Naphthofluorescein

SKU: orb2901002

Description

Naphthofluorescein inhibits the interaction between HIF-1 and Mint3.Naphthofluorescein suppresses Mint3-dependent HIF-1 activity and glycolysis in cancer cells and macrophages without cytotoxicity in vitro and adverse effect in vivo. Naphthofluorescein is also a fluorescent pH-sensitive probe that can be used for functional Cerenkov imaging.

Key Properties

• CAS Number: 61419-02-1
• MW: 432.42
• Purity: >98% (HPLC)
• Formula: C₂₈H₁₆O₅
• SMILES: Oc1ccc2c3Oc4c(ccc5cc(O)ccc45)C4(OC(=O)c5ccccc45)c3ccc2c1
• Target: HIF/HIF Prolyl-hydroxylase
• Solubility: In Vitro: DMSO : 125 mg/mL (289.07 mM; Ultrasonic )

Bioactivity

• In Vivo:
  Naphthofluorescein (compound 19) (100 mg/kg; i.p.; once daily for 5 consecutive days followed by 2 days off for 2 weeks)does not show weight loss or apparent histological abnormalities in the lung, liver, and kidney, or cause cause severe adverse effects for at least 2 weeks in mice. Naphthofluorescein (compound 19) (100 mg/kg; i.p.; once daily for 5 consecutive days followed by 2 days off for 2 weeks) strikingly suppresses the tumour growth of subcutaneously injected E0771 cells and significantly attenuates tumour growth of MDA-MB-231 and AsPC-1 cells in immunodeficient mice. In turn, naphthofluorescein does not attenuate tumour growth of FIH-1-depleted MDA-MB-231 cells. Naphthofluorescein (compound 19) (100 mg/kg; i.p.; once daily for 5 consecutive days followed by 2 days off for 2 weeks) suppresses tumour growth in human cancer cells in an FIH-1-dependent manner. Animal model: Male C57BL/6J mice (8 weeks). Dosage: 100 mg/kg. Administration: i.p.; once daily for 5 consecutive days followed by 2 days off for 2 weeks. Result: Neither showed weight loss or apparent histological abnormalities in the lung, liver, and kidney, or caused cause severe adverse effects for at least 2 weeks in mice. Animal model: Female C57BL/6J mice (E0771) and BALB/c nude mice (HT1080, MDA-MB-231, and AsPC-1) (6 weeks). Dosage: 100 mg/kg. Administration: i.p.; once daily for 5 consecutive days followed by 2 days off for 2 weeks. Result: Strikingly suppressed the tumour growth of subcutaneously injected E0771 cells and significantly attenuated tumour growth of MDA-MB-231 and AsPC-1 cells in immunodeficient mice. In turn, naphthofluorescein did not attenuate tumour growth of FIH-1-depleted MDA-MB-231 cells.
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• In Vitro:
  Naphthofluorescein (compound 19) (0-10 μM; 24 hours) suppresses the HIF-1 reporter activity in a concentration-dependent manner. Cell Viability Assay Cell line: HT1080 cells. Concentration: 0-10 μM. Incubation time: 24 hours. Result: Significantly suppressed the HIF-1 reporter activity in a concentration-dependent manner.
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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

HIF/HIF Prolyl-hydroxylase