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PH-797804

SKU: orb1306903

Description

PH-797804

Research Area

Cell Biology, Signal Transduction

Images & Validation

Key Properties

CAS Number586379-66-0
MW477.3
Purity97.90%
FormulaC22H19BrF2N2O3
SMILESCNC(=O)c1ccc(C)c(c1)-n1c(C)cc(OCc2ccc(F)cc2F)c(Br)c1=O
TargetAutophagy,p38 MAPK
SolubilityH2O:< 1 mg/mL (insoluble or slightly soluble);DMSO:89 mg/mL (186.47 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2.5 mg/mL (5.24 mM);Ethanol:7 mg/mL (14.67 mM)

Bioactivity

Target IC50
p38α:26 nM|p38β:102 nM
In Vivo
PH-797804 exhibits an IC50 value higher than 200 μM against several targets, including CDK2, ERK2, IKK1/2, IKKi, MAPKAP2/3, MKK7 (>100 μM), MNK, MSK (>164 μM), PRAK, RSK2, and TBK1. In the human monocytic U937 cell line, PH-797804 blocks the production of TNF-α and the activity of p38 kinase induced by lipopolysaccharide (LPS) with IC50 values of 5.9 and 1.1 nM, respectively. At a concentration of 1 μM, PH-797804 does not inhibit the JNK pathway (c-Jun phosphorylation) or the ERK pathway (ERK phosphorylation) in U937 cells. Additionally, in primary rat osteoclasts, PH-797804 displays a concentration-dependent inhibition of osteoclast formation induced by RANKL and M-CSF, achieving an IC50 of 3 nM.
In Vitro
PH-797804 exhibits strong anti-inflammatory activity and is effective in treating arthritis induced by streptococcal cell walls and collagen in both mice and rats. A 10-day treatment regimen significantly reduces joint inflammation and associated bone loss. In human endotoxin challenge models, PH-797804 dose- and concentration-dependently inhibits the induction of IL-6, TNF-α, and MK-2 activities by lipopolysaccharides. Oral administration of PH-797804 effectively suppresses acute inflammatory responses induced by systemic administration of endotoxin in rats and crab-eating macaques, with an ED50 of 0.07 and 0.095 mg/kg, respectively.

Storage & Handling

StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

PH 797804, PH797804, PH-797804, p38 MAPK, p38α, p38MAPK, p38β, inhibit, Inhibitor, Autophagy

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Key Properties

No computed properties available.

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Protocol Information

PH-797804 (orb1306903)

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% DMSO +
%+
% Tween 80 +
%

Available Sizes

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1 mg
$ 80.00
1 ml x 10 mM (in DMSO)
$ 140.00
5 mg
$ 140.00
10 mg
$ 190.00
25 mg
$ 310.00
50 mg
$ 470.00
100 mg
$ 710.00
500 mg
$ 1,430.00
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