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PF-3644022

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Chemical Structure| 1276121-88-0 同义名 : -
CAS号 : 1276121-88-0
货号 : A633788
分子式 : C21H18N4OS
纯度 : 99%+
分子量 : 374.459
MDL号 : MFCD21363374
存储条件：

粉末 Keep in dark place,Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 40 mg/mL(106.82 mM)，配合低频超声，并水浴加热至45℃助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 Mitogen-Activated Protein Kinase Activated Protein Kinase 2 (MK2) belongs to serine-threonine kinase family and is activated directly by stress and inflammatory signal through p38MAPK phosphorylation in diverse inflammatory conditions through the Toll-like receptor signaling pathway. MK2 has been thought to be a critical factor involved in the regulation of synthesis and release of pro-inflammatory (TNF-α, IL-6 and IL-1β, etc.) proteins[3]. PF-3644022 is a potent, selective, orally active and ATP-competitive MK2 inhibitor. In the human U937 monocytic cell line or peripheral blood mononuclear cells, PF-3644022 potently inhibits TNFalpha production with similar activity (IC50 = 160 nM). PF-3644022 blocks TNFalpha and IL-6 production in LPS-stimulated human whole blood with IC50 of 1.6 and 10.3 mM, respectively.[4]. PF-3644022 increases the expression of Arg1 and decreases iNOS. Realtime PCR revealed the increased expressions of inflammation related factors (such as IL-1β, NF-κB, TNF-α, MK2) and pro-apoptotic gene (Bax). The BMS score showed a reduced motor function of the twy/twy mice. The motor function was also enhanced with the treatment of PF-3644022[5].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.67mL

0.53mL

0.27mL

13.35mL

2.67mL

1.34mL

26.71mL

5.34mL

2.67mL
参考文献

[1]Dyve Lingelem AB, Hjelseth IA, et al. Geldanamycin Enhances Retrograde Transport of Shiga Toxin in HEp-2 Cells. PLoS One. 2015 May 27;10(5):e0129214.

[2]Mourey RJ, Burnette BL, et al. A benzothiophene inhibitor of mitogen-activated protein kinase-activated protein kinase 2 inhibits tumor necrosis factor alpha production and has oral anti-inflammatory efficacy in acute and chronic models of inflammation. J Pharmacol Exp Ther. 2010 Jun;333(3):797-807.

[3]Rakesh Kumar Singh,et al. Novel Therapeutic Potential of Mitogen-Activated Protein Kinase Activated Protein Kinase 2 (MK2) in Chronic Airway Inflammatory Disorders. Curr Drug Targets. 2019. 20(4), 367-379.

[4]Mourey RJ, et al. A benzothiophene inhibitor of mitogen-activated protein kinase-activated protein kinase 2 inhibits tumor necrosis factor alpha production and has oral anti-inflammatory efficacy in acute and chronic models of inflammation. J Pharmacol Exp Ther. 2010. 333(3), 797-807.

[5]Lei Yu,et al. Role of MK2 signaling pathway mediating microglia/macrophages polarization in chronic compression injury of cervical spinal cord. Ann Palliat Med. 2021.10(2),1304-1312.