PH-797804

Name: PH-797804
Brand: MedChemExpress
SKU: HY-10403
Rating: 5.0 (7 reviews)

Cat. No.: HY-10403 Pureza: 98.94%: Ficha de datos
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PH-797804 is a ATP-competitive, selective p38α/p38β inhibitor (IC₅₀=26 nM and K_i=5.8 nM for p38α; K_i=40 nM for p38β) and does not inhibit JNK2.

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PH-797804 Estructura química

No. CAS : 586379-66-0

Tamaño	Stock	Cantidad

Muestra gratis (0.1 - 0.2 mg)	Solicite ahora
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	En stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	En stock	Estimated Time of Arrival: December 31
Solid
5 mg	En stock	Estimated Time of Arrival: December 31
10 mg	En stock	Estimated Time of Arrival: December 31
25 mg	En stock	Estimated Time of Arrival: December 31
50 mg	En stock	Estimated Time of Arrival: December 31
100 mg	En stock	Estimated Time of Arrival: December 31
200 mg	En stock	Estimated Time of Arrival: December 31
500 mg	Obtener un presupuesto
1 g	Obtener un presupuesto

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Revisión del cliente

Based on 7 publication(s) in Google Scholar

Other Forms of PH-797804:

(aS)-PH-797804 Obtener un presupuesto
PH-797804 (Standard) Obtener un presupuesto

7 Publications Citing Use of MCE PH-797804

Recomendaciones destacadas

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Ver todos los productos específicos de isoformas p38 MAPK:

Ver todas las isoformas

p38 MAPK Akt1 p38α p38β MAPK13 p38δ p38γ

Actividad biológica
Pureza y Documentación
Referencias
Revisión del cliente

Descripciòn

PH-797804 is a ATP-competitive, selective p38α/p38β inhibitor (IC₅₀=26 nM and K_i=5.8 nM for p38α; K_i=40 nM for p38β) and does not inhibit JNK2.

IC₅₀ & Target

IC50: 26 nM (p38α)^[1]
Ki: 5.8 nM (p38α), 40 nM (p38β)^[2]

Cellular Effect

Cell Line	Type	Value	Description	References
Caco-2	IC₅₀	18.85 3 Compound: PH-797804	Determination of IC50 values for inhibition of SARS-CoV-2 induced cytotoxicity of Caco-2 cells after 48 hours by high content imaging 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 3 Compound: PH-797804	Toxicity against Caco-2 cells determined at 48 hours by intracellular ATP concentration using the CellTiter-Glo Luminescent Cell Viability Assay 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
Caco-2	CC₅₀	19.97 3 Compound: PH-797804	Toxicity against Caco-2 cells determined at 48 hours by intracellular ATP concentration using the CellTiter-Glo Luminescent Cell Viability Assay 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
Caco-2	CC₅₀	19.97 3 Compound: PH-797804	Toxicity against Caco-2 cells determined at 48 hours by intracellular ATP concentration using the CellTiter-Glo Luminescent Cell Viability Assay 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
Caco-2	IC₅₀	18.85 3 Compound: PH-797804	Determination of IC50 values for inhibition of SARS-CoV-2 induced cytotoxicity of Caco-2 cells after 48 hours by high content imaging 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	IC₅₀	18.85 3 Compound: PH-797804	Determination of IC50 values for inhibition of SARS-CoV-2 induced cytotoxicity of Caco-2 cells after 48 hours by high content imaging 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
PBMC	IC₅₀	15 1 Compound: (+/-)-4a	Antiinflammatory activity in human PBMC assessed as inhibition of LPS-induced TNFalpha release pretreated for 1 hr before LPS treatment measured after 18 hrs 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 1 Compound: (-)-4a, PH-797804	Antiinflammatory activity in human PBMC assessed as inhibition of LPS-induced TNFalpha release pretreated for 1 hr before LPS treatment measured after 18 hrs 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 1 Compound: (-)-4a, PH-797804	Antiinflammatory activity in human PBMC assessed as inhibition of LPS-induced TNFalpha release pretreated for 1 hr before LPS treatment measured after 18 hrs 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	15 1 Compound: (+/-)-4a	Antiinflammatory activity in human PBMC assessed as inhibition of LPS-induced TNFalpha release pretreated for 1 hr before LPS treatment measured after 18 hrs 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]
Monocyte	IC₅₀	3.4 1 Compound: 1	Antiinflammatory activity in human monocytes assessed as inhibition of LPS-induced IL1-beta production Antiinflammatory activity in human monocytes assessed as inhibition of LPS-induced IL1-beta production	[PMID: 21620699]
Monocyte	IC₅₀	3.4 1 Compound: 1	Antiinflammatory activity in human monocytes assessed as inhibition of LPS-induced TNFalpha production Antiinflammatory activity in human monocytes assessed as inhibition of LPS-induced TNFalpha production	[PMID: 21620699]
PBMC	IC₅₀	15 1 Compound: (+/-)-4a	Antiinflammatory activity in human PBMC assessed as inhibition of LPS-induced TNFalpha release pretreated for 1 hr before LPS treatment measured after 18 hrs 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 1 Compound: (-)-4a, PH-797804	Antiinflammatory activity in human PBMC assessed as inhibition of LPS-induced TNFalpha release pretreated for 1 hr before LPS treatment measured after 18 hrs 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]
U-937	IC₅₀	1.05 1 Compound: 1	Inhibition of p38alpha kinase-dependent HSP-27 phosphorylation in human U937 cells Inhibition of p38alpha kinase-dependent HSP-27 phosphorylation in human U937 cells	[PMID: 21620699]
U-937	IC₅₀	5.9 1 Compound: 1	Antiinflammatory activity in human U937 cells assessed as inhibition of LPS-induced TNFalpha production Antiinflammatory activity in human U937 cells assessed as inhibition of LPS-induced TNFalpha production	[PMID: 21620699]

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Ensayo clínico

Peso molecular

477.30

Fòrmula

C₂₂H₁₉BrF₂N₂O₃

No. CAS

586379-66-0

Appearance

Solid

Color

White to off-white

SMILES

O=C(C1=CC=C(C(N2C(C)=CC(OCC3=CC=C(C=C3F)F)=C(C2=O)Br)=C1)C)NC

Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvente y solubilidad

In Vitro:

DMSO : 50 mg/mL (104.76 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.0951 mL	10.4756 mL	20.9512 mL
5 mM	0.4190 mL	2.0951 mL	4.1902 mL
10 mM	0.2095 mL	1.0476 mL	2.0951 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Calculadora de molaridad
Calculadora de dilución

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 3 mg/mL (6.29 mM); Clear solution

This protocol yields a clear solution of ≥ 3 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (30.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (5.24 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Pureza y Documentación

Purity: 98.94%

Select Batch:

Ficha de datos (274 KB) SDS (393 KB)

COA (246 KB) LCMS (95 KB)

Instrucciones de manejo (2659 KB)

Referencias

[1]. Hope HR, et al. Anti-inflammatory properties of a novel N-phenyl pyridinone inhibitor of p38 mitogen-activated protein kinase: preclinical-to-clinical translation. J Pharmacol Exp Ther, 2009, 331(3), 882-895. [Content Brief]

[2]. Xing L, et al. Structural bioinformatics-based prediction of exceptional selectivity of p38 MAP kinase inhibitor PH-797804. Biochemistry, 2009, 48(27), 6402-6411. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.0951 mL	10.4756 mL	20.9512 mL	52.3780 mL
	5 mM	0.4190 mL	2.0951 mL	4.1902 mL	10.4756 mL
	10 mM	0.2095 mL	1.0476 mL	2.0951 mL	5.2378 mL
	15 mM	0.1397 mL	0.6984 mL	1.3967 mL	3.4919 mL
	20 mM	0.1048 mL	0.5238 mL	1.0476 mL	2.6189 mL
	25 mM	0.0838 mL	0.4190 mL	0.8380 mL	2.0951 mL
	30 mM	0.0698 mL	0.3492 mL	0.6984 mL	1.7459 mL
	40 mM	0.0524 mL	0.2619 mL	0.5238 mL	1.3094 mL
	50 mM	0.0419 mL	0.2095 mL	0.4190 mL	1.0476 mL
	60 mM	0.0349 mL	0.1746 mL	0.3492 mL	0.8730 mL
	80 mM	0.0262 mL	0.1309 mL	0.2619 mL	0.6547 mL
	100 mM	0.0210 mL	0.1048 mL	0.2095 mL	0.5238 mL

PH-797804 Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PH-797804586379-66-0PH797804PH 797804p38 MAPKAutophagyInhibitorinhibitorinhibit

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PH-797804

Revisión del cliente

Other Forms of PH-797804:

PH-797804 Related Antibodies

7 Publications Citing Use of MCE PH-797804

Recomendaciones destacadas

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Ver todos los productos específicos de isoformas p38 MAPK:

Actividad biológica

Pureza y Documentación

Referencias

Revisión del cliente

PH-797804 Related Antibodies

Calculadora de molaridad

Calculadora de dilución

Complete Stock Solution Preparation Table

PH-797804 Related Classifications

Keywords:

Productos vistos recientemente:

Revisión del cliente

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SAFETY DATA SHEET (SDS)

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