Description

Selectively inhibits ALK1 (IC50 = 46 nM) and ALK2 (IC50 = 32 nM) with >300-fold selectivity over ALK3, ALK6, and VEGF type 2 receptor; inhibits BMP4 signaling with an IC50 value of 152 nM in a functional assay

Formal name: 5-[6-(4-methoxyphenyl)pyrazolo[1,5-a]pyrimidin-3-yl]-quinoline

Synonyms:  LDN193719

Molecular weight: 352.4

CAS: 1062368-49-3

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|Activin-like Kinases (ALKs)||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cell Biology|Cell Signaling

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