2. Anti-infection Metabolic Enzyme/Protease Immunology/Inflammation
  3. Bacterial UGT Interleukin Related SOD COX
  4. Haplopine

Haplopine is a substance with anti-inflammatory, antioxidant and photoactivated antibacterial activities. It also acts as an inhibitor of UGT1A7 and a photoactivated restriction endonuclease inhibitor. Haplopine inhibits the mRNA/protein expression of IL-6, TSLP, GM-CSF, G-CSF, IL-4, IL-13 and COX-2, while upregulating the mRNA/protein expression of SOD, CAT and HO-1. Haplopine inhibits the glucuronidation reaction catalyzed by UGT1A7 through competitive hydrophobic binding. Haplopine exerts photoactivated restriction endonuclease inhibitory effects by binding to DNA. Haplopine exhibits photoactivated activity against methicillin-resistant Staphylococcus aureus. Haplopine alleviates symptoms of atopic dermatitis. Haplopine can be used in research related to atopic dermatitis and methicillin-resistant Staphylococcus aureus infections.

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Haplopine

Haplopine Chemical Structure

CAS No. : 5876-17-5

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Haplopine Related Antibodies

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  • Purity & Documentation

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Description

Haplopine is a substance with anti-inflammatory, antioxidant and photoactivated antibacterial activities. It also acts as an inhibitor of UGT1A7 and a photoactivated restriction endonuclease inhibitor. Haplopine inhibits the mRNA/protein expression of IL-6, TSLP, GM-CSF, G-CSF, IL-4, IL-13 and COX-2, while upregulating the mRNA/protein expression of SOD, CAT and HO-1. Haplopine inhibits the glucuronidation reaction catalyzed by UGT1A7 through competitive hydrophobic binding. Haplopine exerts photoactivated restriction endonuclease inhibitory effects by binding to DNA. Haplopine exhibits photoactivated activity against methicillin-resistant Staphylococcus aureus. Haplopine alleviates symptoms of atopic dermatitis. Haplopine can be used in research related to atopic dermatitis and methicillin-resistant Staphylococcus aureus infections[1][2][3][4].

Cellular Effect
Cell Line Type Value Description References
A549 IC50
> 10 μM
Compound: 9
Cytotoxicity against human A549 cells by SRB assay
Cytotoxicity against human A549 cells by SRB assay
[PMID: 18950230]
Neutrophil IC50
57.32 μM
Compound: 9
Antiinflammatory activity in human neutrophils assessed as fMLP-induced superoxide release after 5 mins by spectrometry
Antiinflammatory activity in human neutrophils assessed as fMLP-induced superoxide release after 5 mins by spectrometry
[PMID: 17822293]
In Vitro

Haplopine (12.5-25 μM; 0.5 h pre-incubation, 24 h stimulation) concentration-dependently inhibits the mRNA and protein expression of pro-inflammatory mediators IL-6, TSLP, GM-CSF and G-CSF in HaCaT cells stimulated with TNF-α/IFN-γ[1].
Haplopine (12.5-50 μM; 0.5 h pre-incubation, 24 h stimulation) inhibits the mRNA and protein expression of pro-inflammatory mediators IL-4, IL-13, and COX-2 in TNF-α/IFN-γ-stimulated Jurkat T cells[1].
Haplopine (12.5-50 μM; 0.5 h pre-incubation, 24 h stimulation) concentration-dependently restores the mRNA and protein expressions of antioxidant defense enzymes SOD, CAT and HO-1 in H2O2-stimulated Jurkat T cells[1].
Haplopine (0.5-100 μM; 30-120 min) competitively inhibits the 4-MU glucuronidation reaction catalyzed by recombinant human UGT1A7, with an IC50 of 13.4 μM, a Ki of 7.2 μM, and a calculated in vivo inhibition threshold of 0.72 μM[3].
Haplopine (100 μM; 30-120 min) inhibits the 4-MU glucuronidation reaction catalyzed by recombinant human UGT1A9 by 45% at a concentration of 100 μM[3].
Haplopine (100 μM; 30-120 min) inhibits the 4-MU glucuronidation reaction catalyzed by recombinant human UGT1A3 by 17% at a concentration of 100 μM[3].
Haplopine (100 μM; 30-120 min) inhibits 35% of the 4-MU glucuronidation reaction catalyzed by recombinant human UGT2B4 at a concentration of 100 μM[3].
Haplopine (12.5 nM/spot; overnight at 37°C) exhibits photoactivated antibacterial activity against methicillin-resistant Staphylococcus aureus after UVA irradiation, with a minimum inhibitory dose of 12.5 nM/spot, whereas it shows no activity in the dark[4].
Haplopine (100 nM/spot; overnight at 37°C) exhibits weak photoactivated antibacterial activity against Candida albicans, with a minimum inhibitory dose of 100 nM/spot under UVA irradiation, while it shows no activity in dark conditions[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Haplopine Related Antibodies

Real Time qPCR[1]

Cell Line: HaCaT human keratinocyte cell line
Concentration: 12.5 μM, 25 μM
Incubation Time: 0.5 h pre-incubation; 24 h stimulation
Result: Inhibited TNF-α/IFN-γ-induced IL-6 mRNA expression by 42% at 25 μM.
Suppressed TNF-α/IFN-γ-induced increases in TSLP, GM-CSF, and G-CSF mRNA to 2.7, 1.9, and 1.9-fold versus vehicle controls, respectively, at 12.5 μM.
Reduced TNF-α/IFN-γ-induced increases in TSLP, GM-CSF, and G-CSF mRNA to 1.8, 1.2, and 1.2-fold versus vehicle controls, respectively, at 25 μM.
Reduced the protein levels of IL-6 and GM-CSF in a concentration-dependent manner, with 25 μM causing a greater reduction than 12.5 μM.

Real Time qPCR[1]

Cell Line: Jurkat T human lymphocyte cell line
Concentration: 12.5 μM (protein analysis only), 25 μM, 50 μM
Incubation Time: 0.5 h pre-incubation; 24 h stimulation
Result: Inhibited TNF-α/IFN-γ-induced IL-13 mRNA expression by 63% and COX-2 mRNA expression by 70% versus stimulated controls at 25 μM.
Inhibited TNF-α/IFN-γ-induced IL-13 mRNA expression by 89% and COX-2 mRNA expression by 100% versus stimulated controls at 50 μM.
Suppressed TNF-α/IFN-γ-induced IL-4 mRNA upregulation in a concentration-dependent manner.
Reduced COX-2 protein expression in a concentration-dependent manner.\nIncreased H2O2-reduced SOD mRNA activity to 0.86-fold at 25 μM and 0.91-fold at 50 μM versus vehicle controls.
Increased CAT mRNA activity to 0.84-fold versus vehicle controls at 50 μM.
Increased H2O2-reduced HO-1 mRNA levels to 0.79-fold at 25 μM and 0.88-fold at 50 μM versus vehicle controls.
Restored the reduced protein expressions of SOD, CAT, and HO-1 in a concentration-dependent manner.
In Vivo

Haplopine (0.05-0.1%; topical administration; once daily; for 14 consecutive days) dose-dependently ameliorates DNCB-induced atopic dermatitis-like skin lesions in male Balb/c mice[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Balb/c (6-week-old male, DNCB-induced atopic dermatitis)[1]
Dosage: 0.05%; 0.1%
Administration: topical; daily; 14 days
Result: Reduced clinical dermatitis scores by 50%, total serum IgE levels by 23%, mast cell infiltration by 61%, and epidermal thickening by 50% compared to DNCB-treated controls.
Reduced clinical dermatitis scores by 40%, total serum IgE levels by 41%, mast cell infiltration by 52%, and epidermal thickening by 60% compared to DNCB-treated controls.
Caused dose-dependent decreases in spleen weight relative to DNCB-treated controls.
Molecular Weight

245.23

Formula

C13H11NO4
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

OC1=CC=C2C(OC)=C3C(OC=C3)=NC2=C1OC
Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Purity & Documentation
References
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Haplopine Related Classifications

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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.

Keywords:

Haplopine5876-17-5BacterialUGTInterleukin RelatedSODCOXUDP-glucuronosyltransferaseUridine diphosphate glucuronosyltransferaseILSuperoxide DismutaseCyclooxygenaseTSLPIL-6IL-13methicillin-resistant Staphylococcus aureusGM-CSFG-CSFUGT1A7COX-2Candida albicansIL-4atopic dermatitisInhibitorinhibitorinhibit

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