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Merck

PZ0188

Sigma-Aldrich

PF-3644022 hydrate

≥98% (HPLC)

Sinónimos:

(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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About This Item

Fórmula empírica (notación de Hill):
C21H18N4OS · xH2O
Peso molecular:
374.46 (anhydrous basis)
Número MDL:
Código UNSPSC:
51111800
ID de la sustancia en PubChem:
NACRES:
NA.77

Análisis

≥98% (HPLC)

formulario

powder

color

yellow to orange

solubilidad

DMSO: ≥15 mg/mL

temp. de almacenamiento

2-8°C

cadena SMILES

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

Clave InChI

WHVUIWUUCVXAGR-UTONKHPSSA-N

Aplicación

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).

Acciones bioquímicas o fisiológicas

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.

Características y beneficios

This compound is featured on the MAPKAPs page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.

Otras notas

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.

Pictogramas

Exclamation mark

Palabra de señalización

Warning

Frases de peligro

Clasificaciones de peligro

Acute Tox. 4 Oral - Eye Irrit. 2

Código de clase de almacenamiento

11 - Combustible Solids

Clase de riesgo para el agua (WGK)

WGK 3

Punto de inflamabilidad (°F)

Not applicable

Punto de inflamabilidad (°C)

Not applicable


Certificados de análisis (COA)

Busque Certificados de análisis (COA) introduciendo el número de lote del producto. Los números de lote se encuentran en la etiqueta del producto después de las palabras «Lot» o «Batch»

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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
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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