1. NF-κB
  2. NF-κB

Pyrrolidinedithiocarbamate ammonium (Synonyms: Ammonium pyrrolidinedithiocarbamate; APDC; 1-Pyrrolidinedithiocarboxylic acid ammonium salt)

Cat. No.: HY-18738 Purity: >98.0%
Data Sheet SDS Handling Instructions

Pyrrolidinedithiocarbamate ammonium is a selective NF-kB inhibitor.

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Pyrrolidinedithiocarbamate ammonium Chemical Structure

Pyrrolidinedithiocarbamate ammonium Chemical Structure

CAS No. : 5108-96-3

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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

Pyrrolidinedithiocarbamate ammonium is a selective NF-kB inhibitor.

IC50 & Target

Target: NF-kB

In Vitro

Pretreatment of cells with PDTC (3-1000 mM) dose-dependently attenuate IL-8 production. Furthermore, PDTC (100 mM) suppresses the accumulation of IL-8 mRNA. PDTC inhibites the activation of NF-kB, because PDTC suppresses both NF-kB DNA binding and NF-kB-dependent transcriptional activity. Taken together, our data demonstrate that NF-kB inhibition with PDTC decrease IL-8 production by intestinal epithelial cells[1].

In Vivo

The DSS+PDTC-treated groupⅡ exhibited suppression of shortening of intestinal length and reduction of DAI score. Activated NF-κB level and IL-1β and TNF-α levels are significantly lower in DSS+PDTC-treated groupⅡ. These findings suggest that suppression of NF-κB activity by PDTC can delay the healing of mucosal tissue defects (erosions or ulcers) arising from inflammation, but that it can strongly suppress the expression of inf-lammatory cytokines (IL-1β and TNF-α), resulting in significant alleviation of colitis. PDTC is useful for the treatment of ulcerative colitis[2].

Clinical Trial
NCT Number Sponsor Condition Start Date Phase
NCT02503150 Second Military Medical University|Cancer Institute and Hospital, Chinese Academy of Medical Sciences|Changhai Hospital|Xinhua Hospital, Shanghai Jiao Tong University School of Medicine|Fudan University|Shanghai Changzheng Hospital|Zhejiang Cancer Hospital|Chinese PLA General Hospital|Beijing Cancer Hospital|Shanghai General Hospital, Shanghai Jiao Tong University School of Medicine|RenJi Hospital|Second Affiliated Hospital, School of Medicine, Zhejiang University|First People's Hospital of Hangzhou|The 307th Hospital of Chinese People`s Liberation Army|Huashan Hospital|Ruijin Hospital|Shanghai Haixin Biotechnology Co. Ltd Metastatic Colorectal Cancer July 2015 Phase 3
NCT02503150 Second Military Medical University|Cancer Institute and Hospital, Chinese Academy of Medical Sciences|Changhai Hospital|Xinhua Hospital, Shanghai Jiao Tong University School of Medicine|Fudan University|Shanghai Changzheng Hospital|Zhejiang Cancer Hospital|Chinese PLA General Hospital|Beijing Cancer Hospital|Shanghai General Hospital, Shanghai Jiao Tong University School of Medicine|RenJi Hospital|Second Affiliated Hospital, School of Medicine, Zhejiang University|First People's Hospital of Hangzhou|The 307th Hospital of Chinese People`s Liberation Army|Huashan Hospital|Ruijin Hospital|Shanghai Haixin Biotechnology Co. Ltd Metastatic Colorectal Cancer July 2015 Phase 3
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References
Preparing Stock Solutions
Concentration Volume (DMSO) Mass 1 mg 5 mg 10 mg
1 mM 6.0868 mL 30.4340 mL 60.8680 mL
5 mM 1.2174 mL 6.0868 mL 12.1736 mL
10 mM 0.6087 mL 3.0434 mL 6.0868 mL
Cell Assay
[1]

The human colon cancer cell line HT-29 is obtained and cells are grown in modified McCoy’s 5A medium supplemented with 10% fetal bovine serum. To study the effect of PDTC on IL-8 production, HT-29 cells in 96-well plates are induced with 20 ng/mL of IL-1b for 18 h. Various concentrations (3-1000 mM) of PDTC or its vehicle (culture medium) are added to the cells 30 min prior to IL-1b stimulation. The concentration of IL-8 in the supernatant is determined using solid-phase enzyme-linked immunosorbent assay, as described previously employing the multiple antibody sandwich principle that specifically detects human IL-8[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[2]

Six-week-old female BALB/c mice are used for this study. DSS with a molecular weight of 5000 is dissolved in tap water to obtain 5% DSS solution. Mice are allowed free access to this solution as drinking water for 7 d to prepare a mouse model of DSS-induced colitis. PDTC, dissolved in distilled water, is administered intraperitoneally to mice at dose levels of 100 and 50 mg/kg. Mice are divided into a DSS-untreated group (normal group), DSS-treated control group, DSS+PDTC-treated groupⅠ(low-dose group), and DSS+PDTC-treated groupⅡ (high-dose group). In each group, the disease activity index score (DAI score), intestinal length, histological score, and the levels of activated NF-κB and inflammatory cytokines (IL-1β and TNF-α) in tissue are measured[2]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

164.29

Formula

C₅H₁₂N₂S₂

CAS No.

5108-96-3

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: ≥ 42 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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Pyrrolidinedithiocarbamate ammonium
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HY-18738
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