SKI II (Synonyms: SKI II, SPHK I2) |
カタログ番号GC16701
One-Click Copy Product Info
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ＳＫＩ－ＩＩは、スフィンゴシンキナーゼ（ＳＫ）活性の経口活性および合成阻害剤であり、ＩＣ５０値は、ＳＫ１およびＳＫ２についてそれぞれ７８μＭおよび４５μＭである。 SKI II は、そのリソソームおよび/またはプロテアソーム分解を誘導することにより、SK1 の不可逆的な阻害を引き起こします。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 312636-16-1
Sample solution is provided at 25 µL, 10mM.
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SKI II is an inhibitor of sphingosine kinase with IC50 value of 0.5μM[1].
SKI II is selective against SK and has no inhibition of human protein kinases ERK2, PKC-I and the lipid kinase PI3K. It is reported that SKI II is not a competitive inhibitor at the ATP-binding site of SK. SKI II also inhibits endogenous SK in intact MDA-MB-231 cells [1].
As a SK inhibitor, SKI II prevents SK from catalyzing the generation of sphingosine 1-phosphate (S1P). The blockage of S1P formation leads to inhibition of proliferation, as well as the induction of apoptosis in cancer cells. SKI II shows cytotoxicity in T-24 human bladder carcinoma cells, MCF-7 human breast adenocarcinoma cells and the subline of MCF-7 cells, MCF-7/VP, with IC50 values of 4.6μM, 1.2μM and 0.9μM, respectively [1].
References:
[1] French KJ, Schrecengost RS, Lee BD, Zhuang Y, Smith SN, Eberly JL, Yun JK, Smith CD. Discovery and evaluation of inhibitors of human sphingosine kinase. Cancer Res. 2003 Sep 15;63(18):5962-9.
| Cas No. | 312636-16-1 | SDF | |
| 同義語 | SKI II, SPHK I2 | ||
| Chemical Name | 4-[[4-(4-chlorophenyl)-1,3-thiazol-2-yl]amino]phenol | ||
| Canonical SMILES | C1=CC(=CC=C1C2=CSC(=N2)NC3=CC=C(C=C3)O)Cl | ||
| Formula | C15H11ClN2OS | M.Wt | 302.78 |
| 溶解度 | ≥ 15.15mg/mL in DMSO | Storage | Store at -20° C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 3.3027 mL | 16.5136 mL | 33.0273 mL |
| 5 mM | 660.5 μL | 3.3027 mL | 6.6055 mL |
| 10 mM | 330.3 μL | 1.6514 mL | 3.3027 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 25 reference(s) in Google Scholar.)