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.
- Formula: C21H23NO3
- Molecular Weight:337.41
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
|
PADI4 1.5 μM (IC50) |
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.
-
Cell Line:HL-60 cells
-
Concentration:10 and 100 μM
-
Incubation Time:50 mins
-
Result:Decreased total HL-60 cellular citrullination events and histone H3 citrullination mediated by PADI4.
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.
Chemical Information
-
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
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)