Fig. 1 · Structure

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PH-797804

Cat. No. A11078 CAS 586379-66-0

p38 MAPK inhibitor

PH-797804 is a diarylpyridinone inhibitor of p38 mitogen-activated protein (MAP) kinase.

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Publications for PH-797804

1 publication citing this product

  1. Yuho Ito, .et al. , Biosci Biotechnol Biochem, 2015, 79(11):1794-801 PMID: 26057585

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Biological Activity

Bioactivity / Mechanism

In mouse mammary tumor-derived cells, PH797804 reduced MK2 and Hsp27 phosphorylation, consistent with suppression of p38-pathway signaling. [1]

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

Target & Activity

Target Activity Value
p38α (Cell-free assay) 26 nM
p38β (Cell-free assay) 102 nM

Cellular Effect

Cell Line Activity Value Description Reference
Caco-2 IC50 18.85 μM Determination of IC50 values for inhibition of SARS-CoV-2 induced cytotoxicity of Caco-2 cells after 48 hours by high content imaging 10.21203/rs.3.rs-23951/v1
Caco-2 CC50 19.97 μM Toxicity against Caco-2 cells determined at 48 hours by intracellular ATP concentration using the CellTiter-Glo Luminescent Cell Viability Assay 10.21203/rs.3.rs-23951/v1
PBMC IC50 15 nM Antiinflammatory activity in human PBMC assessed as inhibition of LPS-induced TNFalpha release pretreated for 1 hr before LPS treatment measured after 18 hrs [PMID: 21641211]
PBMC IC50 3.4 nM Antiinflammatory activity in human PBMC assessed as inhibition of LPS-induced TNFalpha release pretreated for 1 hr before LPS treatment measured after 18 hrs [PMID: 21641211]

In Vitro Studies

PH797804 (2 μM) reduced attachment of mouse mammary tumor-derived cells to uncoated and collagen-coated surfaces after overnight pretreatment. [1]

In neonatal rat astrocytes aged in vitro, prolonged PH-797804 treatment (2 μM) was associated with lower GFAP, TNFα and phospho-p38 signals after oxygen-glucose deprivation. These marker results do not establish neuronal protection. [2]

Cellular suppression of p38-pathway phosphorylation

Cell-based study · Mouse mammary tumor-derived cancer cells [1]

PH-treated cells showed lower MK2 and Hsp27 phosphorylation than DMSO controls.

Measured endpoints — not treatment concentrations
EndpointReported resultReference
MK2 and Hsp27 phosphorylationqualitative Decreased[1]

Literature-Reported Treatment Conditions

Exposure duration
24 h
Method
Cell treatment followed by immunoblotting
Vehicle
DMSO control
Reported limits
Fig. 1A concentration is not specified in the inspected methods/caption; the 2 μM, 96 h SILAC exposure is a separate design.
Methods and source locations

Compound reported in the paper: PH-797804; Compound label in the paper: PH

Results concern the material reported by the authors; no Adooq lot, stereochemical composition, or performance was tested.

Fig. 1A and caption, article p. 5 (PDF p. 6); Results, identification of proteome/phosphoproteome changes; Immunoblotting methods, p. 3

MK2 and Hsp27 phosphorylation: Immunoblotting; DMSO control; p38α knockout comparator — Fig. 1A and caption, article p. 5 (PDF p. 6); Results, identification of proteome/phosphoproteome changes; Immunoblotting methods, p. 3

Attachment to uncoated and collagen-coated surfaces

Cell-based study · Mouse mammary tumor-derived cancer cells [1]

Attachment decreased on both surfaces compared with DMSO.

Measured endpoints — not treatment concentrations
EndpointReported resultReference
Attached cells per field normalized to corresponding WT/DMSO conditionqualitative Decreased on both surfaces[1]

Literature-Reported Treatment Conditions

Treatment concentration
2 μM
Exposure duration
Overnight pretreatment, then 1 h attachment assay
Method
Compound present during pretreatment and replating; compare uncoated and collagen-coated plates
Vehicle
DMSO
Reported limits
Exact overnight duration and DMSO percentage not specified in the selected method.
Methods and source locations

Compound reported in the paper: PH-797804; Compound label in the paper: PH

Results concern the material reported by the authors; no Adooq lot, stereochemical composition, or performance was tested.

Cell Attachment Assay, article p. 2; cell-adhesion Results, p. 10; Fig. 6A and caption, p. 12 (PDF p. 13)

Attached cells per field normalized to corresponding WT/DMSO condition: Crystal-violet assay; 1 h attachment; n = 4 biological replicates — Cell Attachment Assay, article p. 2; cell-adhesion Results, p. 10; Fig. 6A and caption, p. 12 (PDF p. 13)

Astrocyte markers after oxygen-glucose deprivation

Cell-based study · Primary neonatal Wistar rat astrocytes maintained to 30 DIV as an in vitro aging model [2]

PH-treated OGD cultures showed lower GFAP, TNFα and phospho-p38 bands than untreated OGD cultures.

Measured endpoints — not treatment concentrations
EndpointReported resultReference
GFAP, TNFα and phospho-p38 protein signals after 4 h OGDqualitative Qualitatively lower with PH treatment[2]

Literature-Reported Treatment Conditions

Treatment concentration
2 μM
Exposure duration
Added at seeding and each medium change; OGD performed at 30 DIV for 4 h
Method
Prolonged culture treatment followed by OGD and immunoblotting
Reported limits
Vehicle, independent replicate count for Fig. 4C, and compound maintenance during OGD/recovery medium exchange are not explicitly specified in the inspected text.
Methods and source locations

Compound reported in the paper: PH-797804; Compound label in the paper: PH

Results concern the material reported by the authors; no Adooq lot, stereochemical composition, or performance was tested.

Materials and Methods: Astrocyte primary cultures and Oxygen-glucose deprivation; treatment Results; Fig. 4C and caption

GFAP, TNFα and phospho-p38 protein signals after 4 h OGD: Immunoblotting; normoxic and OGD cultures with and without PH; α-actinin loading control — Materials and Methods: Astrocyte primary cultures and Oxygen-glucose deprivation; treatment Results; Fig. 4C and caption

Specifications

Manufacturer Adooq Bioscience
Actions Inhibitor
CAS Number 586379-66-0
Applications p38 MAPK inhibitor
Formula C22H19BrF2N2O3
Molecular Weight 477.2
SMILES
CC1=C(C=C(C=C1)C(=O)NC)N2C(=CC(=C(C2=O)Br)OCC3=C(C=C(C=C3)F)F)C

Storage & Solubility

In Vitro Solubility

Reported Solubility

SolventReported Solubility
DMSO 84 mg/mL (175.99 mM)
Water Insoluble
Ethanol 6 mg/mL (12.57 mM)

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.

In Vivo Preparation

Concentration
4 mg/mL
Vehicle
2% DMSO+30% PEG 300+5% Tween 80+ddH2O

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] Dan Y, Radic N, Gay M, et al. Characterization of p38α Signaling Networks in Cancer Cells Using Quantitative Proteomics and Phosphoproteomics. Molecular & cellular proteomics : MCP (2023). PMID: 36894123 DOI: 10.1016/j.mcpro.2023.100527 Source material
  2. [2] Revuelta M, Elicegui A, Scheuer T, et al. In vitro P38MAPK inhibition in aged astrocytes decreases reactive astrocytes, inflammation and increases nutritive capacity after oxygen-glucose deprivation. Aging (2021). PMID: 33563843 DOI: 10.18632/aging.202651 Source material

Publications

1 publication citing this product

  1. Yuho Ito, .et al. , Biosci Biotechnol Biochem, 2015, 79(11):1794-801 PMID: 26057585

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