1. Immunology/Inflammation
    Apoptosis
  2. SPHK
    Apoptosis
  3. SKI-178

SKI-178 

Cat. No.: HY-12892
Handling Instructions

SKI-178 is a potent sphingosine kinase-1 (SphK1) and SphK2 inhibitor. SKI-178 is cytotoxic at IC50 concentrations ranging from 1.8 to 0.1 μM in both drug sensitive and multi-drug resistant cancer cell lines (i.e., MTR3, NCI-ADR and HL60/VCR cells). SKI-178 induces apoptosis in a CDK1-dependent manner in human acute myeloid leukemia cell lines.

For research use only. We do not sell to patients.

SKI-178 Chemical Structure

SKI-178 Chemical Structure

CAS No. : 1259484-97-3

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Description

SKI-178 is a potent sphingosine kinase-1 (SphK1) and SphK2 inhibitor. SKI-178 is cytotoxic at IC50 concentrations ranging from 1.8 to 0.1 μM in both drug sensitive and multi-drug resistant cancer cell lines (i.e., MTR3, NCI-ADR and HL60/VCR cells). SKI-178 induces apoptosis in a CDK1-dependent manner in human acute myeloid leukemia cell lines[1][2].

In Vitro

SKI-178 (5 μM; 24 hours)-induced apoptotic cell death correlates with prolonged Bcl-2 phosphorylation[1].

Apoptosis Analysis[1]

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

SKI-178 (20 mg/kg; retro-orbital injection under isoflurane anesthesia) inhibits leukemic progression in the MLL-AF9 model[3].

Animal Model: MLL-AF9 mouse model (leukemic mice)[3]
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).
Molecular Weight

394.42

Formula

C₂₁H₂₂N₄O₄

CAS No.

1259484-97-3

SMILES

O=C(C1=CC(C2=CC=C(OC)C=C2)=NN1)N/N=C(C3=CC=C(OC)C(OC)=C3)\C

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Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

SKI-178SKI178SKI 178SPHKApoptosisSphingosine kinasecytotoxicdrugsensitivemulti-drugresistantcancercellmyeloidleukemiaInhibitorinhibitorinhibit

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