Cat. No.: HY-100574

Cl-amidine

24 Cited Publications

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Based on 24 publication(s) in Google Scholar

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.

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CAS No.: 913723-61-2
Formule: C₁₄H₁₉ClN₄O₂
Masse moléculaire:310.78

Stockage:

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

Data Sheet (273 KB)

Cl-amidine Chemical Structure

CAS No.: 913723-61-2

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Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (24)
Pureté et documentation
Références
Calculators
Help & FAQs
Classifications
Bioz

Activité biologique

Description

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 mM 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 μM 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 (k_inact/K_I=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.

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.

Chemical Information

CAS No. 913723-61-2
Masse moléculaire 310.78
Formule C₁₄H₁₉ClN₄O₂
SMILES

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

Room temperature in continental US; may vary elsewhere.
Stockage

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

Publications (24)

All Bio/Physico-chemical AssayWBCell Proliferation/Viability AssayIHCIn Vivo Efficacy Study

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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
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 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.
Acta Pharm Sin B

2025 Sep 12.
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
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 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
J Hazard Mater

Interleukin-33 modulates NET formation via an autophagy-dependent manner to promote neutrophilic inflammation in cigarette smoke-exposure asthma. [Abstract]

2025 Apr 5:487:137257. PMID: 39842125

Cl-amidine purchased from MedChemExpress. Usage Cited in: J Hazard Mater. 2025 Apr 5:487:137257. [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.
Free Radic Biol Med

Neutrophil extracellular traps promote M1 macrophage polarization in gouty inflammation via targeting hexokinase-2. [Abstract]

2024 Nov 1:224:540-553. PMID: 39277122

Cl-amidine purchased from MedChemExpress. Usage Cited in: Free Radic Biol Med. 2024 Nov 1:224:540-553. [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 Nov 1:224:540-553. [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.
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
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
J Agric Food Chem

T-2 Toxin Induces Macrophage Extracellular Trap Formation via CLOCK-WNT10B-PAD2/ROS Signaling. [Abstract]

2026 Jun 10;74(22):17392-17404. PMID: 42207496
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
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
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
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 Pathog

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

Giardia duodenalis cysts induce bovine neutrophil extracellular trap formation. [Abstract]

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
Research Square Print

January 4th, 2023.

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (273 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[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]

[5]. Bryan Knuckley, et al. Substrate Specificity and Kinetic Studies of PADs 1, 3, and 4 Identify Potent and Selective Inhibitors of Protein Arginine Deiminase 3. Biochemistry. 2010 Jun 15;49(23):4852-63. [Content Brief]

Calculators

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

Cl-amidine

24 Cited Publications

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Cl-amidine

Publications Citing Use of MedChemExpress (MCE) Cl-amidine

Activité biologique

Chemical Information

Publications (24)

Pureté et documentation

Références

Calculators

Help & FAQs

Cl-amidine Related Classifications

HY-100574 Related Classifications