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Merck
CN
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文件

525330

Sigma-Aldrich

PFKFB3抑制剂,3PO

PFKFB3 Inhibitor, 3PO, is a cell-permeable, selective inhibitor of PFK-2 (6-phosphofructo-2-Kinase) activity.

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别名:
PFKFB3抑制剂,3PO
经验公式(希尔记法):
C13H10N2O
分子量:
210.23
MDL编号:
UNSPSC代码:
12352200
NACRES:
NA.28

质量水平

检测方案

≥99% (HPLC)

形式

solid

制造商/商品名称

Calbiochem®

储存条件

OK to freeze
protect from light

颜色

pale yellow

溶解性

DMSO: 50 mg/mL

运输

ambient

储存温度

2-8°C

一般描述

一种可渗透细胞的联吡啶基丙烯酮化合物,以混合模式方式选择性阻断PFKFB3同工酶相对于PFK-1(6-磷酸果糖-1-激酶)的PFK-2(6-磷酸果糖-2-激酶)活性。迅速降低果糖2,6-二磷酸(F-2,6-P2)和2-脱氧葡萄糖的摄取以及乳酸盐的分泌;有效阻止转化细胞的增殖(NHBE-ht/LT/ras的IC50 ~ 1.4 µ M),并在几种异种移植小鼠模型中抑制肿瘤生长(70 mg/kg,i.p.)。显示3PO的细胞抑制作用和细胞毒性作用对F-6-P(果糖-6-磷酸)和F-2,6-P2的细胞内水平高度敏感。

包装

用惰性气体包装

警告

毒性:标准处理(A)

重悬

复溶后,等分并冷冻保存(-70°C)。贮备液在-70°C下可稳定保存至多6个月。

其他说明

Clem, B., et al. 2008.Mol.Cancer Ther.7, 110.

法律信息

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

WGK

WGK 3

闪点(°F)

Not applicable

闪点(°C)

Not applicable


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Brian Clem et al.
Molecular cancer therapeutics, 7(1), 110-120 (2008-01-19)
6-phosphofructo-1-kinase, a rate-limiting enzyme of glycolysis, is activated in neoplastic cells by fructose-2,6-bisphosphate (Fru-2,6-BP), a product of four 6-phosphofructo-2-kinase/fructose-2,6-bisphosphatase isozymes (PFKFB1-4). The inducible PFKFB3 isozyme is constitutively expressed by neoplastic cells and required for the high glycolytic rate and anchorage-independent
Juliana Escher Toller-Kawahisa et al.
Nature communications, 14(1), 4280-4280 (2023-07-18)
Neutrophils rely predominantly on glycolytic metabolism for their biological functions, including reactive oxygen species (ROS) production. Although pyruvate kinase M2 (PKM2) is a glycolytic enzyme known to be involved in metabolic reprogramming and gene transcription in many immune cell types
Gangqi Wang et al.
Arteriosclerosis, thrombosis, and vascular biology, 40(2), 350-364 (2019-12-13)
Endothelial cells exposed to laminar shear stress express a thick glycocalyx on their surface that plays an important role in reducing vascular permeability and endothelial anti-inflammatory, antithrombotic, and antiangiogenic properties. Production and maintenance of this glycocalyx layer is dependent on

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