SKI II

Name: SKI II
Brand: MedChemExpress
SKU: HY-13822
Rating: 5.0 (8 reviews)

製品番号: HY-13822 純度: 99.25%: Data Sheet SDS COA 取扱説明書
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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.

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。

SKI II 構造式

CAS 番号 : 312636-16-1

容量	価格（税別）	在庫状況	数量
>無料サンプル (0.1 - 0.2 mg)		今すぐ申し込む
10 mg	$72	在庫あり	Estimated Time of Arrival: December 31
25 mg	$144	在庫あり	Estimated Time of Arrival: December 31
50 mg	$252	在庫あり	Estimated Time of Arrival: December 31
100 mg	$468	在庫あり	Estimated Time of Arrival: December 31
200 mg	$840	在庫あり	Estimated Time of Arrival: December 31
500 mg		お問い合わせ
1 g		お問い合わせ

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* アイテムを追加する前、数量をご選択ください

This product is a controlled substance and not for sale in your territory.

カスタマーレビュー

Based on 8 publication(s) in Google Scholar

顧客検証

SphK アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示

SphK1 SphK2

Wnt アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示

Wnt1 Wnt3 Wnt5 Wnt7 Wnt11

生物活性
純度とドキュメンテーション
参考文献
カスタマーレビュー

製品説明

IC₅₀ & Target

IC50 value: 78/45 μM (SK1/2)^[1]^[2].

Cellular Effect

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]

体外実験

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 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.

体内実験

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.

分子量

302.78

分子式

C₁₅H₁₁ClN₂OS

CAS 番号

312636-16-1

Appearance

Solid

Color

White to off-white

SMILES

OC1=CC=C(NC2=NC(C3=CC=C(Cl)C=C3)=CS2)C=C1

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

Powder	-20°C	3 years
	4°C	2 years
* The compound is unstable in solutions, freshly prepared is recommended.

溶剤 & 溶解度

体外:

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
10 mM	0.3303 mL	1.6514 mL	3.3027 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)

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

一般には略語で表示されます：C₁V₁ = C₂V₂

濃度 _（開始）

体積 _（開始）

濃度 _（終了）

体積 _（終了）

体内:

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)

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.

純度とドキュメンテーション

純度: 99.25%

Select Batch:

データシート (281 KB) SDS (392 KB)

COA (250 KB) HNMR (207 KB) LCMS (109 KB)

取扱説明書 (2659 KB)

参考文献

[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

SKI II Related Classifications

Molarity Calculator
Dilution Calculator

The molarity calculator equation

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

質量		濃度		体積		分子量 *
	=		×		×

The dilution calculator equation

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

一般には略語で表示されます：C₁V₁ = C₂V₂

濃度 _（開始）	×	体積 _（開始）	=	濃度 _（終了）	×	体積 _（終了）
	×		=		×
C1		V1		C2		V2

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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SphK アイソフォーム固有の製品をすべて表示:

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生物活性

純度とドキュメンテーション

参考文献

カスタマーレビュー

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

SKI II Related Classifications

Molarity Calculator

Dilution Calculator

The molarity calculator equation

The dilution calculator equation

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おすすめ

•関連スクリーニングライブラリ:

•関連小分子:

•関連タンパク質:

SphK アイソフォーム固有の製品をすべて表示:

Wnt アイソフォーム固有の製品をすべて表示:

生物活性

純度とドキュメンテーション

参考文献

カスタマーレビュー

SKI II 関連抗体

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

SKI II Related Classifications

Molarity Calculator

Dilution Calculator

The molarity calculator equation

The dilution calculator equation

Keywords:

最近チェックした製品:

カスタマーレビュー

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