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

Cl-amidine 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 induces apoptosis in cancer cells. Cl-amidine induces microRNA (miR)-16 (miRNA-16, microRNA-16) expression and causes cell cycle arrest. Cl-Amidine prevents histone 3 citrullination and neutrophil extracellular trap formation, and improves survival in a murine sepsis model.

The free form of the compound is prone to instability, it is advisable to consider the stable salt form (Cl-amidine hydrochloride) that retains the same biological activity.

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CAS No. : 913723-61-2

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Cl-amidine Related Antibodies

Top Publications Citing Use of Products

    Cl-amidine 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 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 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 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 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

    • 순도&문서

    • References

    • 고객리뷰

    제품 설명

    Cl-amidine 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 induces apoptosis in cancer cells. Cl-amidine induces microRNA (miR)-16 (miRNA-16, microRNA-16) expression and causes cell cycle arrest. Cl-Amidine 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].
    Cellular Effect
    Cell Line Type Value Description References
    U2OS EC50
    160 2
    Compound: CI-amidine
    Cytotoxicity against human U2OS cells assessed as reduction in cell viability by CellTiter 96 non-radioactive cell proliferation assay
    Cytotoxicity against human U2OS cells assessed as reduction in cell viability by CellTiter 96 non-radioactive cell proliferation assay
    		[PMID: 32631569]
    U2OS EC50
    160 3
    Compound: Cl-amidine
    Antiproliferative activity against human U2OS cells expressing PAD4 assessed as cell viability after 72 hrs by XTT assay
    Antiproliferative activity against human U2OS cells expressing PAD4 assessed as cell viability after 72 hrs by XTT assay
    		[PMID: 25559347]
    U2OS EC50
    160 2
    Compound: CI-amidine
    Cytotoxicity against human U2OS cells assessed as reduction in cell viability by CellTiter 96 non-radioactive cell proliferation assay
    Cytotoxicity against human U2OS cells assessed as reduction in cell viability by CellTiter 96 non-radioactive cell proliferation assay
    		[PMID: 32631569]
    U2OS EC50
    160 3
    Compound: Cl-amidine
    Antiproliferative activity against human U2OS cells expressing PAD4 assessed as cell viability after 72 hrs by XTT assay
    Antiproliferative activity against human U2OS cells expressing PAD4 assessed as cell viability after 72 hrs by XTT assay
    		[PMID: 25559347]
    U2OS EC50
    160 2
    Compound: CI-amidine
    Cytotoxicity against human U2OS cells assessed as reduction in cell viability by CellTiter 96 non-radioactive cell proliferation assay
    Cytotoxicity against human U2OS cells assessed as reduction in cell viability by CellTiter 96 non-radioactive cell proliferation assay
    		[PMID: 32631569]
    U2OS EC50
    160 3
    Compound: Cl-amidine
    Antiproliferative activity against human U2OS cells expressing PAD4 assessed as cell viability after 72 hrs by XTT assay
    Antiproliferative activity against human U2OS cells expressing PAD4 assessed as cell viability after 72 hrs by XTT assay
    		[PMID: 25559347]
    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 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.
    분자량

    310.78

    화학식

    C14H19ClN4O2
    CAS No.
    SMILES

    O=C(N[C@H](C(N)=O)CCCNC(CCl)=N)C1=CC=CC=C1
    선적

    Room temperature in continental US; may vary elsewhere.
    보관

    Please store the product under the recommended conditions in the Certificate of Analysis.
    순도&문서
    References
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    Cl-amidine Related Classifications

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      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-amidine913723-61-2Protein Arginine DeiminaseApoptosisMicroRNAPeptidylarginine DeiminasemiRNAcolitissepsismiR-16miRNA-16microRNA-16Inhibitorinhibitorinhibit

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