Home Immunology & Inflammation Immunology & Inflammation related chemical - PAD inhibitor - Apoptosis related activator Cl-amidine

Cl-amidine

Catalog No.S8141

For research use only.

Cl-amidine is an irreversible pan-peptidylarginine deiminase (PAD) inhibitor with IC50 values of 5.9 ± 0.3 μM, 0.8 ± 0.3 μM, 6.2 ± 1.0 μM for PAD4, PAD1 and PAD3, respectively. Cl-amidine induces apoptosis.

Cl-amidine Chemical Structure

CAS No. 1043444-18-3

Selleck's Cl-amidine has been cited by 12 Publications

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Biological Activity

Description Cl-amidine is an irreversible pan-peptidylarginine deiminase (PAD) inhibitor with IC50 values of 5.9 ± 0.3 μM, 0.8 ± 0.3 μM, 6.2 ± 1.0 μM for PAD4, PAD1 and PAD3, respectively. Cl-amidine induces apoptosis.
Targets
PAD1 [1]
(Cell-free assay)		 PAD4 [1]
(Cell-free assay)		 PAD3 [1]
(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[1]. Cl-amidine 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). Cl-amidine 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[2].
Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
MDA-MB-231 NX7VXHFES3m2b4TvfIlkcXS7IHHzd4F6 MnHiOFAxKHWP NGC0XFQ6PiCqcoO= MmTvR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUWRCNU2ELUKzNUBk\WyuczDhd5Nme3OnZDDhd{Bl\WO{ZXHz[UBqdiClZXzsJI52dWKncjDheEA1ODBidV2gZYZ1\XJiOU[gbJJ{KGK7IITyfZBidiCkbIXlJIF{e2G7 NFTjdo49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{SyNFYzPCd-MkO0NlA3OjR:L3G+
MDA-MB-231 NFPvdGREgXSxdH;4bYNqfHliYYPzZZk> M2rrRlIxOCC2bzC0NFAhfU1? MnPNPVYhcHK| MmPQR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUWRCNU2ELUKzNUBk\WyuczDhd5Nme3OnZDDhd{Bl\WO{ZXHz[UBqdiClZXzsJJZq[WKrbHn0fUBifCB{MECgeI8hPDByIIXNJIFnfGW{IEm2JIhzeyCkeTD0dplx[W5iYnz1[UBie3OjeR?= NIXZPW09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{SyNFYzPCd-MkO0NlA3OjR:L3G+
HL60 NWT6O3M4TnWwY4Tpc44h[XO|YYm= MV21JJRwKDFyIIXN NIPTRYoyPSCvaX7z NUn0UXk4UW6qaXLpeIlwdiCxZjDQRWQ1KGmwIHj1cYFvKEiONkCgZ4VtdHNiYYPz[ZN{\WRiYYOgdoVlfWO2aX;uJIlvKEF{M{G4O{1qdmS3Y3XkJINqfHK3bHzpcoF1\WRiSESgcIV3\WxiYYSgOUB1dyBzMDD1UUBxemWrbnP1ZoF1\WRiZn;yJFE2KG2rboOg[o9tdG:5ZXSgZpkhSTJ|MUi3JIFl\Gm2aX;uJI1m[XO3cnXkJIFnfGW{IEG1JI1qdnNiYomgW4V{fGW{bjDicI91KGGwYXz5d4l{ NHXY[5k9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEO0OFkxQSd-M{CzOFQ6ODl:L3G+
HEK293T MWnGeY5kfGmxbjDhd5NigQ>? NEHnZ5gyOCCwTTD0c{AyODBidV2= MWjJcohq[mm2aX;uJI9nKGi3bXHuJJJm[2:vYnnuZY51KFCDREOg[ZhxemW|c3XkJIlvKEiHS{K5N3Qh[2WubIOgZZN{\XO|ZXSgZZMh[2:wdnXyd4lwdiCxZjDCRWVGKHSxIIPv[Il2dSCkZX76c5ltNUxvY3n0dpVtdGmwZTDheEAyOCCwTTD0c{AyODBidV2gZpkh[2:ub4LpcYV1emmlIHHuZYx6e2m| M1ruclxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE6PjJ|NkGvK|5EcEWPQly8M4E,
HEK293T MV;GeY5kfGmxbjDhd5NigQ>? Ml74NVAxKHWP M2HM[|I1KGi{cx?= NES4W45KdmirYnn0bY9vKG:oIIToZZB{cWejcnfpck1qdmS3Y3XkJINmdGxiZHXheIghcW5iaIXtZY4hUEWNMkmzWEBk\WyuczDveoVz\XiycnXzd4lv\yCqdX3hckBz\WOxbXLpcoFvfCCSQVSzJIF{e2W|c3XkJIF{KGmwY4LlZZNmKGmwIHPlcIwhe3W{dnn2ZYwh[XRiMUCwJJVOKHS{ZXH0[YQhOTVibXnud{BxemmxcjD0c{B1cGGyc3nnZZJocW5iYXTkbZRqd25ibXXhd5Vz\WRiYX\0[ZIhOjRiaILzJIRzfWdidILlZZRu\W62IHL5JI1mfGi7bHXu[UBjdHV? NYLiWHlFRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTl4MkO2NU8oRkOqRV3CUFww[T5?
Click to View More Cell Line Experimental Data
Assay
Methods Test Index PMID
Western blot PAD4 / H3R17Me / H3Cit / p21 / p53 / p-p53 ; iNOS ; MMP-2 / MMP-9 ; p-Elk-1 / Elk-1 18505818 29077055 28844713 21655091
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, Cl-amidine 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. Cl-amidine delays thrombosis development in NZM mice. It inhibits PADs in mice without significant toxicity and improves disease phenotypes in animal models of inflammatory arthritis and inflammatory bowel disease[3]. And It is shown to reduce disease severity in mouse models of ulcerative colitis and RA[2].

Protocol (from reference)

Cell Research:

[1]
  • Cell lines: CV-1 cells
  • Concentrations: 0-200 μM
  • Incubation Time: 40 h
  • Method:

    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. 

  • (Only for Reference)
Animal Research:

[4]
  • Animal Models: DSS mouse model of colitis (genetic background：C57BL/6 mice)
  • Dosages: 75 mg/kg (i.p); 5, 25, and 75 mg/kg(oral)
  • Administration: by oral gavage or i.p
  • (Only for Reference)

Solubility (25°C)

In vitro

 DMSO 84 mg/mL warmed
(197.74 mM)
Ethanol 84 mg/mL warmed
(197.74 mM)
Water 70 mg/mL warmed
(164.78 mM)

* 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.

Chemical Information

Molecular Weight 424.8
Formula

C14H19ClN4O2.C2HF3O2
CAS No. 1043444-18-3
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1=CC=C(C=C1)C(=O)NC(CCCN=C(CCl)N)C(=O)N.C(=O)(C(F)(F)F)O

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