Amifostine thiol (WR-1065) 是细胞保护剂 Amifostine (HY-B0639) 的活性代谢物。Amifostine thiol 是一种具有辐射防护能力的细胞保护剂。Amifostine thiol 通过 JNK 依赖的信号通路激活 p53。

Amifostine thiol (WR-1065) is an active metabolite of the cytoprotector Amifostine (HY-B0639). Amifostine thiol is a cytoprotective agent with radioprotective abilities. Amifostine thiol activates p53 through a JNK-dependent signaling pathway.

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p53

Amifostine thiol can reduce both the direct and delayed detrimental effects of both high and low-LET radiation exposures.
Amifostine thiol attenuates both the DNA damage and the G1-phase arrest induced by radiation.
Amifostine thiol (4 mM; 30 minutes) protects RKO36 cells from chromosomal damage and death induced by ionizing radiation.
Amifostine thiol (4 mM; 30 minutes) protects irradiated RKO36 cells from delayed genomic instability.
Amifostine thiol is cytotoxic to RKO36 cells at milimolar concentrations, especially after continuous treatment.
Amifostine thiol at 40 μM protects RKO36 cells from delayed genomic instability but not from cell death and immediate chromosomal damage.
Amifostine thiol activates JNK resulting in the phosphorylation of p53 at threonine 81.
Amifostine thiol affects phosphorylation of topoisomerase IIα leading to changes i

Room temperature in continental US; may vary elsewhere.

4°C, protect from light, stored under nitrogen In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

[1]. Jaroslaw Dziegielewski, et al. WR-1065, the Active Metabolite of Amifostine, Mitigates Radiation-Induced Delayed Genomic Instability. Free Radic Biol Med. 2008 Dec 15; 45(12): 1674-1681.
[2]. Olivier Pluquet, 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. J Biol Chem. 2003 Apr 4;278(14):11879-87.

In Vitro: DMSO : 250 mg/mL (1862.34 mM; Need ultrasonic)H₂O : 100 mg/mL (744.93 mM; Need ultrasonic)配制储备液