Amifostine thiol(Synonyms: WR-1065)

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Amifostine thiol (Synonyms: WR-1065)

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(Synonyms: WR-1065)

Amifostine thiol Chemical Structure

CAS No. : 31098-42-7

规格 价格 是否有货 数量
10 mg ￥900 In-stock
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生物活性

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[1][2][3].

IC50 & Target

p53[2]
体外研究
(In Vitro)

Amifostine thiol can reduce both the direct and delayed detrimental effects of both high and low-LET radiation exposures[1].
Amifostine thiol attenuates both the DNA damage and the G1-phase arrest induced by radiation[1].
Amifostine thiol (4 mM; 30 minutes) protects RKO36 cells from chromosomal damage and death induced by ionizing radiation[1].
Amifostine thiol (4 mM; 30 minutes) protects irradiated RKO36 cells from delayed genomic instability[1].
Amifostine thiol is cytotoxic to RKO36 cells at milimolar concentrations, especially after continuous treatment[1].
Amifostine thiol at 40 μM protects RKO36 cells from delayed genomic instability but not from cell death and immediate chromosomal damage[1].
Amifostine thiol activates JNK resulting in the phosphorylation of p53 at threonine 81[2].
Amifostine thiol affects phosphorylation of topoisomerase IIα leading to changes in enzyme activity and cell cycle progression in CHO AA8 cells[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

134.24

Formula

C5H14N2S
CAS 号

31098-42-7
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
溶解性数据
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
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 7.4493 mL 37.2467 mL 74.4934 mL
5 mM 1.4899 mL 7.4493 mL 14.8987 mL
10 mM 0.7449 mL 3.7247 mL 7.4493 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
参考文献

  • [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.

    [3]. J. S. Murley, et al. WR-1065, an active metabolite of the cytoprotector amifostine, affects phosphorylation of topoisomerase IIα leading to changes in enzyme activity and cell cycle progression in CHO AA8 cells. Cell Prolif. 1997 Jun; 30(6): 283-294.

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