Naphthofluorescein

Research use only, not for human use.

Naphthofluorescein （Naphthafluorescein） is a Mint3 inhibitor with potential antitumor and anti-inflammatory activities, inhibits the interaction between HIF-1 and Mint3, inhibits Mint3-dependent HIF-1 activity, and inhibits glycolytic activity in cancer cells and macrophages without showing significant in vitro cytotoxicity or in vivo side effects.

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.

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.

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 weeksResult: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 weeksResult: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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Angiogenesis

HIF/HIF Prolyl-hydroxylase

HIF

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61419-02-1

432.42

C28H16O5

>98% (HPLC)

In Vitro:?DMSO : 125 mg/mL (289.07 mM; Ultrasonic )

Oc1ccc2c3Oc4c(ccc5cc(O)ccc45)C4(OC(=O)c5ccccc45)c3ccc2c1

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(-20℃)

With Ice Pack

≥ 2 years