Amifostine thiol (WR-1065) dihydrochloride can protect normal tissues from the toxic effects of certain cancer drugs and activate p53 through a JNK-dependent signaling pathway.

Product information

CAS Number: 14653-77-1

Molecular Weight: 207.16

Formula: C5H16Cl2N2S

Synonym:

WR-1065 dihydrochloride

Chemical Name: 2-[(3-aminopropyl)amino]ethane-1-thiol dihydrochloride

Smiles: Cl.Cl.NCCCNCCS

InChiKey: XDRLRDHLCIFZIW-UHFFFAOYSA-N

InChi: InChI=1S/C5H14N2S.2ClH/c6-2-1-3-7-4-5-8;;/h7-8H,1-6H2;2*1H

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: H2O : ≥ 100 mg/mL (482.72 mM) DMSO : 25 mg/mL (120.68 mM; Need ultrasonic)

Storage Condition: Soluble in DMSO

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

The DNA-binding activity is increased in a Amifostine thiol dihydrochloride (Amifostine thiol) concentration-dependent manner. Cells treated with 1 mM Amifostine thiol dihydrochloride for 24 h reveal that all of the p53-induced genes analyzed are transactivated following Amifostine thiol dihydrochloride treatment, in a p53-dependent manner. Significantly, treatment with Amifostine thiol 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.

In Vivo:

The results show that Amifostine thiol dihydrochloride (Amifostine thiol) attenuates the severity of 6-OHDA-induced catalepsy (P<0.001) when compare with 6-OHDA-lesioned rats. Also it has been observed that Amifostine thiol dihydrochloride improves catalepsy in dose dependent manner (P<0.001). Pretreatment with three different doses of Amifostine thiol dihydrochloride (20, 40 and 80 μg/2 μL/rat) for 3 days before 6-OHDA administration, significantly (P<0.001) elevates SOD activity and restores it to normal range compare with 6-OHDA lesioned rats.

References:

1. Pluquet O, et al. The cytoprotective aminothiol WR1065 activates p53 through a non-genotoxic signaling pathway involving c-Jun N-terminal kinase. J Biol Chem. 2003 Apr 4;278(14):11879-87.
2. Shen H, et al. Binding of the aminothiol WR-1065 to transcription factors influences cellular response to anticancer drugs. J Pharmacol Exp Ther. 2001 Jun;297(3):1067-73.
3. Afshin Kheradmand, et al. Effect of WR-1065 on 6-hydroxydopamine-induced catalepsy and IL-6 level in rats. Iran J Basic Med Sci. 2016 May; 19(5): 490-496.

Products are for research use only. Not for human use.