1. Metabolic Enzyme/Protease
  2. HIF/HIF Prolyl-Hydroxylase
  3. Naphthofluorescein

Naphthofluorescein  (Synonyms: Naphthafluorescein)

Cat. No.: HY-124473 Purity: 99.52%
COA Handling Instructions

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.

For research use only. We do not sell to patients.

Naphthofluorescein Chemical Structure

Naphthofluorescein Chemical Structure

CAS No. : 61419-02-1

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5 mg USD 25 In-stock
10 mg USD 35 In-stock
25 mg USD 56 In-stock
50 mg USD 78 In-stock
100 mg USD 102 In-stock
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Based on 1 publication(s) in Google Scholar

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

IC50 & Target

HIF-1[1]

In Vitro

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

MedChemExpress (MCE) 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.
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].

MedChemExpress (MCE) 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.
Molecular Weight

432.42

Formula

C28H16O5

CAS No.
Appearance

Solid

Color

Purple to purplish red

SMILES

O=C(C1=C2C=CC=C1)OC32C4=C(OC5=C3C=CC6=CC(O)=CC=C56)C7=CC=C(O)C=C7C=C4

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (289.07 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3126 mL 11.5628 mL 23.1257 mL
5 mM 0.4625 mL 2.3126 mL 4.6251 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.3126 mL 11.5628 mL 23.1257 mL 57.8142 mL
5 mM 0.4625 mL 2.3126 mL 4.6251 mL 11.5628 mL
10 mM 0.2313 mL 1.1563 mL 2.3126 mL 5.7814 mL
15 mM 0.1542 mL 0.7709 mL 1.5417 mL 3.8543 mL
20 mM 0.1156 mL 0.5781 mL 1.1563 mL 2.8907 mL
25 mM 0.0925 mL 0.4625 mL 0.9250 mL 2.3126 mL
30 mM 0.0771 mL 0.3854 mL 0.7709 mL 1.9271 mL
40 mM 0.0578 mL 0.2891 mL 0.5781 mL 1.4454 mL
50 mM 0.0463 mL 0.2313 mL 0.4625 mL 1.1563 mL
60 mM 0.0385 mL 0.1927 mL 0.3854 mL 0.9636 mL
80 mM 0.0289 mL 0.1445 mL 0.2891 mL 0.7227 mL
100 mM 0.0231 mL 0.1156 mL 0.2313 mL 0.5781 mL
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
Naphthofluorescein
Cat. No.:
HY-124473
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