Cl-amidine hydrochloride
Based on 24 publication(s) in Google Scholar
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 (miRNA-16, microRNA-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.
- Purity: 99.82%
- CAS No.: 1373232-26-8
- Formula: C14H20Cl2N4O2
- Molecular Weight:347.24
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Storage:
-20°C, stored under nitrogen, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Apoptosis Compound Library
HY-L003
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HY-L005
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HY-L005M
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Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library
HY-L199
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HY-L907
Publications Citing Use of MedChemExpress (MCE) Cl-amidine hydrochloride
More- Eur Heart J. 2025 Oct 27:ehaf836. [Abstract]
- Nat Biomed Eng. 2024 Sep;8(9):1177-1190. [Abstract]
- Acta Pharm Sin B. 2025 Sep 12.
- Adv Sci (Weinh). 2026 Apr;13(20):e15431. [Abstract]
- Exp Mol Med. 2024 Dec;56(12):2602-2616. [Abstract]
- J Hazard Mater. 2025 Jan 16:487:137257. [Abstract]
- MedComm (2020). 2025 Jan 30;6(2):e70084. [Abstract]
- Free Radic Biol Med. 2024 Sep 12:S0891-5849(24)00656-7. [Abstract]
- Neoplasia. 2022 Nov;33:100835. [Abstract]
- Cell Rep. 2021 Sep 21;36(12):109750. [Abstract]
- J Agric Food Chem. 2026 Jun 10;74(22):17392-17404.
- Transl Res. 2023 May:255:85-96. [Abstract]
- Chin Med. 2026 Jan 4;21(1):1. [Abstract]
- Int Immunopharmacol. 2026 Jan 1;168(Pt 1):115862. [Abstract]
- J Inflamm Res. 2026 Mar 20:19:569462. [Abstract]
- J Inflamm Res. 2026 Feb 13:19:557809. [Abstract]
- Fish Shellfish Immunol. 2022 Oct:129:22-29. [Abstract]
- Chem Res Toxicol. 2022 Apr 18;35(4):597-605. [Abstract]
- Microb Pathogenesis. 2020 Dec;149:104530. [Abstract]
- Immun Inflamm Dis. 2025 Nov;13(11):e70268. [Abstract]
- Microvasc Res. 2023 Nov:150:104592. [Abstract]
- Vet Parasitol. 2026 May:344:110769. [Abstract]
- Vet Parasitol. 2022 Dec:312:109841. [Abstract]
- Research Square Print. January 4th, 2023.
Customer Validation & Images
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Bio/Physico-chemical Assay
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WB
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Cell Proliferation/Viability Assay
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IHC
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In Vivo Efficacy Study
Biological Activity
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:TK6 lymphoblastoid cells and HT29 colon cancer cells.
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Concentration:0, 5, 10, 15, 20, 25, 50 μg/mL.
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Incubation Time:24 h.
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Result:Induced apoptosis dose-dependently.
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.
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Animal Model:C57BL/6 mice (8-12 wk old, DSS mouse model of colitis)[2].
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Dosage:75 mg/kg.
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Administration:IP once daily.
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Result:Suppressed PAD activity, protein citrullination, and PAD levels in the colon in vivo.
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Animal Model:C57BL/6 mice (8-12 wk old, DSS mouse model of colitis)[2].
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Dosage:5, 25, 75 mg/kg.
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Administration:Oral gavage once daily.
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Result:Led to significant reductions in the histology scores.
Chemical Information
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CAS No. 1373232-26-8
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Appearance Solid
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Molecular Weight 347.24
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Formula C14H20Cl2N4O2
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Color White to light yellow
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SMILES
O=C(N[C@H](C(N)=O)CCCNC(CCl)=N)C1=CC=CC=C1.[H]Cl
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
-20°C, stored under nitrogen, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture)
Publications (24)
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Journal Impact Factor
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Most Recent
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Eur Heart J
Targeting P2Y14R alleviates platelet-induced NET formation and venous thrombosis through PKA/AKAP13/RhoA axis. [Abstract]2025 Oct 27:ehaf836. PMID: 41143464 -
Nat Biomed Eng
Bacteria-mediated resistance of neutrophil extracellular traps to enzymatic degradation drives the formation of dental calculi. [Abstract]2024 Sep;8(9):1177-1190. PMID: 38491329 -
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Adv Sci (Weinh)
pH/ROS-Responsive Injectable Hydrogel Co-Loaded with B7-H3 Blocker and NETs Suppressor Boosts OSCC Synergistic Immunotherapy. [Abstract]2026 Apr;13(20):e15431. PMID: 41684277 -
Exp Mol Med
IL33-induced neutrophil extracellular traps (NETs) mediate a positive feedback loop for synovial inflammation and NET amplification in rheumatoid arthritis. [Abstract]2024 Dec;56(12):2602-2616. PMID: 39617790
Cl-amidine hydrochloride 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.
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J Hazard Mater
Interleukin-33 modulates NET formation via an autophagy-dependent manner to promote neutrophilic inflammation in cigarette smoke-exposure asthma. [Abstract]2025 Jan 16:487:137257. PMID: 39842125
Cl-amidine hydrochloride 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.
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MedComm (2020)
Outer membrane vesicle contributes to the Pseudomonas aeruginosa resistance to antimicrobial peptides in the acidic airway of bronchiectasis patients. [Abstract]2025 Jan 30;6(2):e70084. PMID: 39896756
Cl-amidine hydrochloride 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
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Free Radic Biol Med
Neutrophil extracellular traps promote M1 macrophage polarization in gouty inflammation via targeting hexokinase-2. [Abstract]2024 Sep 12:S0891-5849(24)00656-7. PMID: 39277122
Cl-amidine hydrochloride 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 hydrochloride 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.
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Neoplasia
PAD4-dependent citrullination of nuclear translocation of GSK3β promotes colorectal cancer progression via the degradation of nuclear CDKN1A. [Abstract]2022 Nov;33:100835. PMID: 36113195 -
Cell Rep
Inappropriate use of antibiotics exacerbates inflammation through OMV-induced pyroptosis in MDR Klebsiella pneumoniae infection. [Abstract]2021 Sep 21;36(12):109750. PMID: 34551309 -
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Transl Res
Neutrophil Extracellular Traps Induce Abdominal Aortic Aneurysm Formation by Promoting the Synthetic and Proinflammatory Smooth Muscle Cell Phenotype via Hippo-YAP Pathway. [Abstract]2023 May:255:85-96. PMID: 36435329 -
Chin Med
Fuzheng Jiedu formula attenuates acute pneumonia by coordinated regulation of macrophage NLRP3 inflammasome and neutrophil NETs. [Abstract]2026 Jan 4;21(1):1. PMID: 41484909 -
Int Immunopharmacol
Inhibition of neutrophil infiltration and NETosis ameliorates sepsis-induced cardiac injury and reduces myocardial inflammation and apoptosis. [Abstract]2026 Jan 1;168(Pt 1):115862. PMID: 41248570 -
J Inflamm Res
Fire Needling Acupuncture Reduces Neutrophil Extracellular Traps (NETs) Formation and Inhibits TLR4/NF-κB/LCN2 Pathway in Psoriasis-Like Skin Lesions. [Abstract]2026 Mar 20:19:569462. PMID: 41907203 -
J Inflamm Res
Standardized Extract of Flavonoids from Smilax glabra Alleviates Gouty Arthritis by Multi-Target Inhibition of Neutrophil Extracellular Traps via the Raf/ERK and Histone Citrullination Pathways. [Abstract]2026 Feb 13:19:557809. PMID: 41709965 -
Fish Shellfish Immunol
Zinc oxide nanoparticles (ZnO-NPs) exhibit immune toxicity to crucian carp (Carassius carassius) by neutrophil extracellular traps (NETs) release and oxidative stress. [Abstract]2022 Oct:129:22-29. PMID: 35932984 -
Chem Res Toxicol
Polychlorinated Biphenyl Quinone Metabolites Cause Neutrophil Extracellular Traps in Mouse Bone Marrow Neutrophils. [Abstract]2022 Apr 18;35(4):597-605. PMID: 35168318 -
Microb Pathogenesis
Cl-amidine attenuates lipopolysaccharide-induced mouse mastitis by inhibiting NF-κB, MAPK, NLRP3 signaling pathway and neutrophils extracellular traps release. [Abstract]2020 Dec;149:104530. PMID: 32980473 -
Immun Inflamm Dis
Neutrophil Extracellular Traps Activate Meningeal Fibroblast to Aggravate Subarachnoid Fibrosis in Kaolin-Induced Hydrocephalus in Rats. [Abstract]2025 Nov;13(11):e70268. PMID: 41236114 -
Microvasc Res
Light-induced circadian rhythm disorder leads to microvascular dysfunction via up-regulating NETs. [Abstract]2023 Nov:150:104592. PMID: 37567437 -
Vet Parasitol
2026 May:344:110769. PMID: 41967379 -
Vet Parasitol
Giardia duodenalis trophozoites triggered bovine neutrophil extracellular traps formation dependent on P2X1 receptor and PAD4 in vitro. [Abstract]2022 Dec:312:109841. PMID: 36427458 -
Solvent & Solubility
DMSO : 50 mg/mL (143.99 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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 (stored under nitrogen, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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 (stored under nitrogen, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 1.25 mg/mL (3.60 mM); Clear solution
This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 1.25 mg/mL (3.60 mM); Clear solution
This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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.
Add each solvent one by one: PBS
Solubility: 5.5 mg/mL (15.84 mM); Clear solution; Need ultrasonic
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 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 (stored under nitrogen, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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
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Data Sheet (278 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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Handling Instructions (2659 KB)
References
[1]. Yuan Luo, et al. Inhibitors and Inactivators of Protein Arginine Deiminase 4: Functional and Structural Characterization. Biochemistry. 2006 Oct 3; 45(39): 11727–11736. [Content Brief]
[2]. Chumanevich AA, et al. Suppression of colitis in mice by Cl-amidine: a novel peptidylarginine deiminase inhibitor. Am J Physiol Gastrointest Liver Physiol. 2011 Jun;300(6):G929-38. [Content Brief]
[3]. Witalison EE, et al. Molecular targeting of protein arginine deiminases to suppress colitis and prevent colon cancer. Oncotarget. 2015 Nov 3;6(34):36053-62. [Content Brief]
[4]. Biron BM, et al., Cl-Amidine Prevents Histone 3 Citrullination and Neutrophil Extracellular Trap Formation, and Improves Survival in a Murine Sepsis Model. J Innate Immun. 2017;9(1):22-32. [Content Brief]
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 (stored under nitrogen, away from moisture). 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 | 2.8799 mL | 14.3993 mL | 28.7985 mL | 71.9963 mL |
| 5 mM | 0.5760 mL | 2.8799 mL | 5.7597 mL | 14.3993 mL | |
| 10 mM | 0.2880 mL | 1.4399 mL | 2.8799 mL | 7.1996 mL | |
| 15 mM | 0.1920 mL | 0.9600 mL | 1.9199 mL | 4.7998 mL | |
| 20 mM | 0.1440 mL | 0.7200 mL | 1.4399 mL | 3.5998 mL | |
| 25 mM | 0.1152 mL | 0.5760 mL | 1.1519 mL | 2.8799 mL | |
| 30 mM | 0.0960 mL | 0.4800 mL | 0.9600 mL | 2.3999 mL | |
| 40 mM | 0.0720 mL | 0.3600 mL | 0.7200 mL | 1.7999 mL | |
| 50 mM | 0.0576 mL | 0.2880 mL | 0.5760 mL | 1.4399 mL | |
| 60 mM | 0.0480 mL | 0.2400 mL | 0.4800 mL | 1.1999 mL | |
| 80 mM | 0.0360 mL | 0.1800 mL | 0.3600 mL | 0.9000 mL | |
| 100 mM | 0.0288 mL | 0.1440 mL | 0.2880 mL | 0.7200 mL |
Cl-amidine hydrochloride Related Classifications
HY-100574A Related Classifications
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