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LDN-193189 HCl

LDN-193189 HCl structure

LDN-193189 HCl 

structure
  • CAS No:

    1062368-62-0

  • Formula:

    C25H23ClN6

  • Chemical Name:

    LDN-193189 HCl

  • Synonyms:

    4-(6-(4-(piperazin-1-yl)phenyl)pyrazolo[1,5-a]pyrimidin-3-yl)quinoline hydrochloride;4-(6-(4-(Piperazin-1-yl)phenyl)pyrazolo[1,5-a]pyriMidin-3-yl)quinoline HCl;LDN193189 (Hydrochloride);4-[6-[4-(1-Piperazinyl)phenyl]pyrazolo[1,5-a]pyrimidin-3-yl]quinoline hydrochloride (1:1);LDN-193189 HCl

  • Categories:

    Biochemical Engineering  >  Inhibitors

Description

LDN193189 Hydrochloride is a BMP signaling inhibitor, inhibiting ALK1, ALK2, ALK3 and ALK6 with IC50s of 0.8, 0.8, 5.3, 16.7 nM, respectively.

LDN-193189 HCl Basic Attributes

442.94332

442.167

Characteristics

58.4

LDN-193189 HCl Use and Manufacturing

Methods of Manufacturing

A mixture of 18a (640 mg, 1.26 tnmol) in MeOH (10 mL) and HCl in 1 , 4- dioxane (4M, 6.3 mL) was stirred at rt for 24 h before being concentrated to dryness. The residue was washed with a small amount of MeOH to give 13-HCI (550 mg, 98percent yield) as a yellow solid.

Uses

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. 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). 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.[Cayman Chemical]

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