PH-797804

Catalog No.S2726

PH-797804 Chemical Structure

Molecular Weight(MW): 477.3

PH-797804 is a novel pyridinone inhibitor of p38α with IC50 of 26 nM in a cell-free assay; 4-fold more selective versus p38β and does not inhibit JNK2. Phase 2.

Size Price Stock Quantity  
In DMSO USD 320 In stock
USD 170 In stock
USD 320 In stock
USD 970 In stock
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5 Customer Reviews

  • Human perforated disk cells were pretreated with specific pathway inhibitors, BAY11-7082 (NF-jF inhibitor) and PH797804 (p38 inhibitor), atdifferent concentrations (1, 10 ng/ml) for 1 h and then incubated with IL-1b for 48 h. (B) VEGFAexpression was quantified and analyzed; (C) Ang-1 expression; (D) TSP-1 expression; (E) ChM-1 expression. Expression levels were uniformly set to a valueof 1 in PBS group. Data are presented as mean±SEM (n = 3) and analyzed by one-way ANOVA test. *P < 0.05 as compared with IL-1b-induced group.

    J Oral Pathol Med, 2016, 45(8):605-12.. PH-797804 purchased from Selleck.

    Effect of MEK inhibitor PH-797804 in A549 cells. A549 cells were incubated with increasing concentrations of PH-797804 for 2 h. The cell lysates were harvested and phosphorylation of indicated proteins was determined by Western blotting.

    Dr.Wang from Southern Medical Hospital . PH-797804 purchased from Selleck.

  • PH-797804 purchased from Selleck.

    PH-797804 purchased from Selleck.

  • PH-797804 purchased from Selleck.

Purity & Quality Control

Choose Selective p38 MAPK Inhibitors

Biological Activity

Description PH-797804 is a novel pyridinone inhibitor of p38α with IC50 of 26 nM in a cell-free assay; 4-fold more selective versus p38β and does not inhibit JNK2. Phase 2.
Targets
p38α [1]
(Cell-free assay)
p38β [1]
(Cell-free assay)
26 nM 102 nM
In vitro

PH-797804 blocks LPS-induced TNF-α production and p38 kinase activity in the human monocytic U937 cell line, with comparable IC50 of 5.9 nM and 1.1 nM. PH-797804 has no inhibitory effect on either the JNK pathway (c-Jun phosphorylation) or ERK pathway (ERK phosphorylation) in U937 cells at concentrations up to 1 μM. PH-797804 inhibits RANKL- and M-CSF-induced osteoclast formation in a concentration-dependent manner, with IC50 of 3 nM in primary rat bone marrow cells. [1] IC50 values for PH-797804 against the following targets have been determined to be greater than 200 μM (unless specified): CDK2, ERK2, IKK1, IKK2, IKKi, MAPKAP2, MAPKAP3, MKK7 (>100 μM), MNK, MSK (>164 μM), PRAK, RSK2, and TBK1, which means the activity of PH-797804 is specific. [2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human U937 cells MYTGeY5kfGmxbjDhd5NigQ>? M3\kT2lvcGmkaYTpc44hd2ZicEO4ZYxxcGFia3nuZZNmNWSncHXu[IVvfCCKU2CtNlcheGixc4Doc5J6dGG2aX;uJIlvKGi3bXHuJHU6OzdiY3XscJMtKEmFNUC9NE4xODFyNTFOwG0> Mk\hNlE3OjB4OUm=
human monocytes MVTGeY5kfGmxbjDhd5NigQ>? NI\YbmdCdnSraX7mcIFudWG2b4L5JIFkfGm4aYT5JIlvKGi3bXHuJI1wdm:leYTld{Bie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJGxRWy2rbnT1Z4VlKFSQRnHsdIhiKHC{b3T1Z5Rqd25uIFnDOVA:OC5yMEO0JO69VQ>? NVrrUlJSOjF4MkC2PVk>
human PBMC NUjkWog3TnWwY4Tpc44h[XO|YYm= MULBcpRqcW6obHHtcYF1d3K7IHHjeIl3cXS7IHnuJIh2dWGwIGDCUWMh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBNWFNvaX7keYNm\CCWTl\hcJBp[SC{ZXzlZZNmKHC{ZYTy[YF1\WRiZn;yJFEhcHJiYnXmc5JmKEySUzD0doVifG2nboSgcYVie3W{ZXSgZYZ1\XJiMUigbJJ{NCCLQ{WwQVAvODF3IN88US=> NH;OOoozOTZ2MUKxNS=>

... Click to View More Cell Line Experimental Data

In vivo Orally dosing of PH-797804 effectively inhibits acute inflammatory responses induced by systemically administered endotoxin in both rat and cynomolgus monkeys. PH-797804 treatment for 10 days demonstrates robust anti-inflammatory activity in chronic disease models, significantly reducing both joint inflammation and associated bone loss in streptococcal cell wall-induced arthritis in rats and mouse collagen-induced arthritis. Dose-response analysis resulted in ED50 values of 0.07 mg/kg and 0.095 mg/kg in rat and cynomolgus monkeys, respectively. PH-797804 inhibits LPS-induced TNF-α, IL-6, and MK-2 activity in a dose- and concentration-dependent manner in a human endotoxin challenge model. [1]

Protocol

Kinase Assay:

[1]

+ Expand

P38 kinase assay:

A resin capture assay method is used to determine the phosphorylation of epidermal growth factor receptor peptide (EGFRP) or GST-c-Jun by p38 kinases. Reactions mixtures contain 25 mM HEPES, pH 7.5, 10 mM magnesium acetate, ATP (at the indicated concentration), 0.05 to 0.3 μCi of [γ-33P]ATP, 0.8 mM dithiothreitol, and either 200 μM EGFRP or 10 μM GST-c-Jun for p38α kinase reactions. The reaction is initiated by the addition of 25 nM p38α kinase to give a final volume of 50 μl. The p38αkinase reactions are incubated at 25 °C for 30 minutes. Under these conditions, the formation of product for both p38αkinase is linear with time. The reaction is stopped, and the unreacted [γ-33P]ATP is removed by the addition of 150 μl of AG 1 × 8 ion exchange resin in 900 mM sodium formate, pH 3.0. Once thoroughly mixed, solutions are allowed to stand for 5 minutes. A 50-μl aliquot of head volume containing the phosphorylated substrate is removed from the mixture and transferred to a 96-well plate. MicroScint-40 scintillation cocktail (150 μL) is added to each well and the radioactivity quantities using a TopCount NXT microplate scintillation and luminescence counter.
Cell Research:

[1]

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  • Cell lines: Rheumatoid arthritis synovial fibroblast(s)
  • Concentrations: --
  • Incubation Time: --
  • Method:

    Cell viability is evaluated using the 3-(4,5-dimethylthiazol-2-yl)-) diphenyl tetrazolium bromide assay. Absorbance is measured on an ELISA plate reader with a test wavelength of 570 nm and a reference of 630 nm.


    (Only for Reference)
Animal Research:

[1]

+ Expand
  • Animal Models: LPS-induced chronic inflammation rat model
  • Formulation: PH-797804 is prepared as a suspension in a vehicle consisting of 0.5% methylcellulose and 0.025% Tween 20.
  • Dosages: 0.001-1 mg/kg
  • Administration: Oral gavage 4 hours before LPS administration
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 96 mg/mL (201.13 mM)
Ethanol 7 mg/mL (14.66 mM)
Water Insoluble
In vivo Add solvents individually and in order:
2% DMSO+30% PEG 300+5% Tween 80+ddH2O
5mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 477.3
Formula

C22H19BrF2N2O3

CAS No. 586379-66-0
Storage powder
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01924650 Withdrawn Healthy Pfizer March 2014 Phase 1
NCT01862887 Completed Healthy Pfizer April 2013 Phase 1
NCT01589614 Completed Healthy Pfizer June 2012 Phase 1
NCT01543919 Completed Pulmonary Disease, Chronic Obstructive Pfizer April 2012 Phase 2
NCT01479647 Completed Healthy Volunteers Pfizer December 2011 Phase 1
NCT01321463 Completed Pulmonary Disease, Chronic Obstructive Pfizer May 2011 Phase 2

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID