PZ0188
PF-3644022 水合物
≥98% (HPLC)
别名:
(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 hydrate
质量水平
方案
≥98% (HPLC)
表单
powder
颜色
yellow to orange
溶解性
DMSO: ≥15 mg/mL
储存温度
2-8°C
SMILES字符串
O.C[C@@H]1CNc2c(sc3ccc4nc(ccc4c23)-c5ccc(C)nc5)C(=O)N1
InChI
1S/C21H18N4OS.H2O/c1-11-3-4-13(10-22-11)15-6-5-14-16(25-15)7-8-17-18(14)19-20(27-17)21(26)24-12(2)9-23-19;/h3-8,10,12,23H,9H2,1-2H3,(H,24,26);1H2/t12-;/m1./s1
InChI key
WHVUIWUUCVXAGR-UTONKHPSSA-N
应用
PF-3644022 hydrate has been used for the inhibition of mitogen-activated protein kinase 2 (MK2) in human osteosarcoma cells (U2OS) and in colorectal carcinoma cells (CT26).
生化/生理作用
PF-3644022 hydrate is a MK2 inhibitor
PF-3644022 is a potent inhibitor of mitogen-activated protein kinase-activated protein kinase 2 (MK2; Ki = 3 nM). PF-3644022 inhibits TNFa and IL-6 production in LPS-stimulated human whole blood (IC50 = 1.6 and 10.3 μM, respectively) and blocks TNFα production and paw swelling in a streptococcal cell wall-induced arthritis in rats.
特点和优势
This compound is featured on the MAPKAPs page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.
其他说明
PF3644022 has been expertly reviewed and recommended by the Chemical Probes Portal. For more information, please visit the PF3644022 probe summary on the Chemical Probes Portal website.
警示用语:
Warning
危险声明
危险分类
Acute Tox. 4 Oral - Eye Irrit. 2
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
历史批次信息供参考:
分析证书(COA)
Lot/Batch Number
Oncogenic RAS signaling promotes tumor immunoresistance by stabilizing PD-L1 mRNA.
Coelho MA, et al.
Immunity, 47(6), 1083-1099 (2017)
Induction of oxidative metabolism by the p38alpha/MK2 pathway.
Trempolec N, et al.
Scientific Reports, 7(1), 11367-11367 (2017)
Natalia Ronkina et al.
Journal of immunology (Baltimore, Md. : 1950), 203(8), 2291-2300 (2019-09-19)
Tristetraprolin (TTP) is an RNA-binding protein and an essential factor of posttranscriptional repression of cytokine biosynthesis in macrophages. Its activity is temporally inhibited by LPS-induced p38MAPK/MAPKAPK2/3-mediated phosphorylation, leading to a rapid increase in cytokine expression. We compared TTP expression and
Nuria Gutierrez-Prat et al.
Proceedings of the National Academy of Sciences of the United States of America, 118(29) (2021-07-18)
Cell survival in response to stress is determined by the coordination of various signaling pathways. The kinase p38α is activated by many stresses, but the intensity and duration of the signal depends on the stimuli. How different p38α-activation dynamics may
Nicholas Van Sciver et al.
PLoS pathogens, 17(11), e1010045-e1010045 (2021-11-09)
Epstein-Barr virus (EBV) is a human herpesvirus that causes infectious mononucleosis and contributes to both B-cell and epithelial-cell malignancies. EBV-infected epithelial cell tumors, including nasopharyngeal carcinoma (NPC), are largely composed of latently infected cells, but the mechanism(s) maintaining viral latency
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