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MHY1485

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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)。

貨號(hào):HY-B0795
CAS: 326914-06-1
參數(shù)品牌:MCE
產(chǎn)品參數(shù)
品牌:MCE
型號(hào):HY-B0795
起訂量:1
規(guī)格::10mg
價(jià)格::¥700
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產(chǎn)品詳情

MHY1485

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°C3 years

4°C2 years
In solvent-80°C6 months

-20°C1 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)

配制儲(chǔ)備液
濃度溶劑體積質(zhì)量1 mg5 mg10 mg
1 mM2.5814 mL12.9069 mL25.8138 mL
5 mM0.5163 mL2.5814 mL5.1628 mL
10 mM0.2581 mL1.2907 mL2.5814 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。

In Vivo:

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

  • 1.


    請(qǐng)依序添加每種溶劑: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 0.77 mg/mL (1.99 mM); Clear solution


  • 2.


    請(qǐng)依序添加每種溶劑: 10% DMSO    90% corn oil

    Solubility: ≥ 0.77 mg/mL (1.99 mM); Clear solution


參考文獻(xiàn)

[1]. Gao L, et al. Glycochenodeoxycholate promotes hepatocellular carcinoma invasion and migration by AMPK/mTOR dependent autophagy activation. Cancer Lett. 2019 Jul 10;454:215-223.

[2]. Choi YJ, et al. Inhibitory effect of mTOR activator MHY1485 on autophagy: suppression of lysosomal fusion. PLoS One. 2012;7(8):e43418.

[3]. Zhou J, et al.Administration of follicle-stimulating hormone induces autophagy via upregulation of HIF-1α in mouse granulosa cells.Cell Death Dis. 2017 Aug 17;8(8):e3001.






MHY1485
MHY1485

MHY1485

分享到微信

×
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)。

貨號(hào):HY-B0795
CAS: 326914-06-1
品牌:MCE
型號(hào):HY-B0795
起訂量:1
規(guī)格::10mg
價(jià)格::¥700
15906629305
在線客服
產(chǎn)品詳情

MHY1485

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°C3 years

4°C2 years
In solvent-80°C6 months

-20°C1 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)

配制儲(chǔ)備液
濃度溶劑體積質(zhì)量1 mg5 mg10 mg
1 mM2.5814 mL12.9069 mL25.8138 mL
5 mM0.5163 mL2.5814 mL5.1628 mL
10 mM0.2581 mL1.2907 mL2.5814 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。

In Vivo:

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

  • 1.


    請(qǐng)依序添加每種溶劑: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 0.77 mg/mL (1.99 mM); Clear solution


  • 2.


    請(qǐng)依序添加每種溶劑: 10% DMSO    90% corn oil

    Solubility: ≥ 0.77 mg/mL (1.99 mM); Clear solution


參考文獻(xiàn)

[1]. Gao L, et al. Glycochenodeoxycholate promotes hepatocellular carcinoma invasion and migration by AMPK/mTOR dependent autophagy activation. Cancer Lett. 2019 Jul 10;454:215-223.

[2]. Choi YJ, et al. Inhibitory effect of mTOR activator MHY1485 on autophagy: suppression of lysosomal fusion. PLoS One. 2012;7(8):e43418.

[3]. Zhou J, et al.Administration of follicle-stimulating hormone induces autophagy via upregulation of HIF-1α in mouse granulosa cells.Cell Death Dis. 2017 Aug 17;8(8):e3001.






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