製品番号: HY-10403

PH-797804

7 Cited Publications

カスタマーレビュー

Based on 7 publication(s) in Google Scholar

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.

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。

純度: 98.94%
CAS 番号: 586379-66-0
分子式: C₂₂H₁₉BrF₂N₂O₃
分子量:477.30

保管条件:

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

PH-797804 構造式

CAS 番号: 586379-66-0

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Amount: USD 0.00

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

生物活性
- 製品説明
- IC₅₀ & Target
- Cellular Effect
- 体外実験
- 体内実験
- 臨床実験
化学情報
Publications (7)
溶剤 & 溶解度
- 体外
- 体内
純度とドキュメンテーション
参考文献
Help & FAQs
関連分類
Bioz

生物活性

製品説明

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]

p38 MAPK アイソフォーム固有の製品をすべて表示 :

Cellular Effect

Cell Line	Type	Value	Description	References
Caco-2	CC₅₀	19.97 μM 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 μM 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
Monocyte	IC₅₀	3.4 nM 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 nM 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]
U-937	IC₅₀	1.05 nM 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 nM 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]

体外実験

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.

体内実験

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.

臨床実験

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

化学情報

CAS 番号 586379-66-0
性状 Solid
分子量 477.30
分子式 C₂₂H₁₉BrF₂N₂O₃
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
輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

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

Publications (7)

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Sci Transl Med

PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]

2018 Jul 18;10(450):eaaq1093. PMID: 30021885
Cell Death Dis

Quantitative analysis of phosphoproteome in necroptosis reveals a role of TRIM28 phosphorylation in promoting necroptosis-induced cytokine production. [Abstract]

2021 Oct 23;12(11):994. PMID: 34689152
Cell Death Dis

Necroptosis promotes cell-autonomous activation of proinflammatory cytokine gene expression. [Abstract]

2018 Apr 27;9(5):500. PMID: 29703889
Osteoarthritis Cartilage

Chondrocyte apoptosis in temporomandibular joint osteoarthritis promotes bone resorption by enhancing chemotaxis of osteoclast precursors. [Abstract]

2022 Aug;30(8):1140-1153. PMID: 35513247
J Pharmacol Exp Ther

Clinically Advanced p38 Inhibitors Suppress DUX4 Expression in Cellular and Animal Models of Facioscapulohumeral Muscular Dystrophy. [Abstract]

2019 Aug;370(2):219-230. PMID: 31189728
Oral Dis

Disturbed Glycometabolism-Induced Chondrocyte Apoptosis Contributes to TMJOA. [Abstract]

2025 Oct 27. PMID: 41146398
bioRxiv

2023 Feb 8.

溶剤 & 溶解度

体外:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

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.

モル濃度計算機

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

Mass Mass

濃度濃度

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分子量分子量

希釈計算機

濃度 _(開始) × 体積 _(開始) = 濃度 _(終了) × 体積 _(終了)

濃度 _(開始) 濃度 _(開始)

体積 _(開始) 体積 _(開始)

濃度 _(終了) 濃度 _(終了)

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体内:

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

Stock Solution Working Solution

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.

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 Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

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

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

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

データシート (274 KB)
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COA (2659 KB)
元素分析報告書 (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
取扱説明書 (2659 KB)

参考文献

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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.

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

Keywords

PH-797804

7 Cited Publications

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PH-797804

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MedChemExpress（MCE）の使用を引用している文献 PH-797804

p38 MAPK アイソフォーム固有の製品をすべて表示

生物活性

化学情報

Publications (7)

溶剤 & 溶解度

純度とドキュメンテーション

参考文献

Help & FAQs

Complete Stock Solution Preparation Table

PH-797804 関連分類

HY-10403 関連分類