LDN-192960

CAS No. 184582-62-5

LDN-192960( —— )

Catalog No. M23838 CAS No. 184582-62-5

LDN-192960 is a potent inhibitor of Haspin and DYRK2 (IC50s: 10 nM and 48 nM).

LDN-192960 is a potent inhibitor of Haspin and DYRK2 (IC50s: 10 nM and 48 nM).

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    LDN-192960
  • Note
    Research use only, not for human use.
  • Brief Description
    LDN-192960 is a potent inhibitor of Haspin and DYRK2 (IC50s: 10 nM and 48 nM).
  • Description
    LDN-192960 is a potent inhibitor of Haspin and DYRK2 (IC50s: 10 nM and 48 nM).
  • In Vitro
    LDN-192960 (10 μM) is selective and inhibits ten of the other kinases by ≥90%, with only five being potently inhibited (IC50<1 μM),including CLK1 (IC50=0.21 μM), DYRK1A(IC50= 0.10 μM), DYRK2 (IC50=2 nM), DYRK3 (IC50=19 nM) and PIM1 (IC50=0.72 μM).LDN-0192960 (0-5 μM; 2 hours) demonstrates that the classical Haspin inhibition phenotype by reducing levels of p-Thr3H3 in HeLa cells overexpressing Haspin with an EC50 of 1.17 μM. LDN-0192960 (0-1 μM; 1 hour incubation in the presence of nocodazole and MG132) demonstrates the classical Haspin inhibition phenotype by reducing levels of p-Thr3H3 in HeLa cells synchronized in mitosis with an EC50 of 0.02 μM.
  • In Vivo
    ——
  • Synonyms
    ——
  • Pathway
    Others
  • Target
    Other Targets
  • Recptor
    DYRK2| Haspin
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    184582-62-5
  • Formula Weight
    328.43
  • Molecular Formula
    C18H20N2O2S
  • Purity
    >98% (HPLC)
  • Solubility
    DMSO:30 mg/mL (91.34 mM);Water:10 mg/mL (30.45 mM)
  • SMILES
    NCCCSC1=C(C=C(OC)C=C2)C2=NC3=CC=C(OC)C=C31
  • Chemical Name
    ——

Shipping & Storage Information

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

Reference

1.Cuny GD, et al. Structure-activity relationship study of acridine analogs as haspin and DYRK2 kinase inhibitors. Bioorg Med Chem Lett. 2010 Jun 15;20(12):3491-4.
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