2. Epigenetics
  3. Protein Arginine Deiminase
  4. PADI4_3

PADI4_3 is a substrate-competitive and selective PADI4 inhibitor with an IC50 of 56 nM. PADI4_3 blocks citrullination of histone H3 and reduces the formation of neutrophil extracellular traps. PADI4_3 can be used in research related to autoimmune diseases and cancers.

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

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PADI4_3

PADI4_3 Chemical Structure

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PADI4_3 Related Antibodies

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Description

PADI4_3 is a substrate-competitive and selective PADI4 inhibitor with an IC50 of 56 nM. PADI4_3 blocks citrullination of histone H3 and reduces the formation of neutrophil extracellular traps. PADI4_3 can be used in research related to autoimmune diseases and cancers[1][2].

In Vitro

PADI4_3 binds specifically and with high affinity to the active conformation of recombinant PADI4 in the calcium-bound state (KD = 2.7 nM), and does not bind to the calcium-free inactive form or the active form with a blocked active site of this enzyme[1].
PADI4_3 (0.0003-100 μM) potently inhibits the activity of recombinant PADI4 in vitro, with an IC50 of 56 nM[1].
PADI4_3 (200 nM-100 μM; 4 h) exhibits cell permeability in HaLo-GFP-mito HeLa cells, with a CP50 of 1.4 μM at 37°C, and enters cells via an active transport mechanism[1].
PADI4_3 (0.1-1 μM; 3 h) inhibits PADI4 activity in mES cells stably expressing hPADI4, with an EC50 of 0.2 μM. At a concentration of 1 μM, it achieves complete inhibition without cytotoxicity[1].
PADI4_3 (50 μM; 60 min pre-incubation) reduces the citrullination level of histone H3 and the formation of neutrophil extracellular traps (NETosis) in human primary peripheral blood neutrophils stimulated by calcium ionophores, while the inactive control peptide PADI4_3i has no effect on these endpoints[1].
PADI4_3 potently inhibits the activity of recombinant PADI4 (IC50 = 56 nM) with high selectivity; it shows no inhibitory effect on other human PADI isozymes or mouse PADI4 even at concentrations up to 100 μM[2].

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

PADI4_3 Related Antibodies

Immunofluorescence[1]

Cell Line: human PADI4-stable mouse embryonic stem (hPADI4-stable mES) cells
Concentration: 0.1-1 μM
Incubation Time: 3 h
Result: Inhibited intracellular PADI4 activity in a dose-dependent manner, with an EC50 of 0.2 μM.
Achieved complete inhibition at 1 μM.
Showed no cytotoxicity with treatment.
Inactive control peptide PADI4_3i showed no inhibition.
Molecular Weight

1770.93

Formula

C79H107N27O19S
Sequence

{dTyr}-Arg-Asp-His-His-Tyr-Arg-His-Pro-Lys-Tyr-Cys-Gly-NH2 (thioether bond:dTyr1-Cys12)
Sequence Shortening

{dTyr}-RDHHYRHPKYCG-NH2 (thioether bond:dTyr1-Cys12)
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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PADI4_3 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:

PADI4_3Protein Arginine DeiminasePeptidylarginine Deiminasepeptidylarginine deiminase IVautoimmunityneutrophil extracellular trap formationhPADI4-stable mES cellsmouse PADI4human PADI4primary human peripheral neutrophilscancerHaLo-GFP-mito HeLa cellshistone H3 citrullinationInhibitorinhibitorinhibit

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