Cat. No.: HY-12511

SKF-86002

3 Cited Publications

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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.

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Pureté: 99.91%
CAS No.: 72873-74-6
Formule: C₁₆H₁₂FN₃S
Masse moléculaire:297.35

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

SKF-86002 Chemical Structure

CAS No.: 72873-74-6

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Activité biologique
- Description
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (3)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

Voir tous les produits spécifiques à Isoform p38 MAPK :

Cellular Effect

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]

In Vitro

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.

Western Blot Analysis^[4]

Cell Line:

U937 cells
Concentration:

10 μM
Incubation Time:

72 hours
Result:

Significantly reduced CD23 levels on IL-4-treated U937 cells.

In Vivo

SKF-86002 (10-90 mg/kg; p.o.; daily; for 22 days) has antiarthritic activity^[5].

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.

Chemical Information

CAS No. 72873-74-6
Appearance Solid
Masse moléculaire 297.35
Formule C₁₆H₁₂FN₃S
Color Coffee
SMILES

FC1=CC=C(C2=C(C3=CC=NC=C3)N4C(SCC4)=N2)C=C1
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (3)

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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

Solvant et solubilité

In Vitro:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

3.3630 mL

16.8152 mL

33.6304 mL

5 mM

0.6726 mL

3.3630 mL

6.7261 mL

10 mM

0.3363 mL

1.6815 mL

3.3630 mL

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.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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 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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (8.41 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during 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

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

SKF-86002

3 Cited Publications

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SKF-86002

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

MAPK Compound Library

Reprogramming Compound Library

Oxygen Sensing Compound Library

Pyroptosis Compound Library

Orally Active Compound Library

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Protein Kinase Compound Library

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Anti-Rheumatic Arthritis Compound Library

Mass Spectrometry Human Metabolite Library

Posttranslational Modification Library

Lactylation Compound Library

Publications Citing Use of MedChemExpress (MCE) SKF-86002

Voir tous les produits spécifiques à Isoform p38 MAPK

Activité biologique

Chemical Information

Publications (3)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

SKF-86002 Related Classifications

HY-12511 Related Classifications