Fig. 1 · Structure

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SKF 86002 Dihydrochloride

Cat. No. A11101 CAS 116339-68-5

p38 MAPK inhibitor

SKF 86002 Dihydrochloride is inhibitor of p38 MAP kinase (IC50 = 0.1 - 1 uM). Potently inhibits LPS-induced IL-1 and TNF-α production in human monocytes (IC50 = 1 uM).

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In Vitro Studies

In BV-2 microglia stimulated with S1, SKF 86002 at 1 µM reduced TNF-α production by ~ 47.9% compared with S1 alone. In kinase testing using ATF-2 as substrate and DMSO as control, SKF 86002 had no effect on the γ and δ isoforms. [1,2]

Literature-reported observations and conditions; not Adooq-tested protocols or general treatment recommendations.

Reduced TNF-α production in stimulated microglia

Cell-based study · BV-2 microglia [1]

BV-2 microglia were pre-treated with SKF 86002 at 1 µM before stimulation with S1 at 100 ng/ml. TNF-α production was reduced by ~ 47.9% compared with S1 alone.

Measured endpoints — not treatment concentrations
EndpointReported resultReference
TNF-α productionTNF-α production ~ 47.9%[1]

Literature-Reported Treatment Conditions

Treatment concentration
1 µM
Exposure duration
60 min prior to stimulation with S1 (100 ng/ml) for a further 24-h period
Method
pre-treating
Co-treatment
Other interventions in this design: S1 100 ng/ml. Compound effect isolated by the comparison: compared with S1 alone.
Reported limits
Not stated in the sentences used: vehicle.
Methods and source locations

Compound reported in the paper: SKF 86002

The paper names SKF 86002 without stating the salt or form; not verified as the dihydrochloride form supplied as A11101. No dose conversion or lot validation.

Materials and Methods > Effects of BAY11-7082, CRID3 and SKF 86002 on S1-Induced Neuroinflammation (S43); Results > S1 Activated p38 MAP Kinase in BV-2 Microglia (S130)

TNF-α production: TNF-α production; comparator: S1 alone — Results > S1 Activated p38 MAP Kinase in BV-2 Microglia (S130)

No Effect Reported on γ and δ Isoforms

Cell-based study · p38γ [2]

In the p38γ model, the inhibitor was added before the ATF-2 substrate, with DMSO as the control. No effect on the γ and δ isoforms was reported.

Measured endpoints — not treatment concentrations
EndpointReported resultReference
Levels of phosphorylated ATF-2Reported result no effect on the γ and δ isoforms[2]

Literature-Reported Treatment Conditions

Exposure duration
30 min at 37°C
Method
Before adding the ATF-2 protein as a substrate to the kinase reaction the inhibitors or DMSO (control) were added.
Vehicle
DMSO
Reported limits
Not stated in the sentences used: dose.
Methods and source locations

Compound reported in the paper: SKF 86002

The paper names SKF 86002 without stating the salt or form; not verified as the dihydrochloride form supplied as A11101. No dose conversion or lot validation.

Materials and Methods > In Vitro p38 and JNK Kinase Assay and Western Blot Analysis of Flag-tagged Protein (S102, S103); Results > The Effect of p38 Inhibitors SB203580 and SKF86002 on the Various p38 Isoforms Expressed in α2-Transfected Saos-2 Cells (S197, S200); Figure 7 legend (S251, S255, S256)

Levels of phosphorylated ATF-2: Levels of phosphorylated ATF-2; comparator: DMSO (control) — Results > The Effect of p38 Inhibitors SB203580 and SKF86002 on the Various p38 Isoforms Expressed in α2-Transfected Saos-2 Cells (S200); Figure 7 legend (S256)

Specifications

Manufacturer Adooq Bioscience
Actions Inhibitor
CAS Number 116339-68-5
Applications p38 MAPK inhibitor
Formula C16H12FN3S.2HCl
Molecular Weight 370.27
SMILES
C1CSC2=NC(=C(N21)C3=CC=NC=C3)C4=CC=C(C=C4)F.Cl.Cl

Storage & Solubility

In Vitro Solubility

Reported Solubility

No reported solubility data are available for this product.

Preparing Stock Solutions

Stock preparation is unavailable for this product molecular weight.

Calculated stock concentrations do not establish solvent solubility. Refer to the reported solubility data for experimental guidance.

Storage

Store powder at -20°C, keep desiccated.
In powder form, the chemical is stable for 36 months.
In solution, store at -20°C and use within 1 month to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.

Research References

  1. [1] Olajide OA, Iwuanyanwu VU, Adegbola OD, et al. SARS-CoV-2 Spike Glycoprotein S1 Induces Neuroinflammation in BV-2 Microglia. Mol Neurobiol (2022). PMID: 34709564 DOI: 10.1007/s12035-021-02593-6 Source material
  2. [2] Ivaska J, Reunanen H, Westermarck J, et al. Integrin alpha2beta1 mediates isoform-specific activation of p38 and upregulation of collagen gene transcription by a mechanism involving the alpha2 cytoplasmic tail. J Cell Biol (1999). PMID: 10525544 DOI: 10.1083/jcb.147.2.401 Source material

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