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
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关于此项目
经验公式（希尔记法）:
C21H18N4OS · xH2O
分子量:
374.46 (anhydrous basis)
NACRES:
NA.77
PubChem Substance ID:
UNSPSC Code:
51111800
MDL number:
InChI key
WHVUIWUUCVXAGR-UTONKHPSSA-N
SMILES string
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
assay
≥98% (HPLC)
form
powder
color
yellow to orange
solubility
DMSO: ≥15 mg/mL
storage temp.
2-8°C
Quality Level
Application
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).
Biochem/physiol Actions
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.
Features and Benefits
This compound is featured on the MAPKAPs page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.
Other Notes
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.
signalword
Warning
hcodes
Hazard Classifications
Acute Tox. 4 Oral - Eye Irrit. 2
存储类别
11 - Combustible Solids
flash_point_f
Not applicable
flash_point_c
Not applicable
Induction of oxidative metabolism by the p38alpha/MK2 pathway.
Trempolec N, et al.
Scientific Reports, 7(1), 11367-11367 (2017)
Oncogenic RAS signaling promotes tumor immunoresistance by stabilizing PD-L1 mRNA.
Coelho MA, et al.
Immunity, 47(6), 1083-1099 (2017)
Philipp Trulley et al.
Cell reports, 27(10), 2859-2870 (2019-06-06)
Alternative translation is an important mechanism of post-transcriptional gene regulation leading to the expression of different protein isoforms originating from the same mRNA. Here, we describe an abundant long isoform of the stress/p38MAPK-activated protein kinase MK2. This isoform is constitutively
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
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