PH-797804
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
PH-797804是一种新型的、有效的和ATP竞争性的人P38 MAP激酶的可逆性抑制剂,特异性抑制p38α,IC50值为26 nM,Ki值为5.8 nM。
PH-797804以浓度依赖的方式抑制单核细胞中LPS诱导的TNF-α和IL-1β的生成。PH-797804阻断原代大鼠骨髓细胞中RANKL和M-CSF诱导的破骨细胞的形成。
口服给药PH-797804以剂量依赖的方式抑制Lewis大鼠和猕猴中LPS诱导的TNF-α水平。此外,已有研究表明PH-797804能够抑制关节炎小鼠模型中胶原或大鼠链球菌细胞壁(SCW)提取物诱导的慢性炎症。
参考文献:
[1] Hope HR1,Anderson GD,Burnette BL,Compton RP,Devraj RV,Hirsch JL,Keith RH,Li X,Mbalaviele G,Messing DM,Saabye MJ,Schindler JF,Selness SR,Stillwell LI,Webb EG,Zhang J,Monahan JB. 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 Dec;331(3):882-95.
- 1. Maruyama, Hidekazu, et al. "Endothelin-1 alters BMP signaling to promote proliferation of pulmonary artery smooth muscle cells." Can J Physiol Pharmacol. 2022 Oct 1;100(10):1018-1027. PMID: 36037530
- 2.Zheng, Lufeng, et al. "The 3′ UTR of the pseudogene CYP4Z2P promotes tumor angiogenesis in breast cancer by acting as a ceRNA for CYP4Z1." Breast cancer research and treatment (2015): 1-14. PMID: 25701119
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 477.3 |
Cas No. | 586379-66-0 |
Formula | C22H19BrF2N2O3 |
Synonyms | PH797804;PH 797804 |
Solubility | ≥23.85 mg/mL in DMSO; insoluble in H2O; insoluble in EtOH |
Chemical Name | 3-[3-bromo-4-[(2,4-difluorophenyl)methoxy]-6-methyl-2-oxopyridin-1-yl]-N,4-dimethylbenzamide |
SDF | Download SDF |
Canonical SMILES | CC1=C(C=C(C=C1)C(=O)NC)N2C(=CC(=C(C2=O)Br)OCC3=C(C=C(C=C3)F)F)C |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
描述 | PH-797804是p38α的新型吡啶酮抑制剂,IC50值为26 nM,比对p38β的选择性高4倍。 | |||||
靶点 | p38α | |||||
IC50 | 26 nM |
质量控制和MSDS
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