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LDN-193189 2HCl

CAS No. 1435934-00-1

LDN-193189 2HCl( —— )

Catalog No. M34754 CAS No. 1435934-00-1

LDN-193189 2HCl (DM-3189 2HCl) is a selective BMP signaling inhibitor that inhibits ALK1,ALK2,ALK3 and ALK6, showing IC50s of 0.8 nM, 0.8 nM, 5.3 nM, and 16.7 nM, respectively, in kinase assays.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    LDN-193189 2HCl
  • Note
    Research use only, not for human use.
  • Brief Description
    LDN-193189 2HCl (DM-3189 2HCl) is a selective BMP signaling inhibitor that inhibits ALK1,ALK2,ALK3 and ALK6, showing IC50s of 0.8 nM, 0.8 nM, 5.3 nM, and 16.7 nM, respectively, in kinase assays.
  • Description
    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.
  • In Vitro
    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 has weake effects on activin and the TGF-β type I receptors ALK4, ALK5 and ALK7 with IC50 values of ≥ 500 nM.LDN-193189 binds ActRIIA with Kd value of 14 nM.LDN-193189 (0.5 μM; 30 min) targets GDF8 induced Smad2/3 signaling and repression of myogenic transcription factors.LDN-193189 (0.05, 0.5, 5 μM) efficiently inhibits GDF8 induced Smad3/4 reporter gene activity.LDN-193189 (0-5 μM) rescues myogenesis in myoblasts treated with GDF8.
  • 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.LDN-193189 (i.p.; 3 mg/kg; single) shows a reduction in ectopic ossification and functional impairment.
  • Synonyms
    ——
  • Pathway
    Others
  • Target
    Other Targets
  • Recptor
    TGF-beta/Smad | ALK
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    1435934-00-1
  • Formula Weight
    479.4
  • Molecular Formula
    C25H24Cl2N6
  • Purity
    >98% (HPLC)
  • Solubility
    In Vitro:?H2O : 11.11 mg/mL (23.17 mM; Ultrasonic)DMSO : 10 mg/mL (20.86 mM; Ultrasonic (<60°C)
  • SMILES
    C1(C2=C3N=CC(C4=CC=C(N5CCNCC5)C=C4)=CN3N=C2)=C6C=CC=CC6=NC=C1.Cl.Cl
  • Chemical Name
    ——

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. Yu PB, et al. BMP type I receptor inhibition reduces heterotopic [corrected] ossification. Nat Med, 2008, 14(12), 1363-1369.?
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