PH-797804
作者：齊岳
發(fā)布時間：2023-09-11
09:25:37
點擊數(shù)：
產(chǎn)品名稱：PH-797804
產(chǎn)品描述：
| 產(chǎn)品描述 | PH-797804 is a pyridinone inhibitor of p38α (IC50: 26 nM, in a cell-free assay); 4-fold more selective versus p38β and does not inhibit JNK2. |
| 靶點活性 | p38β:102 nM, p38α:26 nM |
| 體外活性 | PH-797804抗炎活性較強,**鏈球菌細胞壁誘導(dǎo)的關(guān)節(jié)炎及大小鼠膠原誘導(dǎo)的關(guān)節(jié)炎時,處理10天可使關(guān)節(jié)發(fā)炎和相關(guān)的骨質(zhì)流失顯著降低.在人類Endotoxin 挑戰(zhàn)模型中,PH-797804劑量和濃度依賴性地抑制脂多糖誘導(dǎo)的 IL-6,TNF-α和MK-2活性.Endotoxin全身給藥大鼠和食蟹猴可造成急性炎癥反應(yīng),口服PH-797804可有效抑制該反應(yīng)（ED50：0.07和0.095 mg/kg）. |
| 體內(nèi)活性 | PH-797804對下述靶點的IC50高于200 μM: CDK2,ERK2,IKK1/2,IKKi,MAPKAP2/3,MKK7 (>100 μM),MNK,MSK (>164 μM),PRAK,RSK2和 TBK1。在人類單核U937細胞系中,PH-797804對脂多糖誘導(dǎo)的TNF-α產(chǎn)生和p38 激酶活性起阻斷作用（IC50：5.9/1.1 nM）。作用于U937 細胞時,PH-797804（1 μM）沒有抑制JNK 通路(c-Jun 磷酸化)或ERK 通路(ERK 磷酸化)。在原代大鼠骨髓細胞中,PH-797804濃度依賴性地抑制RANKL-和M-CSF誘導(dǎo)的破骨細胞形成（IC50：3 nM）。 |
| 激酶實驗 | 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. |
| 別名 | PH797804 |
| 分子量 | 477.3 |
| 分子式 | C22H19BrF2N2O3 |
| CAS No. | 586379-66-0 |
存儲
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
H2O: <1 mg/mL
DMSO: 89 mg/mL (186.5 mM)
Ethanol: 7 mg/mL (14.66 mM)
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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