Inhibits BMP type I receptor-induced phosphorylation of SMAD1/5/8 (IC50 = 4.9 nM); shows specificity for ALK1

LDN-193189 (hydrochloride) – 5 mg

Brand:
Cayman
CAS:
1435934-00-1
Storage:
-20
UN-No:
Non-Hazardous - /

LDN-193189 inhibits SMAD1/5/8 phosphorylation by the bone morphogenetic protein (BMP) type I receptors, which are known as activin receptor-like kinases (ALKs), with an IC50 value of 4.9 nM.{23386} In in vitro kinase assays, it shows specificity for ALK1, 2, 3, and 6 (IC50s = 0.8, 0.8, 5.3, and 16.7 nM, respectively) over ALK4 and 5 (IC50s = 101 and 350 nM, respectively).{23387} LDN-193189 has been used to inhibit BMP type I receptor activity to study the pathogenesis of fibrodysplasia ossificans progressive, a congenital hyperossification disorder, and to examine the role of osteogenesis in prostate tumor metastases in bone.{23384,23385}  

 

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Description

Inhibits BMP type I receptor-induced phosphorylation of SMAD1/5/8 (IC50 = 4.9 nM); shows specificity for ALK1, 2, 3, and 6 (IC50s = 0.8, 0.8, 5.3, and 16.7 nM, respectively) over ALK4 and 5 (IC50s = 101 and 350 nM, respectively)

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

Synonyms:  DM-3189

Molecular weight: 479.4

CAS: 1435934-00-1

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|Activin-like Kinases (ALKs)||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Migration & Metastasis||Research Area|Cancer|Cell Signaling|ALK (Activin-like Kinase) Signaling||Research Area|Endocrinology & Metabolism|Bone Growth & Remodeling||Research Area|Epigenetics, Transcription, & Translation|Transcription Factors

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