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PZ0185

Sigma-Aldrich

PF-431396 hydrate

≥98% (HPLC)

Sinónimos:

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

Fórmula empírica (notación de Hill):
C22H21F3N6O3S · xH2O
Número de CAS:
717906-29-1
Peso molecular:
506.50 (anhydrous basis)
MDL number:
MFCD21608515
UNSPSC Code:
12352200
PubChem Substance ID:
329823759
NACRES:
NA.77

assay

≥98% (HPLC)

form

powder

color

off-white to blue-gray

solubility

DMSO: ≥10 mg/mL

storage temp.

2-8°C

SMILES string

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

InChI key

XSXCARUUZVMRGX-UHFFFAOYSA-N

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 .

Biochem/physiol Actions

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.

Features and Benefits

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.

pictograms

Skull and crossbones
GHS06

signalword

Danger

hcodes

H301,H319

Hazard Classifications

Acute Tox. 3 Oral - Eye Irrit. 2

Storage Class

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

wgk_germany

WGK 3

flash_point_f

Not applicable

flash_point_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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PYK2 negatively regulates the Hippo pathway in TNBC by stabilizing TAZ protein
Kedan A, et al.
Cell Death & Disease, 9(10), 1-15 (2018)
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)
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
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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.

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.

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.

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.

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