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PZ0185

Sigma-Aldrich

PF-431396 hydrate

≥98% (HPLC)

Synonyme(s) :

N-[2-[[[2-[(2,3-dihydro-2-oxo-1H-indol-5-yl)amino]-5-(trifluoromethyl)-4-pyrimidinyl]amino]methyl]phenyl]-N-methyl-Methanesulfonamide hydrate

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About This Item

Formule empirique (notation de Hill):
C22H21F3N6O3S · xH2O
Numéro CAS:
717906-29-1
Poids moléculaire :
506.50 (anhydrous basis)
Numéro MDL:
MFCD21608515
Code UNSPSC :
12352200
ID de substance PubChem :
329823759
Nomenclature NACRES :
NA.77

Pureté

≥98% (HPLC)

Forme

powder

Couleur

off-white to blue-gray

Solubilité

DMSO: ≥10 mg/mL

Température de stockage

2-8°C

Chaîne SMILES 

O.CN(c1ccccc1CNc2nc(Nc3ccc4NC(=O)Cc4c3)ncc2C(F)(F)F)S(C)(=O)=O

InChI

1S/C22H21F3N6O3S.H2O/c1-31(35(2,33)34)18-6-4-3-5-13(18)11-26-20-16(22(23,24)25)12-27-21(30-20)28-15-7-8-17-14(9-15)10-19(32)29-17;/h3-9,12H,10-11H2,1-2H3,(H,29,32)(H2,26,27,28,30);1H2

Clé InChI

XSXCARUUZVMRGX-UHFFFAOYSA-N

Catégories apparentées

Application

PF-431396 hydrate has been used as a dual inhibitor of proline-rich tyrosine kinase 2 (PYK2) / focal adhesion kinase (FAK) inhibitor to study its effects on phosphorylation of Yes-associated protein (YAP) at Ser127 and steady state of transcriptional coactivator with PDZ-binding motif (TAZ) . It has also been used as a PYK2/FAK inhibitor to study its effects on protein kinase A activation in human sperm samples .

Actions biochimiques/physiologiques

PF-431396 is a potent inhibitor of PYK2 and FAK kinases (IC50 = 11 and 1.5 nM, respectively). PF-431396 increases bone formation and protects against bone loss in ovariectomized rats.

Caractéristiques et avantages

This compound is a featured product for Kinase Phosphatase Biology research. Click here to discover more featured Kinase Phosphatase Biology products. Learn more about bioactive small molecules for other areas of research at sigma.com/discover-bsm.

Pictogrammes

Skull and crossbones
GHS06

Mention d'avertissement

Danger

Mentions de danger

H301,H319

Classification des risques

Acute Tox. 3 Oral - Eye Irrit. 2

Code de la classe de stockage

6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects

Classe de danger pour l'eau (WGK)

WGK 3

Point d'éclair (°F)

Not applicable

Point d'éclair (°C)

Not applicable

Certificats d'analyse (COA)

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Consulter la Bibliothèque de documents

Zhen Liu et al.
Neuroreport, 31(10), 754-761 (2020-05-27)
The aim of this study was to investigate the effects of histone deacetylase-6 (HDAC6) on the functional and pathological changes of the amyloid beta (Aβ)-induced cognitive dysfunction rats by regulating protein tyrosine kinase 2 beta (PTK2B). Ninety Sprague Dawley rats
Seyedeh Fatemeh Razavipour et al.
Nature communications, 15(1), 5152-5152 (2024-06-18)
In many cancers, a stem-like cell subpopulation mediates tumor initiation, dissemination and drug resistance. Here, we report that cancer stem cell (CSC) abundance is transcriptionally regulated by C-terminally phosphorylated p27 (p27pT157pT198). Mechanistically, this arises through p27 co-recruitment with STAT3/CBP to
Jialie Luo et al.
Immunity, 56(7), 1533-1547 (2023-06-25)
The crosstalk between the immune and neuroendocrine systems is critical for intestinal homeostasis and gut-brain communications. However, it remains unclear how immune cells participate in gut sensation of hormones and neurotransmitters release in response to environmental cues, such as self-lipids
Evidence for the involvement of proline-rich tyrosine kinase 2 in tyrosine phosphorylation downstream of protein kinase A activation during human sperm capacitation
Battistone M A, et al.
Molecular Human Reproduction, 20(11), 1054-1066 (2014)
PYK2 negatively regulates the Hippo pathway in TNBC by stabilizing TAZ protein
Kedan A, et al.
Cell Death & Disease, 9(10), 1-15 (2018)
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Articles

Focal Adhesion Kinase (FAK) Overview

The focal adhesion kinase (FAK) is a cytoplasmic protein tyrosine kinase. FAK has been implicated as a downstream signaling molecule that functions in the control of several integrin-regulated biological processes.

Discover Bioactive Small Molecules for Kinase Phosphatase Biology

Discover Bioactive Small Molecules for Kinase Phosphatase Biology

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