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PKM2 Activator III-Calbiochem

品牌
Sigma-Aldrich
货号
5.04537
包装型号
规格纯度
价格
2683.2 *本价格含增值税费
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半岛bd体育手机客户端 名称:
PKM2 Activator III-Calbiochem
Pyruvate Kinase M2 Activator III, N-(4-(4-(2-Methoxyphenyl)piperazine-1-carbonyl)phenyl)quinoline-8-sulfonamide
半岛bd体育手机客户端 介绍:

半岛bd体育手机客户端 说明

一般描述

A cell-permeable quinoline-sulfonamide that acts as a potent allosteric PKM2 activator both in cell-free enzymatic assays (AC50= 17 nM with 40 ng recombinant PKM2/200 ?L) and in cultures (AC50= 45 nM in A549 cells) via a high affinity (no dissociation in >1.5 h), 2:1 (compound to PKM2 tetramer) stoichiometric binding, effectively locking PKM2 in an active tetrameric state that is resistant to known intracellular negative regulators of PKM2 tetramer induced by the natural activator FBP (fructose 1,6-bisphosphate). PKM2 stimulation by compound treatment is shown to result in decreased serine biosynthesis (by 56%; 500 nM for 24 h) with concomitant increase in serine influx as a compensating mechanism for maintaining cellular serine level necessary for supporting A549 proliferation. Simultaneous PKM2 activation by drug treatment and culture serine withdrawal results in depletion of cellular serine pool (by ~70% in 24 h) and induction of cytostatic A549 growth arrest (by 56%; 72 h 1 ?M drug treatment in BME + NEAA - Ser), but not apoptosis. Serine-dependent proliferation inhibition upon PKM2 activation is reported to be cell-specific, while it is observed in A549 and H460 cultures, SW480 and H522 are not affected.
A cell-permeable quinoline-sulfonamide that acts as a potent allosteric PKM2 activator both in cell-free enzymatic assays (AC50= 17 nM with 40 ng PKM2/200 ?L) and in cultures (AC50= 45 nM in A549 cells) via a high affinity, 2:1 stoichiometric binding, effectively locking PKM2 in an active tetrameric state resistant to known intracellular negative regulators of FBP-activated PKM2 tetramer. PKM2 stimulation by compound treatment is shown to result in decreased serine biosynthesis (by 56%; 500 nM for 24 h) with concomitant increase in serine influx as a compensating mechanism for maintaining cellular serine level necessary for supporting A549 proliferation. Simultaneous PKM2 activation and culture serine withdrawal results in cytostatic A549 growth arrest, but not apoptosis.

生化/生理作用

Cell permeable: yes
Primary Target
PKM2
Reversible: no

包装

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

重悬

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

其他说明

Kung, C., et al. 2012.Chem. Biol.19,1187.

法律信息

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

基本信息

经验(实验)分子式 C27H26N4O4S
分子量 502.58

半岛bd体育手机客户端 性质

测定 ≥99% (HPLC)
质量水平 100
形式 powder
manufacturer/tradename Calbiochem?
储存条件 OK to freeze
protect from light
颜色 off-white
溶解性 DMSO: 5 mg/mL
储存温度 2-8℃

安全信息

储存分类代码 11 - Combustible Solids
WGK WGK 3
闪点(F) Not applicable
闪点(C) Not applicable

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