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Merck
모든 사진(1)

Key Documents

5.31050

Sigma-Aldrich

PFKFB3 Inhibitor III, YN1

동의어(들):

PFKFB3 Inhibitor III, YN1, 7,8-Dihydroxy-3-(4-hydroxyphenyl)-4H-chromen-4-one, 6-Phosphofructo-2-kinase/fructose-2,6-bisphosphatase 3 Inhibitor, YN1

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About This Item

실험식(Hill 표기법):
C15H10O5
CAS Number:
Molecular Weight:
270.24
UNSPSC 코드:
12352200
NACRES:
NA.77

분석

≥98% (HPLC)

Quality Level

형태

powder

효능

670 nM IC50

제조업체/상표

Calbiochem®

저장 조건

OK to freeze
protect from light

색상

off-white

solubility

DMSO: 100 mg/mL

저장 온도

2-8°C

InChI

1S/C15H10O5/c16-9-3-1-8(2-4-9)11-7-20-15-10(13(11)18)5-6-12(17)14(15)19/h1-7,16-17,19H

InChI key

BMZFZTMWBCFKSS-UHFFFAOYSA-N

일반 설명

A cell-permeable isoflavone compound that acts as a potent and competitive inhibitor of fructose-2,6-bisphosphatase 3 (PFKFB3; IC50 = 670 nM; Ki = 240 nM). Directly docks into the Fru-6-P binding pocket of PFKFB3 and down-regulates Fru-2,6-BP levels (40% decrease in 48 h in HeLa cells) resulting in reduced glycolysis and lactate production. Shown to diminish the proliferation of HCT-116 human adenocarcinoma cells (GI50 = 8.2 µM) and inhibit HeLa cells colony formation on soft agar (~79% reduction at 25 µM). Induces apoptotic (~25 µM) and necrotic (~50 µM) cell death depending on the level of ATP depletion. Also reported to increase autophagy in HCT-116 cells as evidenced by an increase in LC3-II levels and a decrease in p62 levels
A cell-permeable isoflavone compound that acts as a potent and competitive inhibitor of fructose-2,6-bisphosphatase 3 (PFKFB3; IC50 = 670 nM; Ki = 240 nM). Directly docks into the Fru-6-P binding pocket of PFKFB3 and down-regulates Fru-2,6-BP levels (40% decrease in 48 h in HeLa cells) resulting in reduced glycolysis and lactate production. Shown to diminish the proliferation of HCT-116 human adenocarcinoma cells (GI50 = 8.2 µM) and inhibit HeLa cells colony formation on soft agar (~79% reduction at 25 µM). Induces apoptotic (~25 µM) and necrotic (~50 µM) cell death depending on the level of ATP depletion. Also reported to increase autophagy in HCT-116 cells as evidenced by an increase in LC3-II levels and a decrease in p62 levels.

Please note that the molecular weight for this compound is batch-specific due to variable water content.

생화학적/생리학적 작용

Cell permeable: yes
Reversible: yes

포장

Packaged under inert gas

경고

Toxicity: Regulatory Review (Z)

기타 정보

Klarer, A. C., et al. 2014. Cancer Metab.2, 2.
Seo, M., et al. 2011. PLoS ONE6, e24179.

법적 정보

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

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point (°F)

Not applicable

Flash Point (°C)

Not applicable


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