1. Epigenetics
  2. Protein Arginine Deiminase

Cl-amidine 

Cat. No.: HY-100574
Handling Instructions

Cl-amidine is a peptidylarginine deminase (PAD) inhibitor, with an IC50 5.9 μM for PAD4.

For research use only. We do not sell to patients.

Cl-amidine Chemical Structure

Cl-amidine Chemical Structure

CAS No. : 913723-61-2

Size Stock
250 mg Get quote
500 mg Get quote

* Please select Quantity before adding items.

Customer Review

Featured Recommendations

Related Small Molecules:

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

Cl-amidine is a peptidylarginine deminase (PAD) inhibitor, with an IC50 5.9 μM for PAD4.

IC50 & Target

IC50: 5.9 μM (PAD4)[1].

In Vitro

Cl-amidine is a peptidylarginine deminase (PAD) inhibitor, with an IC50 5.9±0.3 μM for PAD4 and 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 induces apoptosis (identified as annexin V-positive/propidium iodide-negative cells) in such cells in a dose-dependent manner, indicating that Cl-amidine induces apoptosis of WBCs in vitro. Interestingly, the colon cancer cell line (HT29) is relatively resistant to apoptosis caused by Cl-amidine[2].

In Vivo

Significantly higher levels of colon inflammation in the 2% DSS than the 2% DSS+Cl-amidine mice are showed. The mean histology scores are 24.2±1.7 (SE) and 13.9±1.6, respectively. Most of the damage in the DSS-only group is in the distal colon, and this damage is suppressed with DSS+Cl-amidine. For the DSS-treated group, the mean colon length is 7.2±0.2 cm. In contrast, the average colon length of the DSS+Cl-amidine group is 8.4±0.2 cm, which is comparable to the mean colon lengths obtained for the wateralone and water+Cl-amidine groups (8.4±0.3 and 7.9±0.2 cm, respectively). The total distance and average speed of mice over a 96-h period are also measured. The results of these analyses demonstrate that the total distance is 5,072±381 and 3,190±401 m for the water-treated and DSS+Cl-amidine mice, but only 800±163 m for the DSS-only group. Similarly, the average speed on the wheel over the 4-day period is 6.2±0.63 and 5.3±0.58 m/min for the water-treated and DSS+Cl-amidine groups, but only 1.8±0.51 m/min for the DSS group. The finding that Cl-amidine improves the speed and distance traveled by the mice is consistent with the histology and colon length data and demonstrates overall improved health, further demonstrating the efficacy of this compound in treating DSS-induced colitis[2].

Solvent & Solubility
In Vitro: 

10 mM in DMSO

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.2177 mL 16.0886 mL 32.1771 mL
5 mM 0.6435 mL 3.2177 mL 6.4354 mL
10 mM 0.3218 mL 1.6089 mL 3.2177 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Cell Assay
[2]

TK6 cells are a lymphoblastoid cell line derived from the spleen >30 years ago. HT29 cells are a colon cancer cell line, with mutant p53. TK6 lymphoblastoid cells and HT29 colon cancer cells are cultured with Cl-amidine in a dose-dependent manner (0, 5, 10, 15, 20, 25, 50 μg/mL) over 24 h. Apoptosis is assessed by annexin V/propidium iodide staining followed by flow cytometry[2].

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

Animal Administration
[2]

Mice[2]
C57BL/6 mice (8-12 wk old) are fed a standard AIN 93M diet. For this DSS mouse model of colitis, mice receive water ad libitum or 2% DSS beginning at day 0 [for oral gavage/treatment experiment or day 7 [for intraperitoneal/prevention experiment. Initial experiments used injections of Cl-amidine (75 mg/kg-1/day-1 ip), beginning concomitantly with the initiation of 2% DSS in the drinking water. This dose is chosen based on results in a RA model that used 100 mg/kg-1/day-1 without overt side effects and without immunosuppressive outcomes. In DSS model, 50 mice in 4 groups are examined, and inflammation scores are recorded[2].

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

References
Molecular Weight

310.78

Formula

C₁₄H₁₉ClN₄O₂

CAS No.

913723-61-2

SMILES

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

Storage

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

Shipping

Room temperature in continental US; may vary elsewhere

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Inquiry Online

Your information is safe with us. * Required Fields.

Product name

 

Salutation

Applicant name *

 

Email address *

Phone number *

 

Organization name *

Country or Region *

 

Requested quantity *

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
Cl-amidine
Cat. No.:
HY-100574
Quantity:

Cl-amidine

Cat. No.: HY-100574