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SKI-178

CAS No. 1259484-97-3

SKI-178( —— )

Catalog No. M23431 CAS No. 1259484-97-3

SKI-178 is a sphingosine kinase 1 (SphK1) inhibitor with IC50 of 0.1-1.8 μM.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    SKI-178
  • Note
    Research use only, not for human use.
  • Brief Description
    SKI-178 is a sphingosine kinase 1 (SphK1) inhibitor with IC50 of 0.1-1.8 μM.
  • Description
    SKI-178 is a sphingosine kinase 1 (SphK1) inhibitor with IC50 of 0.1-1.8 μM. It induces prolonged mitosis followed by apoptotic cell death through the intrinsic apoptotic cascade. The sustained activation of CDK1 during prolonged mitosis, mediated by SKI-178 leads to the simultaneous phosphorylation of the prosurvival Bcl-2 family members, Bcl-2 and Bcl-xl, as well as the phosphorylation and subsequent degradation of Mcl-1.
  • In Vitro
    Apoptosis Analysis Cell Line:HL-60 cells Concentration:5 μM Incubation Time:24 hours Result:JNK activity (indicated by phosphorylation at Thr183/Tyr185) increased in a time-dependent manner starting as early as 2 hours continued to increase for at least 24 hours. There was a concomitant increase in apoptotic cell death indicated by the cleavage of caspase-7. Bcl-2 phosphorylation at Ser70 increased with time in response to SKI-178 treatment, reaching maximal levels at 8 hours, which was consistent with the timing of caspase-7 activation.
  • In Vivo
    Animal Model:MLL-AF9 mouse model (leukemic mice)Dosage:20 mg/kg Administration:Retro-orbital injection under isoflurane anesthesia; three times per week for 1 and 3 weeks Result:White blood cell (WBC) counts decreased from their initial 104 cells/μL levels and continued to decline after 3 weeks of treatment until they reached normal levels (~4×103 cells/μL).
  • Synonyms
    ——
  • Pathway
    Apoptosis
  • Target
    Apoptosis
  • Recptor
    Apoptosis|SphK1|SphK2
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    1259484-97-3
  • Formula Weight
    394.43
  • Molecular Formula
    C21H22N4O4
  • Purity
    >98% (HPLC)
  • Solubility
    DMSO:50 mg/mL?(126.77 mM;?Need ultrasonic)
  • SMILES
    O=C(C1=CC(C2=CC=C(OC)C=C2)=NN1)N/N=C(C3=CC=C(OC)C(OC)=C3)\C
  • Chemical Name
    ——

Shipping & Storage Information

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

Reference

1.Hengst JA, et al. SKI-178: A Multitargeted Inhibitor of Sphingosine Kinase and Microtubule Dynamics Demonstrating Therapeutic Efficacy in Acute Myeloid Leukemia Models. Cancer Transl Med. 2017;3(4):109-121.
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