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PZ0188

PF-3644022 hydrate

≥98% (HPLC)

Synonym(s):

(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

Empirical Formula (Hill Notation):
C21H18N4OS · xH2O
Molecular Weight:
374.46 (anhydrous basis)
NACRES:
NA.77
PubChem Substance ID:
329823762
UNSPSC Code:
51111800
MDL number:
MFCD21363374
Assay:
≥98% (HPLC)
Form:
powder
Quality level:
100

Key Documents

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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

100

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Show Differences

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This Item
PZ0158PZ0346SML1741
PF-3644022 hydrate ≥98% (HPLC)

Sigma-Aldrich

PZ0188

PF-3644022 hydrate

PF 3845 hydrate ≥98% (HPLC)

Sigma-Aldrich

PZ0158

PF 3845 hydrate

PF-06726304 acetate ≥98% (HPLC)

Sigma-Aldrich

PZ0346

PF-06726304 acetate

TH1020 ≥95% (HPLC)

Sigma-Aldrich

SML1741

TH1020

assay

≥98% (HPLC)

assay

≥98% (HPLC)

assay

≥98% (HPLC)

assay

≥95% (HPLC)

form

powder

form

powder

form

powder

form

powder

Quality Level

100

Quality Level

100

Quality Level

100

Quality Level

100

storage temp.

2-8°C

storage temp.

2-8°C

storage temp.

room temp

storage temp.

2-8°C

solubility

DMSO: ≥15 mg/mL

solubility

DMSO: ≥45 mg/mL

solubility

DMSO: 20 mg/mL, clear

solubility

DMSO: 3 mg/mL, clear (warmed)

color

yellow to orange

color

white to tan

color

white to beige

color

white to beige

Application

PF-3644022 hydrate has been used for the inhibition of mitogen-activated protein kinase 2 (MK2) in human osteosarcoma cells (U2OS)[1] and in colorectal carcinoma cells (CT26).[2]

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.

pictograms

Exclamation mark
GHS07

signalword

Warning

hcodes

H302,H319

Hazard Classifications

Acute Tox. 4 Oral - Eye Irrit. 2

Storage Class

11 - Combustible Solids

flash_point_f

Not applicable

flash_point_c

Not applicable

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Certificates of Analysis (COA)

Lot/Batch Number
0000152507
0000152507
0000139542
0000139543
0000107080

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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
View All Related Papers

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