In Vivo (Add solvents to the product individually and in order.)
Homogeneous suspension
CMC-NA
≥5mg/ml
Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)
Preparing Stock Solutions
Biological Activity
Description
Cl-amidine is an irreversible pan-peptidylarginine deiminase (PAD) inhibitor with IC50 values of 5.9
0.3
M, 0.8
0.3
M, 6.2
1.0
M for PAD4, PAD1 and PAD3, respectively. Cl-amidine induces apoptosis.
Targets
PAD1 (Cell-free assay)
PAD4 (Cell-free assay)
PAD3 (Cell-free assay)
0.8 μM
5.9 μM
6.2 μM
In vitro
Cl-amidine antagonizes the PAD4-mediated enhancement of the the p300GBD-GRIP1 interaction in a dose-dependent manner. The inhibitory effect of this compound is not a nonspecific one but is targeted at the active PAD4 enzyme. This compound increases p53 expression in CD45 positive immune cells. It triggers the differentiation and apoptosis of multiple cancer cell lines that are p53+/+ and p53
(e.g., HL60, HT29, TK6, and U2-OS cells). This chemical induces the expression of p53 and several downstream target genes including the cyclin dependent kinase inhibitor p21, GADD45, and the proapoptotic protein PUMA in U2-OS osteosarcoma cells.
In Vivo
Cl-amidine treatment inhibits NZM(New Zealand mixed 2328) NET(neutrophil extracellular trap) formation in vivo and significantly alters circulating autoantibody profiles and complement levels while reducing glomerular IgG deposition. Further, this compound increases the differentiation capacity of bone marrow endothelial progenitor cells, improves endothelium-dependent vasorelaxation, and markedly delays time to arterial thrombosis induced by photochemical injury. It delays thrombosis development in NZM mice. This chemical inhibits PADs in mice without significant toxicity and improves disease phenotypes in animal models of inflammatory arthritis and inflammatory bowel disease. And it is shown to reduce disease severity in mouse models of ulcerative colitis and RA.
CV-1 cells are transiently transfected with plasmids encoding a luciferase reporter construct, p300GBD fused to the Gal4 DNA binding domain, the p300 binding domain of GRIP1 (i.e., the AD1 domain) fused to the VP16 activation domain (AD), and either wild-type PAD4 or the catalytically defective C645S mutant. Cl-amidine (0-200 μM) is then added to the cell culture medium and incubated for 40 h. Cell extracts are then prepared, and the luciferase activity present in these extracts is quantified.
Moxibustion-mediated alleviation of synovitis in rats with rheumatoid arthritis through the regulation of NLRP3 inflammasome by modulating neutrophil extracellular traps
[ Heliyon, 2024, 10(1):e23633]
Constraint-induced movement therapy alleviates motor impairment by inhibiting the accumulation of neutrophil extracellular traps in ischemic cortex
[ Neurobiol Dis, 2023, 179:106064]
RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.
SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.
NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.
