SKI II
Based on 8 publication(s) in Google Scholar
SKI-II is an oral active and synthetic inhibitor of sphingosine kinase (SK) activity, with IC50 values of 78 μM and 45 μM for SK1 and for SK2, respectively. SKI II causes an irreversible inhibition of SK1 by inducing its lysosomal and/or proteasomal degradation.
For research use only. We do not sell to patients.
- Purity: 99.25%
- CAS No.: 312636-16-1
- Formula: C15H11ClN2OS
- Molecular Weight:302.78
-
Storage:Powder -20°C, 3 years , 4°C, 2 years
* The compound is unstable in solutions, freshly prepared is recommended.
-
Biological Activity
-
Chemical Information
-
Solvent & Solubility
- Purity & Documentation
- References
-
Help & FAQs
Publications Citing Use of MedChemExpress (MCE) SKI II
More- Cancer Commun (Lond). 2025 Jul 16. [Abstract]
- Autophagy. 2025 Apr 3. [Abstract]
- Cell Commun Signal. 2024 Aug 7;22(1):391. [Abstract]
- J Virol. 2025 Jan 10:e0122024. [Abstract]
- Mol Med Rep. 2024 Jan;29(1):16. [Abstract]
- J Leukoc Biol. 2025 Aug 5;117(8):qiaf111. [Abstract]
- Cell Biol Int. 2021 Apr;45(4):775-784. [Abstract]
- bioRxiv. 2024 July 15.
Biological Activity
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
7.8 μM
Compound: 13, SKI-II
|
Cytotoxicity against human A549 cells after 72 hrs by SRB assay
Cytotoxicity against human A549 cells after 72 hrs by SRB assay
|
[PMID: 20598402] |
| HeLa | EC50 |
<1.2 μM
Compound: 12
|
Inhibition of VCP in human HeLa cells assessed as stabilization of ubiquitin-tagged luciferase after 24 hrs by reporter gene assay
Inhibition of VCP in human HeLa cells assessed as stabilization of ubiquitin-tagged luciferase after 24 hrs by reporter gene assay
|
[PMID: 20137940] |
| HeLa | IC50 |
9.1 μM
Compound: 13, SKI-II
|
Cytotoxicity against human HeLa cells after 72 hrs by SRB assay
Cytotoxicity against human HeLa cells after 72 hrs by SRB assay
|
[PMID: 20598402] |
| MCF-10A | IC50 |
14.5 μM
Compound: 13, SKI-II
|
Cytotoxicity against human MCF10A cells after 72 hrs by SRB assay
Cytotoxicity against human MCF10A cells after 72 hrs by SRB assay
|
[PMID: 20598402] |
| MDA-MB-231 | IC50 |
8.2 μM
Compound: 13, SKI-II
|
Cytotoxicity against human MDA-MB-231 cells after 72 hrs by SRB assay
Cytotoxicity against human MDA-MB-231 cells after 72 hrs by SRB assay
|
[PMID: 20598402] |
| MEF | IC50 |
8.9 μM
Compound: 13, SKI-II
|
Cytotoxicity against MEF after 72 hrs by SRB assay
Cytotoxicity against MEF after 72 hrs by SRB assay
|
[PMID: 20598402] |
| MIA PaCa-2 | IC50 |
7.7 μM
Compound: 13, SKI-II
|
Cytotoxicity against human MIAPaCa2 cells after 72 hrs by SRB assay
Cytotoxicity against human MIAPaCa2 cells after 72 hrs by SRB assay
|
[PMID: 20598402] |
| NCI-H226 | IC50 |
8.6 μM
Compound: 13, SKI-II
|
Cytotoxicity against human NCI-H226 cells after 72 hrs by SRB assay
Cytotoxicity against human NCI-H226 cells after 72 hrs by SRB assay
|
[PMID: 20598402] |
| NCI-H441 | IC50 |
8 μM
Compound: 13, SKI-II
|
Cytotoxicity against human H441 cells after 72 hrs by SRB assay
Cytotoxicity against human H441 cells after 72 hrs by SRB assay
|
[PMID: 20598402] |
| NCI-H460 | IC50 |
9.2 μM
Compound: 13, SKI-II
|
Cytotoxicity against human H460 cells after 72 hrs by SRB assay
Cytotoxicity against human H460 cells after 72 hrs by SRB assay
|
[PMID: 20598402] |
| PBL | CC50 |
>5 μM
Compound: 99; SKI II
|
Cytotoxicity in human PBL cells
Cytotoxicity in human PBL cells
|
[PMID: 33539089] |
| PC-3 | GI50 |
11 μM
Compound: 1; SKI-II
|
Antiproliferative activity against human PC3 cells after 72 hrs by MTS assay
Antiproliferative activity against human PC3 cells after 72 hrs by MTS assay
|
[PMID: 26780304] |
| U-87MG ATCC | IC50 |
10.7 μM
Compound: 13, SKI-II
|
Cytotoxicity against human U87MG cells after 72 hrs by SRB assay
Cytotoxicity against human U87MG cells after 72 hrs by SRB assay
|
[PMID: 20598402] |
SKI II inhibits cell proliferation by suppressing the Wnt/β-catenin signaling pathway. SKI II promotes the degradation of β-catenin by enhancing Wnt5A[1].
?
SKI II (1.25 μM, 48 h) in combination with DDP has a clear synergistic effect in human gastric carcinoma SGC7901/DDP cell line[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:The human gastric carcinoma SGC7901/DDP cell line.
-
Concentration:0 μM, 1.25 μM (combined with DDP).
-
Incubation Time:48 hours.
-
Result:SKI II in combination with DDP had a greater effect on the SGC-7901/DDP cells compared with DDP or SKI II alone.
? SKI II (50.0 mg/kg, IP; 100 mg/kg, PO) treatment reduces tumor growth in mice bearing solid tumor model[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:8 week-old female LDL-R-/- mice[3].
-
Dosage:50.0 mg/kg.
-
Administration:IP injection daily, 3 days a week for 16 weeks.
-
Result:A single administration of produced a significant reduction of plasma S1P with the maximum (~40%) observed 12 h after injection. At sacrifice (72 h after last injection) S1P levels were 266 ± 18 ng/mL and 328 ± 30 ng/mL in the SKI-II-treated and control groups, respectively.
-
Animal Model:BALB/c mouse solid tumor model that uses JC mammary adenocarcinoma cells[4].
-
Dosage:50.0 mg/kg.
-
Administration:IP injection daily, 3 days a week for 16 weeks.
-
Result:Had strong inhibition of tumor growth from the start of treatment of 65%, with no toxicity or weight loss.
-
Animal Model:BALB/c JC tumor model[4].
-
Dosage:100 mg/kg.
-
Administration:PO every other day.
-
Result:Caused significant antitumor activity in well-established tumors as early as day 5, with maximal response seen at the end of the study. Showed 79% inhibition of tumor growth from the start of treatment.
Chemical Information
-
CAS No. 312636-16-1
-
Appearance Solid
-
Molecular Weight 302.78
-
Formula C15H11ClN2OS
-
Color White to off-white
-
SMILES
OC1=CC=C(NC2=NC(C3=CC=C(Cl)C=C3)=CS2)C=C1
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Powder -20°C 3 years 4°C 2 years * The compound is unstable in solutions, freshly prepared is recommended.
Publications (8)
-
Journal Impact Factor
-
Most Recent
-
Cancer Commun (Lond)
Targeting SPHK1 in macrophages remodels the tumor microenvironment and enhances anti-PD-1 immunotherapy efficacy in colorectal cancer liver metastasis. [Abstract]2025 Jul 16. PMID: 40665874 -
Autophagy
Mitophagy-mediated S1P facilitates muscle adaptive responses to endurance exercise through SPHK1-S1PR1/S1PR2 in slow-twitch myofibers. [Abstract]2025 Apr 3. PMID: 40181214 -
Cell Commun Signal
Concomitant targeting of FLT3 and SPHK1 exerts synergistic cytotoxicity in FLT3-ITD+ acute myeloid leukemia by inhibiting β-catenin activity via the PP2A-GSK3β axis. [Abstract]2024 Aug 7;22(1):391. PMID: 39113090 -
J Virol
Epithelial-to-mesenchymal transition and live cell extrusion contribute to measles virus release from human airway epithelia. [Abstract]2025 Jan 10:e0122024. PMID: 39791903 -
Mol Med Rep
Notoginsenoside R1 ameliorates the inflammation induced by amyloid‑β by suppressing SphK1‑mediated NF‑κB activation in PC12 cells. [Abstract]2024 Jan;29(1):16. PMID: 38063180 -
J Leukoc Biol
Microvesicles derived from activated T cells promote human mast cell migration via the S1P1 receptor. [Abstract]2025 Aug 5;117(8):qiaf111. PMID: 40743264 -
Cell Biol Int
Bone marrow mesenchymal stem cells-derived exosomes reduce Aβ deposition and improve cognitive function recovery in mice with Alzheimer's disease by activating sphingosine kinase/sphingosine-1-phosphate signaling pathway. [Abstract]2021 Apr;45(4):775-784. PMID: 33300254 -
Solvent & Solubility
DMSO : ≥ 100 mg/mL (330.27 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.
Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.75 mg/mL (9.08 mM); Clear solution
This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.75 mg/mL (9.08 mM); Clear solution
This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * The compound is unstable in solutions, freshly prepared is recommended.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
-
Data Sheet (281 KB)
-
SDS (392 KB)
- English - EN (392 KB)
- Français - FR (392 KB)
- Deutsch - DE (392 KB)
- Norwegian - NO (392 KB)
- Español - ES (392 KB)
- Swedish - SV (392 KB)
- Italian - IT (392 KB)
- Portuguese - PT (392 KB)
-
Handling Instructions (2659 KB)
References
[1]. Liu H, et al. SphK1 inhibitor SKI II inhibits the proliferation of human hepatoma HepG2 cells via the Wnt5A/β-catenin signaling pathway. Life Sci. 2016 Apr 15;151:23-9. [Content Brief]
[2]. Potì F, et al. SKI-II--a sphingosine kinase 1 inhibitor--exacerbates atherosclerosis in low-density lipoprotein receptor-deficient (LDL-R-/-) mice on high cholesterol diet. Atherosclerosis. 2015 May;240(1):212-5. [Content Brief]
[3]. Liu Y, et al. SKI-II reverses the chemoresistance of SGC7901/DDP gastric cancer cells. Oncol Lett. 2014 Jul;8(1):367-373. [Content Brief]
[4]. French KJ, et al. Antitumor activity of sphingosine kinase inhibitors. J Pharmacol Exp Ther. 2006 Aug;318(2):596-603. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.3027 mL | 16.5136 mL | 33.0273 mL | 82.5682 mL |
| 5 mM | 0.6605 mL | 3.3027 mL | 6.6055 mL | 16.5136 mL | |
| 10 mM | 0.3303 mL | 1.6514 mL | 3.3027 mL | 8.2568 mL | |
| 15 mM | 0.2202 mL | 1.1009 mL | 2.2018 mL | 5.5045 mL | |
| 20 mM | 0.1651 mL | 0.8257 mL | 1.6514 mL | 4.1284 mL | |
| 25 mM | 0.1321 mL | 0.6605 mL | 1.3211 mL | 3.3027 mL | |
| 30 mM | 0.1101 mL | 0.5505 mL | 1.1009 mL | 2.7523 mL | |
| 40 mM | 0.0826 mL | 0.4128 mL | 0.8257 mL | 2.0642 mL | |
| 50 mM | 0.0661 mL | 0.3303 mL | 0.6605 mL | 1.6514 mL | |
| 60 mM | 0.0550 mL | 0.2752 mL | 0.5505 mL | 1.3761 mL | |
| 80 mM | 0.0413 mL | 0.2064 mL | 0.4128 mL | 1.0321 mL | |
| 100 mM | 0.0330 mL | 0.1651 mL | 0.3303 mL | 0.8257 mL |
Powered by Bioz