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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)

Recherchez un Certificats d'analyse (COA) en saisissant le numéro de lot du produit. Les numéros de lot figurent sur l'étiquette du produit après les mots "Lot" ou "Batch".

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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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