2. Immunology/Inflammation Stem Cell/Wnt Apoptosis
  3. SphK Wnt Apoptosis
  4. SKI II

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.

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SKI II Chemical Structure

SKI II Chemical Structure

CAS No. : 312636-16-1

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Based on 2 publication(s) in Google Scholar

SKI II Related Antibodies

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  • Biological Activity

  • Purity & Documentation

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Description

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[1][2].

IC50 & Target

IC50 value: 78/45 μM (SK1/2)[1][2].
In Vitro

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.

SKI II Related Antibodies

Cell Cytotoxicity Assay[1]

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.
In Vivo

Chronic SKI II (50.0 mg/kg, 3-weekly i.p. for 16 weeks) administration leads to permanent reduction of S1P concentrations in plasma in mice[3].
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.
Molecular Weight

302.78

Formula

C15H11ClN2OS
CAS No.
Appearance

Solid

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.

Solvent & Solubility
In Vitro: 

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.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.3027 mL 16.5136 mL 33.0273 mL
5 mM 0.6605 mL 3.3027 mL 6.6055 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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.

  • Protocol 1

    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.
  • Protocol 2

    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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: 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.

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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
References

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
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SKI II Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

SKI II312636-16-1SphKWntApoptosisSphingosine kinaseInhibitorinhibitorinhibit

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