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MHY1485 是一種有效的細(xì)胞滲透性 mTOR 激huo劑,靶向 mTOR 的 ATP 結(jié)構(gòu)域。MHY 1485 通過抑制自噬體和溶酶體之間的融合來抑制自噬 (autophagy)。
生物活性
MHY1485 is a potent cell-permeable mTOR activator that targets the ATP domain of mTOR. MHY1485 inhibits autophagy by suppression of fusion between autophagosomes and lysosomes[1].
IC50 & Target
mTORC1 mTORC2 Autophagy
體外研究(In Vitro)
MHY1485 (10 μM; 4 hours) shows that GCDC-induced autophagic activity is inhibited by upregulating p-mTOR expression and downregulating LC3 and p62 expression in HCC cells[1].
MHY1485 (5 μM; 6 hours) increases the LC3II/LC3I ratio in a dose and time-dependently manner due to presumably inhibited LC3II degradation in rat liver Ac2F cells[2].
MHY1485 (0.5-2 μM; 6 hours) increases the phosphorylation of mTOR at ser2448 and upregulates the level of phosphorylation of 4E-BP1 in a dose-dependently manner in Ac2F cells[2].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Western Blot Analysis[1]
Cell Line: | HCC cells |
Concentration: | 10 μM |
Incubation Time: | 4 hours |
Result: | Upregulated p-mTOR and downregulated LC3 and p62 expression. |
體內(nèi)研究(In Vivo)
MHY1485 (intraperitoneal injection; 10?mg/kg, 2 days) blocks the autophagy signaling induced by follicle-stimulating hormone (FSH). It increases p-mTOR and p-S6K1 expression levels, whereas LC3 expression shows no marked change compared to that in the control group[3].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model: | 4-week-old female ICR mice[3] |
Dosage: | 10?mg/kg, 2 days |
Administration: | Intraperitoneal injection |
Result: | Suppressed the autophagy level following FSH treatment. |
分子量:387.39
Formula:C17H21N7O4
CAS 號(hào):326914-06-1
運(yùn)輸條件:Room temperature in continental US; may vary elsewhere.
儲(chǔ)存方式
Powder | -20°C | 3 years |
---|---|---|
4°C | 2 years | |
In solvent | -80°C | 6 months |
-20°C | 1 month |
溶解性數(shù)據(jù)
DMSO : 7.69 mg/mL (19.85 mM; Need ultrasonic)
H2O : 1 mg/mL (2.58 mM; Need ultrasonic)
濃度溶劑體積質(zhì)量 | 1 mg | 5 mg | 10 mg |
---|
1 mM | 2.5814 mL | 12.9069 mL | 25.8138 mL |
5 mM | 0.5163 mL | 2.5814 mL | 5.1628 mL |
10 mM | 0.2581 mL | 1.2907 mL | 2.5814 mL |
請(qǐng)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(chǔ)備液;一旦配成溶液,請(qǐng)分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 儲(chǔ)存時(shí),請(qǐng)?jiān)?6 個(gè)月內(nèi)使用,-20°C 儲(chǔ)存時(shí),請(qǐng)?jiān)?1 個(gè)月內(nèi)使用。
以下溶解方案都請(qǐng)先按照 In Vitro 方式配制澄清的儲(chǔ)備液,再依次添加助溶劑:
——為保證實(shí)驗(yàn)結(jié)果的可靠性,澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件,適當(dāng)保存;體內(nèi)實(shí)驗(yàn)的工作液,建議您現(xiàn)用現(xiàn)配,當(dāng)天使用; 以下溶劑前顯示的百
分比是指該溶劑在您配制終溶液中的體積占比;如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象,可以通過加熱和/或超聲的方式助溶
參考文獻(xiàn)
MHY1485 是一種有效的細(xì)胞滲透性 mTOR 激huo劑,靶向 mTOR 的 ATP 結(jié)構(gòu)域。MHY 1485 通過抑制自噬體和溶酶體之間的融合來抑制自噬 (autophagy)。
生物活性
MHY1485 is a potent cell-permeable mTOR activator that targets the ATP domain of mTOR. MHY1485 inhibits autophagy by suppression of fusion between autophagosomes and lysosomes[1].
IC50 & Target
mTORC1 mTORC2 Autophagy
體外研究(In Vitro)
MHY1485 (10 μM; 4 hours) shows that GCDC-induced autophagic activity is inhibited by upregulating p-mTOR expression and downregulating LC3 and p62 expression in HCC cells[1].
MHY1485 (5 μM; 6 hours) increases the LC3II/LC3I ratio in a dose and time-dependently manner due to presumably inhibited LC3II degradation in rat liver Ac2F cells[2].
MHY1485 (0.5-2 μM; 6 hours) increases the phosphorylation of mTOR at ser2448 and upregulates the level of phosphorylation of 4E-BP1 in a dose-dependently manner in Ac2F cells[2].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Western Blot Analysis[1]
Cell Line: | HCC cells |
Concentration: | 10 μM |
Incubation Time: | 4 hours |
Result: | Upregulated p-mTOR and downregulated LC3 and p62 expression. |
體內(nèi)研究(In Vivo)
MHY1485 (intraperitoneal injection; 10?mg/kg, 2 days) blocks the autophagy signaling induced by follicle-stimulating hormone (FSH). It increases p-mTOR and p-S6K1 expression levels, whereas LC3 expression shows no marked change compared to that in the control group[3].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model: | 4-week-old female ICR mice[3] |
Dosage: | 10?mg/kg, 2 days |
Administration: | Intraperitoneal injection |
Result: | Suppressed the autophagy level following FSH treatment. |
分子量:387.39
Formula:C17H21N7O4
CAS 號(hào):326914-06-1
運(yùn)輸條件:Room temperature in continental US; may vary elsewhere.
儲(chǔ)存方式
Powder | -20°C | 3 years |
---|---|---|
4°C | 2 years | |
In solvent | -80°C | 6 months |
-20°C | 1 month |
溶解性數(shù)據(jù)
DMSO : 7.69 mg/mL (19.85 mM; Need ultrasonic)
H2O : 1 mg/mL (2.58 mM; Need ultrasonic)
濃度溶劑體積質(zhì)量 | 1 mg | 5 mg | 10 mg |
---|
1 mM | 2.5814 mL | 12.9069 mL | 25.8138 mL |
5 mM | 0.5163 mL | 2.5814 mL | 5.1628 mL |
10 mM | 0.2581 mL | 1.2907 mL | 2.5814 mL |
請(qǐng)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(chǔ)備液;一旦配成溶液,請(qǐng)分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 儲(chǔ)存時(shí),請(qǐng)?jiān)?6 個(gè)月內(nèi)使用,-20°C 儲(chǔ)存時(shí),請(qǐng)?jiān)?1 個(gè)月內(nèi)使用。
以下溶解方案都請(qǐng)先按照 In Vitro 方式配制澄清的儲(chǔ)備液,再依次添加助溶劑:
——為保證實(shí)驗(yàn)結(jié)果的可靠性,澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件,適當(dāng)保存;體內(nèi)實(shí)驗(yàn)的工作液,建議您現(xiàn)用現(xiàn)配,當(dāng)天使用; 以下溶劑前顯示的百
分比是指該溶劑在您配制終溶液中的體積占比;如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象,可以通過加熱和/或超聲的方式助溶
參考文獻(xiàn)