SKF-86002
Based on 3 publication(s) in Google Scholar
SKF-86002 is an orally active p38 MAPK inhibitor, with anti-inflammatory, anti-arthritic and analgesic activities. SKF-86002 inhibits lipopolysaccharide (LPS)-stimulate human monocyte IL-1 and TNF-α production (IC50 = 1 μM). SKF-86002 inhibits lipoxygenase- and cyclooxygenase-mediated metabolism of arachidonic acid.
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。
- 純度: 99.91%
- CAS 番号: 72873-74-6
- 分子式: C16H12FN3S
- 分子量:297.35
-
保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
生物活性
-
化学情報
-
溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
-
Help & FAQs
-
Immunology/Inflammation Compound Library
HY-L007
-
Kinase Inhibitor Library
HY-L009
-
MAPK Compound Library
HY-L010
-
Reprogramming Compound Library
HY-L039
-
Oxygen Sensing Compound Library
HY-L045
-
Pyroptosis Compound Library
HY-L059
-
Orally Active Compound Library
HY-L061
-
Anti-Lung Cancer Compound Library
HY-L075
-
Anti-Cancer Metabolism Compound Library
HY-L083
-
Neurodegenerative Disease-related Compound Library
HY-L086
-
Anti-Obesity Compound Library
HY-L087
-
Angiogenesis-Related Compound Library
HY-L088
-
Targeted Diversity Library
HY-L099
-
Antidepressant Compound Library
HY-L108
-
Human Metabolite Library
HY-L123
-
Anti-Prostate Cancer Compound Library
HY-L124
-
Anti-Pulmonary Fibrosis Compound Library
HY-L125
-
Cancer Stem Cells Compound Library
HY-L135
-
Heterocyclic Compound Library
HY-L138
-
Pain-Related Compound Library
HY-L139
-
Serine/Threonine Kinase Inhibitor Library
HY-L164
-
Anti-Ovarian Cancer Compound Library
HY-L173
-
Bioactive Compound Library Max
HY-L181
-
MCE Bioactive Compound Library
HY-L001V
-
Bioactive Compound Library
HY-L001
-
Anti-Gastric Cancer Compound Library
HY-L184
-
Protein Kinase Compound Library
HY-L196
-
Cell Proliferation Compound Library
HY-L201
-
High-Throughput Bioactive Compound Library
HY-L205
-
Anti-Rheumatic Arthritis Compound Library
HY-L210
-
Mass Spectrometry Human Metabolite Library
HY-L215
-
Posttranslational Modification Library
HY-L226
-
Lactylation Compound Library
HY-L249
MedChemExpress（MCE）の使用を引用している文献 SKF-86002
More
生物活性
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| RBL-1 | IC50 |
10 μM
Compound: SKF-86002
|
Inhibitory concentration against 5-lipoxygenase in rat RBL-1 cells
Inhibitory concentration against 5-lipoxygenase in rat RBL-1 cells
|
[PMID: 8831759] |
SKF-86002 (10 μM; 1 hour) inhibits apoptosis induced by stress stimulation with UV irradiation (UV)[1].
?
SKF-86002 does not inhibit UV-induced apoptosis in undifferentiated HL-60 cells[1].
?
SKF-86002 (10 μM; 72 hours) prevent IL-4-induced monocyte or U937 cell CD23 surface expression and protein formation with no effect on CD23 mRNA levels[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:U937 cells
-
Concentration:10 μM
-
Incubation Time:72 hours
-
Result:Significantly reduced CD23 levels on IL-4-treated U937 cells.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:Lewis rats, with adjuvant-induced arthritis (AA)[5]
-
Dosage:10 mg/kg, 30 mg/kg, 90 mg/kg
-
Administration:Oral administration, daily, for 22 days
-
Result:Significantly decreased hindleg volumes after injection of adjuvant.
化学情報
-
CAS 番号 72873-74-6
-
性状 Solid
-
分子量 297.35
-
分子式 C16H12FN3S
-
Color Coffee
-
SMILES
FC1=CC=C(C2=C(C3=CC=NC=C3)N4C(SCC4)=N2)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 In solvent -80°C 2 years -20°C 1 year
Publications (3)
-
Journal Impact Factor
-
Most Recent
-
Sci Transl Med
Inhibition of p38α MAPK restores neuronal p38γ MAPK and ameliorates synaptic degeneration in a mouse model of DLB/PD. [Abstract]2023 May 10;15(695):eabq6089. PMID: 37163617 -
Stem Cells
β-Arrestin 2 and Epac2 Cooperatively Mediate DRD1-Stimulated Proliferation of Human Neural Stem Cells and Growth of Human Cerebral Organoids. [Abstract]2022 Sep 26;40(9):857-869. PMID: 35772103 -
J Stroke Cerebrovasc Dis
Blockage of p38MAPK in astrocytes alleviates brain damage in a mouse model of embolic stroke through the CX43/AQP4 axis. [Abstract]2024 Dec;33(12):108085. PMID: 39393507
溶剤 & 溶解度
DMSO : 33.33 mg/mL (112.09 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
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 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (8.41 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
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.
純度とドキュメンテーション
-
データシート (280 KB)
-
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
-
取扱説明書 (2659 KB)
参考文献
[1]. Frasch SC, et al. p38 mitogen-activated protein kinase-dependent and -independent intracellular signal transduction pathways leading to apoptosis in human neutrophils. J Biol Chem. 1998 Apr 3;273(14):8389-97. [Content Brief]
[2]. Griswold DE, et al. SK&F 86002: a structurally novel anti-inflammatory agent that inhibits lipoxygenase- and cyclooxygenase-mediated metabolism of arachidonic acid. Biochem Pharmacol. 1987 Oct 15;36(20):3463-70. [Content Brief]
[3]. Lee JC, et al. A protein kinase involved in the regulation of inflammatory cytokine biosynthesis. Nature. 1994;372(6508):739-746. [Content Brief]
[4]. L A Marshall, et al. Inhibitors of the p38 mitogen-activated kinase modulate IL-4 induction of low affinity IgE receptor (CD23) in human monocytes. J Immunol. 1998 Dec 1;161(11):6005-13. [Content Brief]
[5]. M J DiMartino, et al. Pharmacologic characterization of the antiinflammatory properties of a new dual inhibitor of lipoxygenase and cyclooxygenase. Agents Actions. 1987 Feb;20(1-2):113-23. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.3630 mL | 16.8152 mL | 33.6304 mL | 84.0760 mL |
| 5 mM | 0.6726 mL | 3.3630 mL | 6.7261 mL | 16.8152 mL | |
| 10 mM | 0.3363 mL | 1.6815 mL | 3.3630 mL | 8.4076 mL | |
| 15 mM | 0.2242 mL | 1.1210 mL | 2.2420 mL | 5.6051 mL | |
| 20 mM | 0.1682 mL | 0.8408 mL | 1.6815 mL | 4.2038 mL | |
| 25 mM | 0.1345 mL | 0.6726 mL | 1.3452 mL | 3.3630 mL | |
| 30 mM | 0.1121 mL | 0.5605 mL | 1.1210 mL | 2.8025 mL | |
| 40 mM | 0.0841 mL | 0.4204 mL | 0.8408 mL | 2.1019 mL | |
| 50 mM | 0.0673 mL | 0.3363 mL | 0.6726 mL | 1.6815 mL | |
| 60 mM | 0.0561 mL | 0.2803 mL | 0.5605 mL | 1.4013 mL | |
| 80 mM | 0.0420 mL | 0.2102 mL | 0.4204 mL | 1.0510 mL | |
| 100 mM | 0.0336 mL | 0.1682 mL | 0.3363 mL | 0.8408 mL |
SKF-86002 関連分類
HY-12511 関連分類
Powered by Bioz