3PO

SKU: orb1218574

Description

3PO is a small-molecule inhibitor of PFKFB3 (IC50: 22.9 μM), inhibiting the proliferation of several human malignant hematopoietic and adenocarcinoma cell lines (IC50: 1.4-24 μM). It suppresses glucose uptake, and decreases the intracellular concentration of Fru-2,6-BP, lactate, ATP, NAD+, and NADH.

Key Properties

• CAS Number: 18550-98-6
• MW: 210.23
• Purity: >98% (HPLC)
• Formula: C₁₃H₁₀N₂O
• SMILES: O=C(/C=C/c1cnccc1)c1ccncc1
• Target: Glucokinase
• Solubility: DMSO:113mg/ml（537.51mM）;Ethanol:11 mg/mL (52.32 mM);Water:Insoluble

Bioactivity

• In Vivo:
  3PO (0.07 mg/g; i.p. once per day for 14 days) inhibits the growth of Lewis lung carcinoma xenografts in C57Bl/6 mice. 3PO (0.07 mg/g; i.p. three sequential daily injections followed by 3 off days for 14 days) inhibits the tumor growth in BALB/c athymic mice. 3PO (0.07 mg/g; i.p. two daily injections followed a 7-day rest for 14 days) inhibits the tumor growth in BALB/c athymic mice. 3PO (0.07 mg/g; i.p. once) inhibits Fru-2, 6-BP and glucose uptake in C57Bl/6 mice. Animal model: Female C57Bl/6 mice with Lewis lung carcinoma xenografts. Dosage: 0.07 mg/g. Administration: Intraperitoneal injection; 0.07 mg/g once a day; for 14 days. Result: Suppressed the growth of Lewis lung carcinoma xenografts in C57Bl/6 mice compared to the control group. Animal model: Female BALB/c athymic mice with MDA-MB231 human breast adenocarcinoma xenografts. Dosage: 0.07 mg/g. Administration: Intraperitoneal injection; 0.07 mg/g three sequential daily injections of either DMSO or 3PO followed by 3 off days; for 14 days. Result: Suppressed xenograft tumorigenic growth of MDA-MB231 cells compared with the controls. Animal model: Female BALB/c athymic mice with HL-60 leukemia xenografts. Dosage: 0.07 mg/g. Administration: Intraperitoneal injection; 0.07 mg/g two daily injections followed a 7-day rest; for 14 days. Result: Suppressed xenograft tumorigenic growth of HL-60 leukemia compared with the controls, especially from the second administration cycle. Animal model: Female C57Bl/6 mice with Lewis lung carcinoma xenografts. Dosage: 0.07 mg/g. Administration: Intraperitoneal injection; once. Result: Decreased Fru-2, 6-BP and glucose uptake in C57Bl/6 mice compared to control group.
• In Vitro:
  3PO (0-33 μM; 0-36 h) inhibits Jurkat cells proliferation by influence cell cycle.3PO (10 μM/L; 0-36 h) suppresses glycolytic flux to lactate in Jurkat cells.3PO (10 μM/L; 0-36 h) inhibits cellular proliferation of transformed tumor cell lines. Cell Proliferation Assay Cell line: Jurkat cells. Concentration: 0.3, 1, 3, 10 and 33 μM Incubation time: 0, 4, 8, 16, 24 and 36 hours. Result: Inhibited Jurkat T cells proliferation by G2-M phase cell cycle arrest. Cell Viability Assay Cell line: Jurkat cells. Concentration: 0.3, 1, 3, 10 and 33 μM Incubation time: 0, 4, 8, 16, 24 and 36 hours. Result: Decreased lactate secretion, NADH, NAD+ and ATP in Jurkat cells. Cell Proliferation Assay Cell line: Jurkat, K562, HL-60, MDA-MB231, HL-60, HeLa, Melanoma and Lewis Lung. Concentration: 0-20 μM. Incubation time: 0, 4, 8, 16, 24 and 36 hours. Result: Inhibited solid tumor and hematologic cell lines with IC50s of 1.4-24 μM/L.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

Glucokinase