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

Cl-amidine hydrochloride 

Cat. No.: HY-100574A Purity: >95.0%
Handling Instructions

Cl-amidine hydrochloride 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 hydrochloride induces apoptosis in cancer cells. Cl-amidine hydrochloride induces microRNA (miR)-16 expression and causes cell cycle arrest. Cl-Amidine hydrochloride 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 hydrochloride Chemical Structure

Cl-amidine hydrochloride Chemical Structure

CAS No. : 1373232-26-8

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 132 In-stock
Estimated Time of Arrival: December 31
5 mg USD 120 In-stock
Estimated Time of Arrival: December 31
10 mg USD 190 In-stock
Estimated Time of Arrival: December 31
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Description

Cl-amidine hydrochloride 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 hydrochloride induces apoptosis in cancer cells. Cl-amidine hydrochloride induces microRNA (miR)-16 expression and causes cell cycle arrest. Cl-Amidine hydrochloride 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 prevents histone 3 citrullination and neutrophil extracellular trap formation, and improves survival in a murine sepsis model[4].

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

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].

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

347.24

Formula

C₁₄H₂₀Cl₂N₄O₂

CAS No.

1373232-26-8

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

H2O : 50 mg/mL (143.99 mM; Need ultrasonic)

DMSO : 19.23 mg/mL (55.38 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.8799 mL 14.3993 mL 28.7985 mL
5 mM 0.5760 mL 2.8799 mL 5.7597 mL
10 mM 0.2880 mL 1.4399 mL 2.8799 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  PBS

    Solubility: 5.5 mg/mL (15.84 mM); Clear solution; Need ultrasonic

*All of the co-solvents are provided by MCE.
References
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Keywords:

Cl-amidineProtein Arginine DeiminaseApoptosisMicroRNAPeptidylarginine DeiminasemiRNAInhibitorinhibitorinhibit

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Cl-amidine hydrochloride
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