Amifostine thiol dihydrochloride

SKU: orb1296180

Description

Amifostine thiol dihydrochloride (WR-1065) is a cytoprotective agent that activates p53 via a JNK-dependent pathway. It is widely used in research to investigate radioprotection and chemoprotection in normal tissues during in vitro and in vivo oncology studies.

Research Area

Cell Biology, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 14653-77-1
• MW: 207.165
• Purity: >99.99% (May vary between batches)
• Formula: C₅H₁₆Cl₂N₂S
• SMILES: Cl.Cl.NCCCNCCS
• Target: MDM-2/p53,p53
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:1 mg/mL (4.83 mM);DMSO:24 mg/mL (115.85 mM);H2O:100 mg/mL (482.71 mM)

Bioactivity

• In Vivo:
  WR-1065 attenuates the severity of 6-OHDA-induced catalepsy when compared with 6-OHDA-lesioned rats. Also, it has been observed that WR-1065 dihydrochloride improves catalepsy in a dose-dependent manner. Pretreatment with three different doses of WR-1065 dihydrochloride (20, 40, and 80 μg/2 μL/rat) for 3 days before 6-OHDA administration, significantly elevates SOD activity and restores it to normal range compare with 6-OHDA lesioned rats .
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• In Vitro:
  The DNA-binding activity is increased in a WR-1065 concentration-dependent manner. Cells treated with 1 mM WR-1065 dihydrochloride for 24 h revealed that all of the p53-induced genes analyzed are transactivated following WR-1065 dihydrochloride treatment, in a p53-dependent manner. Significantly, treatment with WR-1065 dihydrochloride leads to a 3-fold increase in luciferase expression driven by AP-1 and a 5-fold increase when this reporter gene is driven by NF-κB when these values are normalized to the level of the cotransfected β-galactosidase gene .
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• Cell Research:
  For Western analysis, cells are treated with 1 mM WR-1065 for 24 h, and subconfluent cultures of cells are harvested and lysed in RIPA buffer supplemented with protease inhibitors. Protein concentrations are determined by a detergent-compatible assay. Western blots are blocked and incubated in antibody in PBS/0.2% Tween 20/5% nonfat dry milk. Blots are incubated with 1 μg/mL antibody for 1 h at room temperature, followed by washing in PBS/0.2% Tween 20 and incubation in peroxidase-conjugated secondary antibody and chemiluminescence detection .
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• Animal Research:
  Seventy-two rats are divided randomly into 9 equal groups: 1) Control group receives no injection and is left untreated for the entire period of the experiment as intact animals; 2) Sham-operated group is subjected only to surgical procedure; 3) Vehicle (saline)-treated group receives 2 μL saline (Intra-SNc); 4) Lesioned group receives 6-hydroxydopamine; 5) Vehicle+6OHDA group receives saline as a vehicle 3 days once daily (2 μL/rat) before 6-OHDA injection; 6 to 8) Rats in these groups are pretreated with Intra-SNc injection of WR-1065 (20, 40 and 80 μg/2 μL/rat) 3 days before 6-OHDA injection; 9) Non-lesioned animals receive intra-SNc injection of WR-1065 dihydrochloride (80 μg/2 μL/rat) for three days .
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

WR1065, WR-1065, WR 1065, p53, inhibit, Inhibitor, MDM-2/p53, Amifostine thiol, Amifostine thiol dihydrochloride, Amifostine thiol Dihydrochloride

Compound Identifiers

PubChem CID

146169