Catalog No.S2726

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.

Price Stock Quantity  
USD 320 In stock
USD 170 In stock
USD 320 In stock
USD 970 In stock
Bulk Inquiry

Massive Discount Available

Free Overnight Delivery on all orders over $ 500.

PH-797804 Chemical Structure

PH-797804 Chemical Structure
Molecular Weight: 477.3

Validation & Quality Control

4 customer reviews :

Quality Control & MSDS

Related Compound Libraries

p38 MAPK Inhibitors with Unique Features

  • Pan p38 MAPK Inhibitor

    SB202190 (FHPI) Pan-p38α/β inhibitor, IC50=50 nM/100 nM.

  • Most Potent p38 MAPK Inhibitor

    Skepinone-L p38α-MAPK, IC50=5 nM.

  • p38 MAPK Inhibitor in Clinical Trial

    VX-702 Phase II for Rheumatoid Arthritis.

  • Newest p38 MAPK Inhibitor

    Skepinone-L Selective p38α-MAPK inhibitor with IC50 of 5 nM.

Product Information

  • Compare p38 MAPK Inhibitors
    Compare p38 MAPK Products
  • Research Area
  • PH-797804 Mechanism

Product Description

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)
IC50 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]
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(Only for Reference)

Kinase Assay: [1]

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 Assay: [1]

Cell lines Rheumatoid arthritis synovial fibroblast(s)
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.

Animal Study: [1]

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

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)
Body Surface Area (m2)0.0070.0250.
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)


[1] Hope HR, et al, J Pharmacol Exp Ther, 2009, 331(3), 882-895.

[2] Xing L, et al. Biochemistry, 2009, 48(27), 6402-6411.

Clinical Trial Information( data from, updated on 2016-07-30)

NCT Number Recruitment Conditions Sponsor
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

view more

Chemical Information

Download PH-797804 SDF
Molecular Weight (MW) 477.3


CAS No. 586379-66-0
Storage 3 years -20℃powder
2 years -80℃in solvent
Synonyms N/A
Solubility (25°C) * In vitro DMSO 96 mg/mL (201.13 mM)
Ethanol 7 mg/mL (14.66 mM)
Water <1 mg/mL (<1 mM)
In vivo 2% DMSO+30% PEG 300+5% Tween 80+ddH2O 5mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* 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 Name 3-(4-(2,4-difluorobenzyloxy)-3-bromo-6-methyl-2-oxopyridin-1(2H)-yl)-N,4-dimethylbenzamide

Tech Support

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.

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

* Indicates a Required Field

Related p38 MAPK Products

  • Pexmetinib (ARRY-614)

    Pexmetinib (ARRY-614) is a potent, orally bioavailable, dual p38 MAPK/Tie-2 inhibitor with IC50 of 4 nM/18 nM in a HEK-293 cell line. Phase 1.

  • SB239063

    SB239063 is a potent and selective p38 MAPKα/β inhibitor with IC50 of 44 nM, showing no activity against the γ- and δ-kinase isoforms.

  • GDC-0994

    GDC-0994 is a potent, orally available ERK1/2 inhibitor with IC50 of 1.1 nM and 0.3 nM, respectively. Phase 1.

  • SB203580

    SB203580 is a p38 MAPK inhibitor with IC50 of 0.3-0.5 μM in THP-1 cells, 10-fold less sensitive to SAPK3(106T) and SAPK4(106T) and blocks PKB phosphorylation with IC50 of 3-5 μM.

    Features:First reported p38 inhibitor.

  • BIRB 796 (Doramapimod)

    BIRB 796 (Doramapimod) is a pan-p38 MAPK inhibitor with IC50 of 38 nM, 65 nM, 200 nM and 520 nM for p38α/β/γ/δ in cell-free assays, and binds p38α with Kd of 0.1 nM in THP-1 cells, 330-fold greater selectivity versus JNK2, weak inhibition for c-RAF, Fyn and Lck, insignificant inhibition of ERK-1, SYK, IKK2.

    Features:The first p38 MAPK inhibitor to be tested in a phase III clinical trial.

  • SB202190 (FHPI)

    SB202190 (FHPI) is a potent p38 MAPK inhibitor targeting p38α/β with IC50 of 50 nM/100 nM in cell-free assays, sometimes used instead of SB 203580 to investigate potential roles for SAPK2a/p38 in vivo.

  • LY2228820

    LY2228820 is a novel and potent inhibitor of p38 MAPK with IC50 of 7 nM in a cell-free assay, does not alter p38 MAPK activation. Phase 1/2.

  • Losmapimod (GW856553X)

    Losmapimod (GW856553X) is a selective, potent, and orally active p38 MAPK inhibitor with pKi of 8.1 and 7.6 for p38α and p38β, respectively. Phase 3.

  • VX-702

    VX-702 is a highly selective inhibitor of p38α MAPK, 14-fold higher potency against the p38α versus p38β. Phase 2.

    Features:Highly selective, orally active inhibitor of p38 MAPK.

  • TAK-715

    TAK-715 is a p38 MAPK inhibitor for p38α with IC50 of 7.1 nM, 28-fold more selective for p38α over p38β, no inhibition to p38γ/δ, JNK1, ERK1, IKKβ, MEKK1 or TAK1. Phase 2.

Recently Viewed Items

Tags: buy PH-797804 | PH-797804 supplier | purchase PH-797804 | PH-797804 cost | PH-797804 manufacturer | order PH-797804 | PH-797804 distributor
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Contact Us