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Erastin 是鐵誘導(dǎo)的細胞死亡 (ferroptosis) 誘導(dǎo)劑。Erastin 結(jié)合且抑制電壓依賴性陰離子通道 (VDAC2/VDAC3)。
生物活性 |
Erastin is a ferroptosis inducer. Erastin binds and inhibits voltage-dependent anion channels (VDAC2/VDAC3)[1]. |
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體外研究 (In Vitro) |
Erastin triggers oxidative, iron-dependent cell death. Treatment of NRAS-mutant HT-1080 fibrosarcoma cells with the RSL molecule erastin (10 μM) results in a time-dependent increase in cytosolic and lipid ROS beginning at 2 hours[1]. Cell death triggered by erastin is significantly inhibited by antioxidants (e.g., α-tocopherol, butylated hydroxytoluene, and β-carotene) and iron chelators, suggesting that ROS- and iron-dependent signaling is required for erastin-induced ferroptosis. Erastin can directly bind to VDAC2/3 in BJeLR cells. Knockdown of VDAC2 and VDAC3, but not VDAC1, leads to erastin resistance. Erastin has the ability to reduce glutathione level by directly inhibiting cystine/glutamate antiporter system Xc? activity, with activation of the ER stress response[2]. Erastin potently inhibits HT-29 cell survival. Erastin shows a dose-dependent effect, and 30 μM of erastin displays the most dramatic effect[3]. |
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體內(nèi)研究 (In Vivo) |
Intraperitoneal injection of erastin at well-tolerated doses dramatically inhibits HT-29 xenograft growth in severe combined immunodeficient mice[3]. |
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分子量 |
547.04 |
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Formula |
C30H31ClN4O4 |
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CAS 號 |
571203-78-6 |
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運輸條件 |
Room temperature in continental US; may vary elsewhere. |
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儲存方式 |
*該產(chǎn)品在溶液狀態(tài)不穩(wěn)定,建議您現(xiàn)用現(xiàn)配,即刻使用。 |
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溶解性數(shù)據(jù) |
In Vitro: DMSO : 12.5 mg/mL (22.85 mM; Need ultrasonic) H2O : < 0.1 mg/mL (insoluble)
配制儲備液
*
請根據(jù)產(chǎn)品在不同溶劑中的溶解度,選擇合適的溶劑配制儲備液;該產(chǎn)品在溶液狀態(tài)不穩(wěn)定,建議您現(xiàn)用現(xiàn)配,即刻使用。
In Vivo:
——為保證實驗結(jié)果的可靠性,澄清的儲備液可以根據(jù)儲存條件,適當保存;體內(nèi)實驗的工作液,建議您現(xiàn)用現(xiàn)配,當天使用; 以下溶劑前顯示的百
|
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參考文獻 |
[2]. Xie Y, et al. Ferroptosis: process and function. Cell Death Differ. 2016 Mar;23(3):369-79. |
Erastin 是鐵誘導(dǎo)的細胞死亡 (ferroptosis) 誘導(dǎo)劑。Erastin 結(jié)合且抑制電壓依賴性陰離子通道 (VDAC2/VDAC3)。
生物活性 |
Erastin is a ferroptosis inducer. Erastin binds and inhibits voltage-dependent anion channels (VDAC2/VDAC3)[1]. |
||||||||||||||||
體外研究 (In Vitro) |
Erastin triggers oxidative, iron-dependent cell death. Treatment of NRAS-mutant HT-1080 fibrosarcoma cells with the RSL molecule erastin (10 μM) results in a time-dependent increase in cytosolic and lipid ROS beginning at 2 hours[1]. Cell death triggered by erastin is significantly inhibited by antioxidants (e.g., α-tocopherol, butylated hydroxytoluene, and β-carotene) and iron chelators, suggesting that ROS- and iron-dependent signaling is required for erastin-induced ferroptosis. Erastin can directly bind to VDAC2/3 in BJeLR cells. Knockdown of VDAC2 and VDAC3, but not VDAC1, leads to erastin resistance. Erastin has the ability to reduce glutathione level by directly inhibiting cystine/glutamate antiporter system Xc? activity, with activation of the ER stress response[2]. Erastin potently inhibits HT-29 cell survival. Erastin shows a dose-dependent effect, and 30 μM of erastin displays the most dramatic effect[3]. |
||||||||||||||||
體內(nèi)研究 (In Vivo) |
Intraperitoneal injection of erastin at well-tolerated doses dramatically inhibits HT-29 xenograft growth in severe combined immunodeficient mice[3]. |
||||||||||||||||
分子量 |
547.04 |
||||||||||||||||
Formula |
C30H31ClN4O4 |
||||||||||||||||
CAS 號 |
571203-78-6 |
||||||||||||||||
運輸條件 |
Room temperature in continental US; may vary elsewhere. |
||||||||||||||||
儲存方式 |
*該產(chǎn)品在溶液狀態(tài)不穩(wěn)定,建議您現(xiàn)用現(xiàn)配,即刻使用。 |
||||||||||||||||
溶解性數(shù)據(jù) |
In Vitro: DMSO : 12.5 mg/mL (22.85 mM; Need ultrasonic) H2O : < 0.1 mg/mL (insoluble)
配制儲備液
*
請根據(jù)產(chǎn)品在不同溶劑中的溶解度,選擇合適的溶劑配制儲備液;該產(chǎn)品在溶液狀態(tài)不穩(wěn)定,建議您現(xiàn)用現(xiàn)配,即刻使用。
In Vivo:
——為保證實驗結(jié)果的可靠性,澄清的儲備液可以根據(jù)儲存條件,適當保存;體內(nèi)實驗的工作液,建議您現(xiàn)用現(xiàn)配,當天使用; 以下溶劑前顯示的百
|
||||||||||||||||
參考文獻 |
[2]. Xie Y, et al. Ferroptosis: process and function. Cell Death Differ. 2016 Mar;23(3):369-79. |