5.31050

PFKFB3 Inhibitor III, YN1

• Sinonimo/i: 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
• Formula empirica (notazione di Hill): C₁₅H₁₀O₅
• Numero CAS: 75187-63-2
• Peso molecolare: 270.24
• Codice UNSPSC: 12352200
• NACRES: NA.77

Proprietà

• Saggio: ≥98% (HPLC)
• Livello qualitativo: 100
• Forma fisica: powder
• Potenza: 670 nM IC₅₀
• Produttore/marchio commerciale: Calbiochem^®
• Condizioni di stoccaggio: OK to freeze; protect from light
• Colore: off-white
• Solubilità: DMSO: 100 mg/mL
• Temperatura di conservazione: 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; BMZFZTMWBCFKSS-UHFFFAOYSA-N

Descrizione

Descrizione generale

A cell-permeable isoflavone compound that acts as a potent and competitive inhibitor of fructose-2,6-bisphosphatase 3 (PFKFB3; IC₅₀ = 670 nM; K_i = 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; K_i = 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.

Azioni biochim/fisiol

Cell permeable: yes

Reversible: yes

Confezionamento

Packaged under inert gas

Attenzione

Toxicity: Regulatory Review (Z)

Altre note

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

Note legali

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

Informazioni sulla sicurezza

• Codice della classe di stoccaggio: 11 - Combustible Solids
• Classe di pericolosità dell'acqua (WGK): WGK 3
• Punto d’infiammabilità (°F): Not applicable
• Punto d’infiammabilità (°C): Not applicable