1. Epigenetics
  2. Protein Arginine Deiminase
  3. PADI4-IN-1

PADI4-IN-1 is a potent peptidylarginine deiminase isoform 4 (PADI4) inhibitor with an IC50 of 1.5 μM and SI (PADI1/PADI4) of 52.1. PADI4-IN-1 can inhibit cellular citrullination events. PADI4-IN-1 can be used for the research of inflammation, such as rheumatoid arthritis.

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

PADI4-IN-1

PADI4-IN-1 Chemical Structure

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Description

PADI4-IN-1 is a potent peptidylarginine deiminase isoform 4 (PADI4) inhibitor with an IC50 of 1.5 μM and SI (PADI1/PADI4) of 52.1. PADI4-IN-1 can inhibit cellular citrullination events. PADI4-IN-1 can be used for the research of inflammation, such as rheumatoid arthritis[1].

IC50 & Target[1]

PADI4

1.5 μM (IC50)

In Vitro

PADI4-IN-1 (Compound 7) (10-100 μM, 50 mins) decreases total cellular citrullination events and histone H3 citrullination mediated by PADI4 in HL-60 cell lysates[1].

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

Western Blot Analysis[1]

Cell Line: HL-60 cells
Concentration: 10 and 100 μM
Incubation Time:
Result: Decreased total HL-60 cellular citrullination events and histone H3 citrullination mediated by PADI4.
In Vivo

PADI4-IN-1 (Compound 7) (20 mg/kg, i.p., at days 3, 4, 5, 6, and 7) ameliorates the severity and pathologic progress in collagen type II antibody/LPS (HY-D1056) induced rheumatoid arthritis mice models[1].

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

Animal Model: Collagen type II antibody/LPS (HY-D1056) induced rheumatoid arthritis mice models[1]
Dosage: 20 mg/kg
Administration: Intraperitoneally injection
Result: Decreased the arthritis score of the mice by 66 % treated at days 4, 5, 6, and 7.
Decreased the arthritis score of the mice by 100 % treated at days 3 and 4.
Reduced the expression of IL-6, IL-1β, IFN-γ, RANKL, IL-17A, CXCL15, ANXA2, HIF-1α, iNOS, and TNF-αtreated at days 3 and 4.
Reduced inflammatory cell influx, pannus formation, cartilage destruction, cartilage remnant, edema, and accumulation of inflammatory cells (mononuclear cells and neutrophil).
Reduced the erosion of cartilage and bone.
Reduced the levels of citrullinated antigens.
Molecular Weight

337.41

Formula

C21H23NO3

SMILES

COC1=CC2=C(C(OC)=C1)OC3(N(C4=CC=CC=C4C3(C)C)C)C=C2

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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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:
PADI4-IN-1
Cat. No.:
HY-175518
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