Naphthofluorescein(Synonyms: Naphthafluorescein)

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Naphthofluorescein (Synonyms: Naphthafluorescein)

Naphthofluorescein 抑制 HIF-1 和 Mint3 之间的相互作用。Naphthofluorescein 抑制 Mint3 依赖性 HIF-1 活性以及癌细胞和巨噬细胞的糖酵解活动，同时不引起体外细胞毒性和体内副作用。Naphthofluorescein 也是一种荧光 pH 敏感探针，可用于功能性切伦科夫成像。

Naphthofluorescein(Synonyms: Naphthafluorescein)

Naphthofluorescein Chemical Structure

CAS No. : 61419-02-1

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生物活性

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[1]. Naphthofluorescein is also a fluorescent pH-sensitive probe that can be used for functional Cerenkov imaging[2].

IC50 & Target

HIF-1[1]
体外研究
(In Vitro)

Naphthofluorescein (compound 19) (0-10 μM; 24 hours) suppresses the HIF-1 reporter activity in a concentration-dependent manner[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

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.

体内研究
(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[1].
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[1].
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[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male C57BL/6J mice (8 weeks)[1]
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)[1]
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.

分子量

432.42

Formula

C28H16O5
CAS 号

61419-02-1
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Sakamoto T, et al. Pharmacological inhibition of Mint3 attenuates tumour growth, metastasis, and endotoxic shock. Commun Biol. 2021;4(1):1165. Published 2021 Oct 7.

    [2]. Arroyo AD, et al. Development of fluorinated naphthofluoresceins for Cerenkov imaging. J Fluor Chem. 2019;225:27-34.

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