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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
| Size | Price / USD | Stock | Quantity |
| 1 mL x 10 mM in DMSO | 69 | In Stock |
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| 2MG | 39 | In Stock |
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| 5MG | 63 | In Stock |
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| 10MG | 110 | In Stock |
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| 25MG | 215 | In Stock |
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| 50MG | 338 | In Stock |
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| 100MG | 509 | In Stock |
|
| 200MG | Get Quote | In Stock |
|
| 500MG | 1088 | In Stock |
|
| 1G | Get Quote | In Stock |
|
Biological Information
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Product NameSKI-178
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NoteResearch use only, not for human use.
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Brief DescriptionSKI-178 is a sphingosine kinase 1 (SphK1) inhibitor with IC50 of 0.1-1.8 μM.
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DescriptionSKI-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.
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In VitroApoptosis 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.
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In VivoAnimal 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).
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Synonyms——
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PathwayApoptosis
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TargetApoptosis
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RecptorApoptosis|SphK1|SphK2
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Research Area——
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Indication——
Chemical Information
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CAS Number1259484-97-3
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Formula Weight394.43
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Molecular FormulaC21H22N4O4
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Purity>98% (HPLC)
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SolubilityDMSO:50 mg/mL?(126.77 mM;?Need ultrasonic)
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SMILESO=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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Chemical Name——
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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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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