ChemicalBook--->CAS DataBase List--->1435934-00-1

1435934-00-1

1435934-00-1 Structure

1435934-00-1 Structure
IdentificationBack Directory
[Name]

LDN 193189 hydrochloride
[CAS]

1435934-00-1
[Synonyms]

LDN-193189 2HCl
LDN 193189 dihydrochloride
Viomycin LDN 193189 Dihydrochloride
4-[6-[4-(1-Piperazinyl)phenyl]pyrazolo[1,5-a]pyrimidin-3-yl]quinoline dihydrochloride
[Molecular Formula]

C25H24Cl2N6
[MOL File]

1435934-00-1.mol
[Molecular Weight]

479.404
Chemical PropertiesBack Directory
[storage temp. ]

-20°C
[solubility ]

Soluble in DMSO or in Water (up to 5 mg/ml)
[form ]

solid
[color ]

Orange-yellow
[Stability:]

Stable for 1 year from date of purchase as supplied. Solutions in DMSO or distilled water may be stored at -20°C for up to 2 months.
Hazard InformationBack Directory
[Description]

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.
[Uses]

LDN-193189 (dihydrochloride) is a potent selective BMP type I receptor (BMP I) inhibitor. LDN-193189 efficiently inhibits transcriptional activity of the BMP type I receptors ALK2 and ALK3 with IC50 values of 5 nM and 30 nM, respectively. LDN-193189 can be used for the research of bone morphogenetic protein signalling, such as fibrodysplasia ossificans progressiva[1][2][3].
[in vivo]

LDN-193189 (i.p.; 3 mg/kg; daily; for 35 days) might affect the interaction between breast cancer cells and the bone environment[3].
LDN-193189 (i.p.; 3 mg/kg; single) shows a reduction in ectopic ossification and functional impairment[1].

[storage]

Store at -20°C
[References]

1) Yu?et al.?(2008),?BMP type 1 receptor inhibition reduces heterotropic ossification; Nature Med.,14?1363 2) Chambers?et al.?(2012),?Combined small-molecule inhibition accelerates developmental timing and converts human pluripotent stem cells into nociceptors; Nature Biotechnol.?30?715 3) Kreitzer?et al. (2013)?A robust method to derive functional neural crest cells from human pluripotent stem cells; Am. J. Stem Cells,?2?119 4) Lee?et al.?(2011)?BMP4 promotes prostate tumor growth in bone through osteogenesis; Cancer Res.?71?5194
Spectrum DetailBack Directory
[Spectrum Detail]

LDN 193189 hydrochloride(1435934-00-1)1HNMR
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