5.31050

PFKFB3 Inhibitor III, YN1

• Synonim(y): 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
• Wzór empiryczny (zapis Hilla): C₁₅H₁₀O₅
• Numer CAS: 75187-63-2
• Masa cząsteczkowa: 270.24
• Kod UNSPSC: 12352200
• NACRES: NA.77

Właściwości

• Próba: ≥98% (HPLC)
• Poziom jakości: 100
• Postać: powder
• siła działania: 670 nM IC₅₀
• producent / nazwa handlowa: Calbiochem^®
• warunki przechowywania: OK to freeze; protect from light
• kolor: off-white
• rozpuszczalność: DMSO: 100 mg/mL
• temp. przechowywania: 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
• Klucz InChI: BMZFZTMWBCFKSS-UHFFFAOYSA-N

Opis

Opis ogólny

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.

Działania biochem./fizjol.

Cell permeable: yes

Reversible: yes

Opakowanie

Packaged under inert gas

Ostrzeżenie

Toxicity: Regulatory Review (Z)

Inne uwagi

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

Informacje prawne

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

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Informacja o środkach bezpieczeństwa

• Kod klasy składowania: 11 - Combustible Solids
• Klasa zagrożenia wodnego (WGK): WGK 3
• Temperatura zapłonu (°F): Not applicable
• Temperatura zapłonu (°C): Not applicable