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Merck
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文件

PZ0403

Sigma-Aldrich

PF-9366

≥98% (HPLC)

别名:

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

经验公式（希尔记法）:
C20H19ClN4
CAS号:
72882-78-1
分子量:
350.84
MDL號碼:
MFCD31630724
分類程式碼代碼:
51111800
NACRES:
NA.77

品質等級

100

化驗

≥98% (HPLC)

形狀

powder

顏色

white to beige

溶解度

DMSO: 2 mg/mL, clear

儲存溫度

room temp

SMILES 字串

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

生化／生理作用

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.

儲存類別代碼

11 - Combustible Solids

水污染物質分類（WGK）

WGK 3

閃點（°F）

Not applicable

閃點（°C）

Not applicable

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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

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