2. Epigenetics
  3. Protein Arginine Deiminase
  4. PAD4-IN-4

PAD4-IN-4 (compound 28) is a potent PAD4 inhibitor (IC50=0.79±0.09 μM). PAD4-IN-4 improves the tumor immune microenvironment by reshaping neutrophil phenotype, upregulating the proportions of dendritic cells and M1 macrophages, and reducing the amount of myeloid-derived suppressor cells. PAD4-IN-4 can be used for Triple-negative breast cancer research.

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

PAD4-IN-4

PAD4-IN-4 Chemical Structure

Size Stock
50 mg   Get quote  
100 mg   Get quote  
250 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

PAD4-IN-4 Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

PAD4-IN-4 (compound 28) is a potent PAD4 inhibitor (IC50=0.79±0.09 μM). PAD4-IN-4 improves the tumor immune microenvironment by reshaping neutrophil phenotype, upregulating the proportions of dendritic cells and M1 macrophages, and reducing the amount of myeloid-derived suppressor cells. PAD4-IN-4 can be used for Triple-negative breast cancer research[1].

IC50 & Target[1]

PAD4

0.79 μM (IC50)

PAD2

2.97 μM (IC50)

Cellular Effect
Cell Line Type Value Description References
4T1 IC50
2.39 μM
Compound: 28
Antiproliferative activity against mouse 4T1 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
Antiproliferative activity against mouse 4T1 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
[PMID: 38728549]
MCF-10A IC50
8.39 μM
Compound: 28
Cytotoxicity against human MCF-10A cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
Cytotoxicity against human MCF-10A cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
[PMID: 38728549]
MDA-MB-468 IC50
2.34 μM
Compound: 28
Antiproliferative activity against human MDA-MB-468 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
Antiproliferative activity against human MDA-MB-468 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
[PMID: 38728549]
In Vitro

PAD4-IN-4 displays substantial inhibitory activity toward PAD2 and PAD4 (IC50=2.97 ± 0.29 and 0.79 ± 0.09 μM), with the best PAD4 selectivity[1].
PAD4-IN-4 suppresses the proliferation of TNBC cells in vitro (4T1 IC50: 2.39 ± 0.54 μM; MDA-MB468 IC50: 2.34 ± 0.23 μM), with relatively low toxicity toward normal breast cells (MCF-10A IC50: 8.39 ± 0.60 μM)[1].
PAD4-IN-4 (0.5, 1, 2 μM; 48 h) has enhanced antimetastasis activity for TNBC cells[1].
PAD4-IN-4 (0.5, 1, 2 μM; 48 h) is a potent PAD4 inhibitor for blocking histone citrullination and neutrophil extracellular trap (NET) formation[1].

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

PAD4-IN-4 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: TNBC cells
Concentration: 0.5, 1, 2 μM
Incubation Time: 48 h
Result: Reduced the number of metastatic cells and wound closure rate less than that of 7 at the equivalent dose, indicating that compound 28 had enhanced antimetastasis activity.

Immunofluorescence[1]

Cell Line: TNBC cells and neutrophils
Concentration: 0.5, 1, 2 μM
Incubation Time: 48 h
Result: Inhibited histone citrullination and NET formation.
In Vivo

PAD4-IN-4 (1, 5, 10 mg/kg; i.v.; every 2 days for a total of nine times) can dosedependently suppress the lung metastasis of TNBC. PAD4-IN-4 is a promising candidate against TNBC without obvious toxicity in orthotopic 4T1-luc xenograft model in BALB/c mice[1].
PAD4-IN-4 alters the tumor microenvironment from a suppressive condition to an antitumor milieu by modulating the proportion of immune cells and reshaping the neutrophil phenotype and function[1].
Pharmacokinetic Analysis in Male Sprague−Dawley rats[1]

Compound Route Dose (mg/kg) AUC0_t (ng•h/mL) AUC0_INF (ng•h/mL) T1/2 (h) Tmax (h) Cmax (ng/mL) Cl (L•h/kg)
7 i.v. 3.5 14893.52 17214.17 0.13 0.08 251.2 571.87
28 i.v. 3.5 9525.86 17346.55 0.25 0.08 297.71 105.24

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

Animal Model: orthotopic 4T1-luc xenograft model in BALB/c mice[1].
Dosage: 1, 5, 10 mg/kg
Administration: Intravenous injection (i.v.)
Result: The tumor growth inhibition of the high-dose 28-treated group was 61.8%, whereas the positive control doxorubicin hydrochloride group reached 54.6%.
Had no significant differences in viscero−somatic ratio and serum biochemical indices (ALT, AST, UREA, and CREA-S) were observed in the 28-treated group.
Increased the proportion of mature TANs MHC-II+ TANs whereas it suppressed the proportion of pro-tumor phenotypes PD-L1+ /MHC-II+ TANs and MHC-II− TANs.
Molecular Weight

567.08

Formula

C32H31ClN6O2
SMILES

O=C(C1=CC2=C(C(C3=CC=CC=C3)=N1)NC4=C2C=CC=C4)N[C@H](C(NCC5=CC=CC=C5)=O)CCCNC(CCl)=N
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
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

PAD4-IN-4 Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2
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:

PAD4-IN-4Protein Arginine DeiminasePeptidylarginine DeiminasePAD4 InhibitorTriple-negative breast cancerTNBC cellsorthotopic 4T1-luc xenograft modelInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Requested Quantity *

Applicant Name *

 

Salutation

Email Address *

 

Phone Number *

Department

 

Organization Name *

City

State

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
PAD4-IN-4
Cat. No.:
HY-162494
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

SAFETY DATA SHEET (SDS)

Request for HNMR Report

We have received your request and will respond to you as soon as possible.