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Submit ReviewPF 3644022
说明： Potent MK2 inhibitor
化学名： (10R)-9,10,11,12-Tetrahydro-10-methyl-3-(6-methyl-3-pyridinyl)-8H-[1,4]diazepino[5',6':4,5]thieno[3,2-f]quinolin-8-one
纯度： ≥98% (HPLC)
生物活性 for PF 3644022
PF 3644022 is a potent, ATP-competitive inhibitor of mitogen-activated protein kinase (MAPK)-activated protein kinase-2 (MK2) (IC50 = 5.2 nM; Ki = 3 nM). Inhibits tumor necrosis factor α (TNFα) production in U937 monocytic cells and peripheral blood mononuclear cells (PBMCs) (IC50 = 160 nM); exhibits oral efficacy in acute and chronic inflammatory models.
许可信息
Sold for research purposes under agreement from Pfizer Inc.
External Portal Information for PF 3644022
Chemicalprobes.org is a portal that offers independent guidance on the selection and/or application of small molecules for research. The use of PF 3644022 is reviewed on the chemical probes website..
技术数据 for PF 3644022
| 分子量 | 374.46 |
| 公式 | C21H18N4OS |
| 储存 | Store at +4°C |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 1276121-88-0 |
| PubChem ID | 44631903 |
| InChI Key | CMWRPDHVGMHLSZ-GFCCVEGCSA-N |
| Smiles | O=C(N[C@H](C)CN4)C3=C4C1=C(S3)C=CC2=C1C=CC(C5=CC=C(C)N=C5)=N2 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for PF 3644022
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 14.98 | 40 |
制备储备液 for PF 3644022
以下数据基于产品分子量 374.46。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| 浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.4 mM | 6.68 mL | 33.38 mL | 66.76 mL |
| 2 mM | 1.34 mL | 6.68 mL | 13.35 mL |
| 4 mM | 0.67 mL | 3.34 mL | 6.68 mL |
| 20 mM | 0.13 mL | 0.67 mL | 1.34 mL |
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产品说明书 for PF 3644022
参考文献 for PF 3644022
参考文献是支持产品生物活性的出版物。
Mourey et al (2010) A benzothiophene inhibitor of mitogen-activated protein kinase-activated protein kinase 2 inhibits tumor necrosis factor α production and has oral anti-inflammatory efficacy in acute and chronic models of inflammation. J.Pharmacol.Exp.Ther. 333 797 PMID: 20237073
If you know of a relevant reference for PF 3644022, please let us know.
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关键词: PF 3644022, PF 3644022 supplier, PF3644022, mapk, mitogen-activated, protein, kinase-activated, kinase, 2, MK-2, MK2, potent, anti-inflammatory, inhibitors, inhibits, pfizer, 4279, Tocris Bioscience
7 篇 PF 3644022 的引用文献
引用文献是使用了 Tocris 产品的出版物。 PF 3644022 的部分引用包括：
Tang et al (2019) K63-linked ubiquitination regulates RIPK1 kinase activity to prevent cell death during embryogenesis and inflammation. Nat Commun 10 4157 PMID: 31519887
Jaco et al (2017) MK2 Phosphorylates RIPK1 to Prevent TNF-Induced Cell Death. Mol Cell 66 698 PMID: 28506461
Stephen J et al (2019) Clinically Advanced p38 Inhibitors Suppress DUX4 Expression in Cellular and Animal Models of Facioscapulohumeral Muscular Dystrophy. J Pharmacol Exp Ther 370 219-230 PMID: 31189728
Singh et al (2018) Differential effect of p38 and MK2 kinase inhibitors on the inflammatory and toxicity biomarkers in vitro. Hum Exp Toxicol 37 521 PMID: 28629242
Lingelem et al (2015) Geldanamycin Enhances Retrograde Transport of Shiga Toxin in HEp-2 Cells. PLoS One 10 e0129214 PMID: 26017782
Simon et al (2023) PRMT5-mediated regulatory arginine methylation of RIPK3. Cell Death Discov 9 14 PMID: 36658119
Bouhaddou et al (2020) The Global Phosphorylation Landscape of SARS-CoV-2 Infection Cell 182 685 PMID: 32645325
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