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PZ0403

Sigma-Aldrich

PF-9366

≥98% (HPLC)

Synonym(e):

7-Chloro-N,N-dimethyl-5-phenyl-[1,2,4]triazolo[4,3-a]quinoline-1-ethanamine, PF 9366, PF9366

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About This Item

Empirische Formel (Hill-System):
C20H19ClN4
CAS-Nummer:
72882-78-1
Molekulargewicht:
350.84
MDL-Nummer:
MFCD31630724
UNSPSC-Code:
51111800
NACRES:
NA.77

Qualitätsniveau

100

Assay

≥98% (HPLC)

Form

powder

Farbe

white to beige

Löslichkeit

DMSO: 2 mg/mL, clear

Lagertemp.

room temp

SMILES String

ClC(C=C1)=CC(C(C2=CC=CC=C2)=C3)=C1N4C3=NN=C4CCN(C)C

Biochem./physiol. Wirkung

PF-9366 is a methionine adenosyltransferase 2A allosteric inhibitor (human Mat2A IC50/Kd = 420 nM/170 nM) whose binding site overlaps with that of the Mat2A regulator, Mat2B. PF-9366 inhibits cellular SAM production in a Mat2B-competitive manner (IC50 post 6-hr treatment = 1.2 μM wihout vs. 0.86 μM with Mat2B knockdown; H520 lung carcinoma cells) without antiproliferation efficacy in cancer cultures due to an induction of Mat2A upregulation upon allosteric inhibition. Similar to Mat2B, PF-9366 allosteric binding alters Mat2A active site, causing increased substrate affinity and decreased enzyme turnover.

Lagerklassenschlüssel

11 - Combustible Solids

WGK

WGK 3

Flammpunkt (°F)

Not applicable

Flammpunkt (°C)

Not applicable

Analysenzertifikate (COA)

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Weiwei Yu et al.
Molecular cell, 75(6), 1147-1160 (2019-08-20)
Activated macrophages adapt their metabolic pathways to drive the pro-inflammatory phenotype, but little is known about the biochemical underpinnings of this process. Here, we find that lipopolysaccharide (LPS) activates the pentose phosphate pathway, the serine synthesis pathway, and one-carbon metabolism
Jiraporn Panmanee et al.
The FEBS journal, 286(11), 2135-2154 (2019-02-19)
Methylation is an underpinning process of life and provides control for biological processes such as DNA synthesis, cell growth, and apoptosis. Methionine adenosyltransferases (MAT) produce the cellular methyl donor, S-Adenosylmethionine (SAMe). Dysregulation of SAMe level is a relevant event in
Casey L Quinlan et al.
Nature chemical biology, 13(7), 785-792 (2017-05-30)
S-Adenosyl-L-methionine (SAM) is an enzyme cofactor used in methyl transfer reactions and polyamine biosynthesis. The biosynthesis of SAM from ATP and L-methionine is performed by the methionine adenosyltransferase enzyme family (Mat; EC 2.5.1.6). Human methionine adenosyltransferase 2A (Mat2A), the extrahepatic

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