2. Epigenetics Immunology/Inflammation
  3. DNA Methyltransferase Interleukin Related
  4. EGR-1-IN-1

EGR-1-IN-1 is a EGR-1 inhibitor with an IC50 of 1.86 μM. EGR-1-IN-1 binds to the zinc finger DNA-binding domain of EGR-1 and promotes the dissociation of the EGR-1-DNA complex. EGR-1-IN-1 reduces the mRNA expression levels of EGR-1-regulated inflammatory genes induced by TNFα. EGR-1-IN-1 alleviates atopic dermatitis-like lesions in the ear skin of mice. EGR-1-IN-1 serves as a lead compound for the development of targeted compounds for inflammatory skin diseases. EGR-1-IN-1 can be used in studies related to atopic dermatitis.

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

CAS No. : 3077196-25-6

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Customer Review

Based on 2 publication(s) in Google Scholar

EGR-1-IN-1 Related Antibodies

Top Publications Citing Use of Products
WB
Cell Proliferation/Viability Assay
Flow Cytometry
Bio/Physico-chemical Assay

    EGR-1-IN-1 purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2026 Feb;13(10):e17825.  [Abstract]

    EGR-1-IN-1 (5 µM) decreased the expression of SMPD1 in Cre- microglia while not in Cre+ microglia after OAM.

    EGR-1-IN-1 purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2026 Feb;13(10):e17825.  [Abstract]

    EGR-1-IN-1 (5 µM) increased the BODIPY+ lipid droplets in Cre- microglia after OAM for 6 h.

    EGR-1-IN-1 purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2026 Feb;13(10):e17825.  [Abstract]

    EGR-1-IN-1 (5 µM) significantly reduced EGR1 binding to Site-1 and Site-2 regions of the SMPD1 promoter in BV2 cells under OAM conditions.

    EGR-1-IN-1 purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2026 Feb;13(10):e17825.  [Abstract]

    EGR-1-IN-1 (5 µM) significantly increased LDs formation in primary microglia in vitro.

    EGR-1-IN-1 purchased from MedChemExpress. Usage Cited in: Cell Signal. 2025 Sep 10:136:112127.  [Abstract]

    EGR-1-IN-1 (2 μM; 1 h) partially restored viability of HUVECs treated with Erastin.

    View All DNA Methyltransferase Isoform Specific Products:

    View All Isoforms
    DNA Methyltransferase DNMT1 DNMT3 MGMT

    View All Interleukin Related Isoform Specific Products:

    View All Isoforms
    IL-1 IL-2 IL-3 IL-4 IL-5 IL-6 IL-8 IL-10 IL-12 IL-13 IL-15 IL-17 IL-23 IL-7 IL-33 IL-22 IL-18

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    Description

    EGR-1-IN-1 is a EGR-1 inhibitor with an IC50 of 1.86 μM. EGR-1-IN-1 binds to the zinc finger DNA-binding domain of EGR-1 and promotes the dissociation of the EGR-1-DNA complex. EGR-1-IN-1 reduces the mRNA expression levels of EGR-1-regulated inflammatory genes induced by TNFα. EGR-1-IN-1 alleviates atopic dermatitis-like lesions in the ear skin of mice. EGR-1-IN-1 serves as a lead compound for the development of targeted compounds for inflammatory skin diseases. EGR-1-IN-1 can be used in studies related to atopic dermatitis[1].

    IC50 & Target

    13030

    1.86 μM (IC50)

    In Vitro

    EGR-1-IN-1 (IT25) potently inhibits the DNA-binding activity of human EGR-1, with an IC50 of 1.86 μM in in vitro biochemical assays, and achieves an inhibition rate of 76.1% at a concentration of 50 μM[1].
    EGR-1-IN-1 (0-5 μM; 30 min pre-incubation, followed by 1 h TNFα stimulation) inhibits TNFα-induced formation of EGR-1-DNA complexes in human HaCaT keratinocytes[1].
    EGR-1-IN-1 (0-5 μM; 30 min pre-incubation, followed by 12 h TNFα stimulation) reduces the mRNA expression of TNFα-induced, EGR-1-regulated inflammatory genes in human HaCaT keratinocytes[1].

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

    EGR-1-IN-1 Related Antibodies

    RT-PCR[1]

    Cell Line: human HaCaT keratinocytes
    Concentration: 0, 1, 5 μM
    Incubation Time: 30 min pre-incubation, followed by 12 h TNFα stimulation
    Result: Dose-dependently reduced TNFα-induced mRNA expression of multiple EGR-1-regulated inflammatory genes, including TSLP, IL17, IL4, IL13, IL23, IL33, IL1β, IL6, CCL2, CCL5, and Artemin.
    In Vivo

    EGR-1-IN-1 (0.1%; topical administration; once daily, five times per week for 14 consecutive days) significantly alleviates 2,4-dinitrochlorobenzene (DNCB)-induced atopic dermatitis-like skin lesions in BALB/c mice, including reducing skin thickening, inflammatory cell infiltration, TSLP expression and sensory innervation[1].

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

    Animal Model: BALB/c (male, 6-8-week-old, DNCB-induced atopic dermatitis)[1]
    Dosage: 0.1%
    Administration: topical; once daily five times weekly; 14 days
    Result: Considerably improved gross ear skin lesions.
    Effectively reduced DNCB-induced epidermal and dermal thickness.
    Reduced infiltration of MPO-positive neutrophils, F4/80-positive macrophages, CD3ε-positive Th subsets, and toluidine blue-stained mast cells.
    Reduced TSLP expression in the epidermal layer.
    Substantially reduced sensory nerve density and intraepidermal innervation at the epidermal-dermal interface.
    Molecular Weight

    351.38

    Formula

    C17H13N5O2S
    CAS No.
    Appearance

    Solid

    Color

    Light yellow to orange

    SMILES

    COC1=CC2=C(/C(C(N2)=O)=N/NC(NC3=CC=C(C=C3)C#N)=S)C=C1
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 1 mg/mL (2.85 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Acetone : < 1 mg/mL (insoluble)

    THF : < 1 mg/mL (insoluble)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.8459 mL 14.2296 mL 28.4592 mL
    5 mM --- --- ---
    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.

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    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 2.8459 mL 14.2296 mL 28.4592 mL 71.1480 mL
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    EGR-1-IN-1 Related Classifications

    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:

    EGR-1-IN-13077196-25-6DNA MethyltransferaseInterleukin RelatedDNMTsDNA MTasesILEGR-1 zinc-finger DNA-binding domainTSLPhuman HaCaT keratinocytesmouse ear skinEGR-1-regulated inflammatory genesBALB/c miceTNFαEGR-1-DNA complexatopic dermatitis-like skin lesionsinflammatory skin disordersInhibitorinhibitorinhibit

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