PH-797804
作者：齐岳
发布时间：2023-09-11
09:25:37
点击数：
产品名称：PH-797804
产品描述：
| 产品描述 | 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. |
| 靶点活性 | p38β:102 nM, p38α:26 nM |
| 体外活性 | PH-797804抗炎活性较强,治疗链球菌细胞壁诱导的关节炎及大小鼠胶原诱导的关节炎时,处理10天可使关节发炎和相关的骨质流失显著降低.在人类Endotoxin 挑战模型中,PH-797804剂量和浓度依赖性地抑制脂多糖诱导的 IL-6,TNF-α和MK-2活性.Endotoxin全身给药大鼠和食蟹猴可造成急性炎症反应,口服PH-797804可有效抑制该反应（ED50：0.07和0.095 mg/kg）. |
| 体内活性 | PH-797804对下述靶点的IC50高于200 μM: CDK2,ERK2,IKK1/2,IKKi,MAPKAP2/3,MKK7 (>100 μM),MNK,MSK (>164 μM),PRAK,RSK2和 TBK1。在人类单核U937细胞系中,PH-797804对脂多糖诱导的TNF-α产生和p38 激酶活性起阻断作用（IC50：5.9/1.1 nM）。作用于U937 细胞时,PH-797804（1 μM）没有抑制JNK 通路(c-Jun 磷酸化)或ERK 通路(ERK 磷酸化)。在原代大鼠骨髓细胞中,PH-797804浓度依赖性地抑制RANKL-和M-CSF诱导的破骨细胞形成（IC50：3 nM）。 |
| 激酶实验 | 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. |
| 别名 | PH797804 |
| 分子量 | 477.3 |
| 分子式 | C22H19BrF2N2O3 |
| CAS No. | 586379-66-0 |
存储
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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西安齐岳生物科技有限公司是集化学科研和定制与一体的高科技化学公司。业务范围包括化学试剂和产品的研发、生产、销售等。涉及产品为通用试剂的分销、非通用试剂的定制与研发，涵盖生物科技、化学品、中间体和化工材料等领域。
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