1. Epigenetics
    Apoptosis
  2. Protein Arginine Deiminase
    Apoptosis
    MicroRNA
  3. Cl-amidine TFA

Cl-amidine TFA 

Cat. No.: HY-100574B
Handling Instructions

Cl-amidine TFA is an orally active peptidylarginine deminase (PAD) inhibitor, with IC50 values of 0.8 μM, 6.2 μM and 5.9 μM for PAD1, PAD3, and PAD4, respectively. Cl-amidine TFA induces apoptosis in cancer cells. Cl-amidine TFA induces microRNA (miR)-16 expression and causes cell cycle arrest. Cl-Amidine TFA prevents histone 3 citrullination and neutrophil extracellular trap formation, and improves survival in a murine sepsis model.

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

Cl-amidine TFA Chemical Structure

Cl-amidine TFA Chemical Structure

CAS No. : 1043444-18-3

Size Stock
100 mg   Get quote  
250 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Other In-stock Forms of Cl-amidine TFA:

Other Forms of Cl-amidine TFA:

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Cl-amidine TFA is an orally active peptidylarginine deminase (PAD) inhibitor, with IC50 values of 0.8 μM, 6.2 μM and 5.9 μM for PAD1, PAD3, and PAD4, respectively. Cl-amidine TFA induces apoptosis in cancer cells. Cl-amidine TFA induces microRNA (miR)-16 expression and causes cell cycle arrest. Cl-Amidine TFA prevents histone 3 citrullination and neutrophil extracellular trap formation, and improves survival in a murine sepsis model[1][2][3][4][5].

IC50 & Target

IC50: 0.8 μM (PAD1), 5.9 μM (PAD4), 6.2 μM (PAD3)[1][5].

In Vitro

Cl-amidine is a bioavailable haloacetamidine-based compound that inhibits all the active PAD isozymes with near equal potency (kinact/KI=13,000 M-1•min-1 for PAD4)[1].
Cl-amidine (0, 5, 10, 15, 20, 25, 50 μg/mL, 24 hours) induces apoptosis in TK6 lymphoblastoid cells and HT29 colon cancer cells in a dose-dependent manner. Interestingly, the colon cancer cell line (HT29) is relatively resistant to apoptosis caused by Cl-amidine[2].
Cl-amidine irreversibly inactivates PADs by covalently modifying an active site cysteine that is important for its catalytic activity[4].

Apoptosis Analysis[2].

Cell Line: TK6 lymphoblastoid cells and HT29 colon cancer cells.
Concentration: 0, 5, 10, 15, 20, 25, 50 μg/mL.
Incubation Time: 24 h.
Result: Induced apoptosis dose-dependently.
In Vivo

Cl-amidine (75 mg/kg, ip once daily) suppresses and treats DSS-induced colitis in mice[2].
Cl-amidine (5, 25, 75 mg/kg, oral gavage, once daily) leads to significant reductions in the histology scores dose-dependently[2].

Animal Model: C57BL/6 mice (8-12 wk old, DSS mouse model of colitis)[2].
Dosage: 75 mg/kg.
Administration: IP once daily.
Result: Suppressed PAD activity, protein citrullination, and PAD levels in the colon in vivo.
Animal Model: C57BL/6 mice (8-12 wk old, DSS mouse model of colitis)[2].
Dosage: 5, 25, 75 mg/kg.
Administration: Oral gavage once daily.
Result: Led to significant reductions in the histology scores.
Molecular Weight

424.80

Formula

C₁₆H₂₀ClF₃N₄O₄

CAS No.

1043444-18-3

SMILES

O=C(N[[email protected]](C(N)=O)CCCNC(CCl)=N)C1=CC=CC=C1.O=C(O)C(F)(F)F

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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.
  • 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

Keywords:

Cl-amidineProtein Arginine DeiminaseApoptosisMicroRNAPeptidylarginine DeiminasemiRNAcolitissepsisInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product name

 

Salutation

Applicant name *

 

Email address *

Phone number *

 

Organization name *

Country or Region *

 

Requested quantity *

Remarks

Bulk Inquiry

Inquiry Information

Product name:
Cl-amidine TFA
Cat. No.:
HY-100574B
Quantity:
MCE Japan Authorized Agent: