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

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 (miRNA-16, microRNA-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.

CAS No. : 1043444-18-3

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Based on 22 publication(s) in Google Scholar

Other Forms of Cl-amidine TFA:

Cl-amidine TFA Related Antibodies

Top Publications Citing Use of Products

    Cl-amidine TFA purchased from MedChemExpress. Usage Cited in: Exp Mol Med. 2024 Dec;56(12):2602-2616.  [Abstract]

    NET-DNA levels produced by RA neutrophils pretreated with 10 μM DPI, 10 μM Cl-Amidine or 20 μM sivelestat for 1 h prior to stimulation with 100 ng/mL IL-33 or 40 nM PMA for 4 h.

    Cl-amidine TFA purchased from MedChemExpress. Usage Cited in: J Hazard Mater. 2025 Jan 16:487:137257.  [Abstract]

    In the co-culture, inhibiting NET formation (treated with 200 μM Cl-amidine for 15 min) downregulated the HIF-1αpathway and upregulated p-mTOR, while stimulating NETs (treated with 100 nM PMA for 3 h) had the opposite effect.

    Cl-amidine TFA purchased from MedChemExpress. Usage Cited in: MedComm (2020). 2025 Jan 30;6(2):e70084.  [Abstract]

    Inhibition of OMV release with Cl-amidine, a protein arginine deiminase inhibitor, significantly reversed the reinforcing effect of lactate-adjusted low-pH conditions on the P. aeruginosa LL-37 resistance

    Cl-amidine TFA purchased from MedChemExpress. Usage Cited in: Free Radic Biol Med. 2024 Sep 12:S0891-5849(24)00656-7.  [Abstract]

    GA mice were pretreated with DNase I or Cl-Amidine (a PAD4 inhibitor). Elevated NETs (marked with histone H3 and MPO) in GA mice were significantly reduced after treatment with DNase I or Cl-Amidine (50 mg/kg, ip).

    Cl-amidine TFA purchased from MedChemExpress. Usage Cited in: Free Radic Biol Med. 2024 Sep 12:S0891-5849(24)00656-7.  [Abstract]

    Based on the analysis of the ankle swelling index, the swelling index was significantly increased in the MSU group when compared with the control group. DNase I or Cl-Amidine (50 mg/kg, ip) treatment significantly reduced the swelling index in GA mice.

    • 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 (miRNA-16, microRNA-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].

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

    Cl-amidine TFA Related Antibodies

    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].

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

    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.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C(N[C@H](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

    -20°C, sealed storage, away from moisture and light

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

    Solvent & Solubility
    In Vitro: 

    DMSO : 6.67 mg/mL (15.70 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.3540 mL 11.7702 mL 23.5405 mL
    5 mM 0.4708 mL 2.3540 mL 4.7081 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    • Molarity Calculator

    • Dilution Calculator

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

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

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    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 0.67 mg/mL (1.58 mM); Clear solution

      This protocol yields a clear solution of ≥ 0.67 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (6.7 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 0.67 mg/mL (1.58 mM); Clear solution

      This protocol yields a clear solution of ≥ 0.67 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (6.7 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation
    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.3540 mL 11.7702 mL 23.5405 mL 58.8512 mL
    5 mM 0.4708 mL 2.3540 mL 4.7081 mL 11.7702 mL
    10 mM 0.2354 mL 1.1770 mL 2.3540 mL 5.8851 mL
    15 mM 0.1569 mL 0.7847 mL 1.5694 mL 3.9234 mL
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    Cl-amidine TFA Related Classifications

    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:

    Cl-amidine1043444-18-3Protein Arginine DeiminaseApoptosisMicroRNAPeptidylarginine DeiminasemiRNAcolitissepsismiR-16miRNA-16microRNA-16Inhibitorinhibitorinhibit

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