2. Epigenetics Stem Cell/Wnt Protein Tyrosine Kinase/RTK JAK/STAT Signaling Neuronal Signaling Membrane Transporter/Ion Channel Metabolic Enzyme/Protease
  3. JAK TRP Channel MetAP
  4. Ovalicin

Ovalicin is a multi-target inhibitor that targets MetAP2, HRH2, JAK2 and TRPV1, with anti-inflammatory and anti-atopic dermatitis activities. Ovalicin covalently binds to MetAP2 to inhibit its function, thereby blocking the replication of Enterocytozoon bieneusi and Vittaforma corneae. Ovalicin alleviates intestinal injury and prolongs survival in infected mouse models, without showing obvious hepatorenal toxicity. Ovalicin attenuates LPS-induced calcium influx, reduces the infiltration of macrophages and mast cells in the skin, and regulates the expression of inflammation-related genes such as IL-31, effectively relieving allergic symptoms in mouse models. Ovalicin can be used for the research of microsporidiosis and atopic dermatitis.

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

Ovalicin

Ovalicin Chemical Structure

CAS No. : 19683-98-8

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Ovalicin Related Antibodies

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Description

Ovalicin is a multi-target inhibitor that targets MetAP2, HRH2, JAK2 and TRPV1, with anti-inflammatory and anti-atopic dermatitis activities. Ovalicin covalently binds to MetAP2 to inhibit its function, thereby blocking the replication of Enterocytozoon bieneusi and Vittaforma corneae. Ovalicin alleviates intestinal injury and prolongs survival in infected mouse models, without showing obvious hepatorenal toxicity. Ovalicin attenuates LPS-induced calcium influx, reduces the infiltration of macrophages and mast cells in the skin, and regulates the expression of inflammation-related genes such as IL-31, effectively relieving allergic symptoms in mouse models. Ovalicin can be used for the research of microsporidiosis and atopic dermatitis[1][2].

IC50 & Target

JAK2

 

MetAp2

 

TRPV1

 

Cellular Effect
Cell Line Type Value Description References
A-431 IC50
7.5 μM
Compound: 1 (Ovalicin)
In vitro antiproliferative effect against A431 human epidermoid carcinoma cells
In vitro antiproliferative effect against A431 human epidermoid carcinoma cells
10.1016/S0960-894X(96)00564-1
A549 GI50
4.1 μM
Compound: 8
Cytotoxicity against human A549 cells after 72 hrs by SRB assay
Cytotoxicity against human A549 cells after 72 hrs by SRB assay
[PMID: 23964677]
In Vitro

Treatment of RK-13 rabbit kidney cells with Ovalicin (10 μM; 10 d) at a non-toxic concentration for 10 days results in over 70% replication inhibition of Encephalitozoon intestinalis (IC50=0.004 μM) and Vittaforma corneae (IC50=0.002 μM)[1].
Ovalicin (1-200 μg/mL; 24-72 h) reduces the viability of DH82 cells in a dose-dependent manner[2].
Ovalicin (2-8 μg/mL; 1 d) dose-dependently reduces the increased cell viability of DH82 cells pretreated with LPS[2].
Ovalicin (2-10 μg/mL; 1 d) dose-dependently inhibits the LPS-induced upregulation of IL4, IFNG, TRPV1, HRH2 and IL31RA mRNA expression in DH82 cells, with the inhibitory effect of 10 μg/mL Ovalicin being stronger than that of Dexamethasone (HY-14648)[2].
Ovalicin (2-10 μg/mL; 1 d) dose-dependently inhibits LPS-induced activation of the IL-31 signaling pathway in DH82 cells by reducing the expression of IL31RA, OSMR, JAK2 and p-STAT3; at concentrations of 4 and 10 μg/mL, its inhibitory effect is stronger than that of Dexamethasone (HY-14648)[2].
Ovalicin (10 μg/mL; 1 d) attenuates LPS-induced calcium influx in DH82 cells, and its efficacy is stronger than that of Dexamethasone (HY-14648) and Ruxolitinib (HY-50856)[2].
Ovalicin (2-10 μg/mL; 1 d) inhibits LPS-induced inflammatory responses in DH82 cells in a dose-dependent manner by reducing the levels of iNOS, COX2, NF-κB and ROS, and its inhibitory effect is stronger than that of Dexamethasone (HY-14648)[2].

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

Ovalicin Related Antibodies

Cell Viability Assay[2]

Cell Line: canine macrophage cell line DH82
Concentration: 1-200 μg/mL
Incubation Time: 24 h; 48 h; 72 h
Result: Decreased DH82 cell viability dose-dependently.
Maintained more than 90% cell survival at 1 and 10 μg/mL after 24 and 48 hours.

Cell Viability Assay[2]

Cell Line: LPS-pretreated canine macrophage cell line DH82
Concentration: 2-8 μg/mL
Incubation Time: 1 day
Result: Decreased cell viability dose-dependently in LPS-pretreated DH82 cells, where LPS pretreatment had increased cell viability compared to LPS-untreated cells.

Real Time qPCR[2]

Cell Line: LPS-pretreated canine macrophage cell line DH82
Concentration: 2-10 μg/mL
Incubation Time: 1 day
Result: Significantly attenuated LPS-induced upregulation of IL4 and IFNG mRNA expression.
Exerted a stronger inhibitory effect on these mRNA levels at 10 μg/mL than Dexamethasone.\nSignificantly inhibited LPS-induced increases in TRPV1 and HRH2 mRNA expression.
Exerted a stronger inhibitory effect than dexamethasone and ruxolitinib.
More significantly inhibited LPS-induced increases in IL31RA, TRPV1, and HRH2 mRNA expression than ruxolitinib.

ELISA Assay[2]

Cell Line: LPS-pretreated canine macrophage cell line DH82
Concentration: 2-10 μg/mL
Incubation Time: 1 day
Result: Significantly inhibited LPS-induced IL-31 protein expression in DH82 cells.
Exerted a stronger inhibitory effect than dexamethasone treatment.
In Vivo

Ovalicin (5-20 mg/kg; s.c.; daily) administered at 5 mg/kg subcutaneously daily statistically significantly prolongs survival of V. corneae-infected athymic mice and reduces parasite-associated small intestinal lesions[1].
Ovalicin (1-10 μg/mL; topical; daily; 5 days) dose-dependently alleviates atopic dermatitis symptoms in DNCB-induced BALB/C mice by reducing dermal immune cell infiltration, normalizing serum parameters, and inhibiting IL-31 signaling and pruritus-related gene expression[2].
Ovalicin (10 μg/mL; topical; daily; 5 days) does not induce skin morphologic changes or dermatitis in healthy BALB/C mice[2].

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

Animal Model: CRL:CD-1nuBR (7-week-old male, intraperitoneally inoculated with Vittaforma corneae spores)[1]
Dosage: 5 mg/kg; 10 mg/kg; 20 mg/kg
Administration: s.c.; daily
Result: Prolonged mean survival time to 19.9 days and reduced mean number of parasite-associated small intestinal lesions to 11.6 at 5 mg/kg.
Showed no statistically significant increases in survival time relative to controls at 10 mg/kg or 20 mg/kg.
Showed no significant differences in mean numbers of lesions in the small intestine, liver, and pancreas relative to controls at 10 mg/kg or 20 mg/kg.
Resulted in full study duration survival with no drug-associated lesions in uninfected mice at 20 mg/kg.
Animal Model: BALB/C (female, 5 weeks old, atopic dermatitis induced by DNCB)[2]
Dosage: 1 μg/mL; 10 μg/mL
Administration: topical; daily; 5 days
Result: Decreased the number of IBA1-positive macrophages and mast cells infiltrated in the dermis in a dose-dependent manner.
Significantly reduced dermatitis lesion scores (assessed by hemorrhage, scarring, edema, and erosion).
Reversed elevated serum albumin and total protein levels.
Decreased elevated serum IL-31 concentration in a dose-dependent manner.
Reduced mRNA expression of TRPV1 and HRH2 in skin tissue.
Decreased expression of IL-31 receptor (IL-31R) in skin tissue.
Enhanced re-epithelialization and granulation tissue formation in skin.
Molecular Weight

296.36

Formula

C16H24O5
CAS No.
SMILES

O[C@@]([C@@H]1OC)([C@]([C@H]2C/C=C(C)\C)(O2)C)[C@]3(CCC1=O)CO3
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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Ovalicin 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:

Ovalicin19683-98-8JAKTRP ChannelMetAPJanus kinaseTransient receptor potential channelsMethionine AminopeptidaseJAK2Vittaforma corneaeDH82 cellsTRPV1BALB/C miceHRH2RK-13 rabbit kidney cellsEncephalitozoon intestinalisMetAP2athymic miceInhibitorinhibitorinhibit

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