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Thiamet G

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Thiamet G 為有效，選擇性的 O-GlcNAcase 抑制劑，抑制人 OGA 的 Ki 值為 20 nM。O-GlcNAcase 的作用是從修飾的蛋白質(zhì)中去除 O-GlcNAc。
參數(shù)品牌：MCE
產(chǎn)品參數(shù)
品牌：MCE
型號：HY-12588
起訂量：1
規(guī)格:：5mg
價格:：￥600
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產(chǎn)品詳情

Thiamet G

Thiamet G 為有效，選擇性的 O-GlcNAcase 抑制劑，抑制人 OGA 的 Ki 值為 20 nM。O-GlcNAcase 的作用是從修飾的蛋白質(zhì)中去除 O-GlcNAc。

生物活性

Thiamet G is a potent and selective inhibitor of O-GlcNAcase (OGA), which acts to remove O-GlcNAc from modified proteins, with Ki of 20 nM for human OGA.


IC50 & Target

Ki: 20 nM (Human OGA)[1]


體外研究(In Vitro)

Thiamet G (1 μM) induces a clear increase in the accumulation of O-GlcNAcylated proteins of ATDC5 cells. O-GlcNAc accumulation induced by Thiamet G also evokes a clear increase in the activity of these MMPs. Thiamet G (1 μM) induces the phosphorylation of JNK, ERK, and p38 but not phosphorylation of Akt[2]. Thiamet G (0.1-10 μM) does not significantly affect the cell viability. Thiamet G decreases phosphorylation of tau and alters the microtubule dynamics[3].


體內(nèi)研究(In Vivo)

Thiamet G (500 mg/kg/d) increases global and tau O-GlcNAc and reduces neurodegeneration. Thiamet G-treated group has 1.4-fold more motor neurons and hinders tau-driven neurodegeneration within this transgenic model. Thiamet G treatment therefore has no detectable effect on mice lacking the P301L transgene, indicating that prevention of neurodegeneration and weight loss is mediated by Thiamet G treatment only in the context of the P301L transgene. In Thiamet G-treated mice, the O-GlcNAc increases in the brain and spinal cord tissues[1]. Thiamet G (20 mg/kg, i.p.) increases O-GlcNAc levels in brain, liver, and knee of the C57BL/6 mice in a dose-dependent manner[2].


分子量：248.30


性狀：Solid


Formula：C9H16N2O4S


CAS 號：1009816-48-1


運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.


儲存方式

Powder-20°C3 years

4°C2 years
In solvent-80°C6 months

-20°C1 month


溶解性數(shù)據(jù)


In Vitro: 

H2O : ≥ 50 mg/mL (201.37 mM)

DMSO : ≥ 45 mg/mL (181.23 mM)

* "≥" means soluble, but saturation unknown.

配制儲備液
濃度溶劑體積質(zhì)量1 mg5 mg10 mg
1 mM4.0274 mL20.1369 mL40.2739 mL
5 mM0.8055 mL4.0274 mL8.0548 mL
10 mM0.4027 mL2.0137 mL4.0274 mL
*

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；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 儲存時，請在 6 個月內(nèi)使用，-20°C 儲存時，請在 1 個月內(nèi)使用。

In Vivo:

以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液，再依次添加助溶劑：

——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(dāng)保存；體內(nèi)實驗的工作液，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.


    請依序添加每種溶劑： PBS

    Solubility: 50 mg/mL (201.37 mM); Clear solution; Need ultrasonic


  • 2.


    請依序添加每種溶劑： 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (8.38 mM); Clear solution


  • 3.


    請依序添加每種溶劑： 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (8.38 mM); Clear solution


  • 4.


    請依序添加每種溶劑： 10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (8.38 mM); Clear solution



參考文獻(xiàn)

[1]. Yuzwa SA, et al. Increasing O-GlcNAc slows neurodegeneration and stabilizes tau against aggregation. Nat Chem Biol. 2012 Feb 26;8(4):393-9. [Content Brief]

[2]. Andrés-Bergós J, et al. The increase in O-linked N-acetylglucosamine protein modification stimulates chondrogenic differentiation both in vitro and in vivo. J Biol Chem. 2012 Sep 28;287(40):33615-28.  [Content Brief]

[3]. Ding N, et al. Thiamet-G-mediated inhibition of O-GlcNAcase sensitizes human leukemia cells to microtubule-stabilizing agent NSC 125973. Biochem Biophys Res Commun. 2014 Oct 24;453(3):392-7.  [Content Brief]



Thiamet G
Thiamet G

Thiamet G

分享到微信

×
Thiamet G 為有效，選擇性的 O-GlcNAcase 抑制劑，抑制人 OGA 的 Ki 值為 20 nM。O-GlcNAcase 的作用是從修飾的蛋白質(zhì)中去除 O-GlcNAc。
品牌：MCE
型號：HY-12588
起訂量：1
規(guī)格:：5mg
價格:：￥600
15906629305
在線客服
產(chǎn)品詳情

Thiamet G

Thiamet G 為有效，選擇性的 O-GlcNAcase 抑制劑，抑制人 OGA 的 Ki 值為 20 nM。O-GlcNAcase 的作用是從修飾的蛋白質(zhì)中去除 O-GlcNAc。

生物活性

Thiamet G is a potent and selective inhibitor of O-GlcNAcase (OGA), which acts to remove O-GlcNAc from modified proteins, with Ki of 20 nM for human OGA.


IC50 & Target

Ki: 20 nM (Human OGA)[1]


體外研究(In Vitro)

Thiamet G (1 μM) induces a clear increase in the accumulation of O-GlcNAcylated proteins of ATDC5 cells. O-GlcNAc accumulation induced by Thiamet G also evokes a clear increase in the activity of these MMPs. Thiamet G (1 μM) induces the phosphorylation of JNK, ERK, and p38 but not phosphorylation of Akt[2]. Thiamet G (0.1-10 μM) does not significantly affect the cell viability. Thiamet G decreases phosphorylation of tau and alters the microtubule dynamics[3].


體內(nèi)研究(In Vivo)

Thiamet G (500 mg/kg/d) increases global and tau O-GlcNAc and reduces neurodegeneration. Thiamet G-treated group has 1.4-fold more motor neurons and hinders tau-driven neurodegeneration within this transgenic model. Thiamet G treatment therefore has no detectable effect on mice lacking the P301L transgene, indicating that prevention of neurodegeneration and weight loss is mediated by Thiamet G treatment only in the context of the P301L transgene. In Thiamet G-treated mice, the O-GlcNAc increases in the brain and spinal cord tissues[1]. Thiamet G (20 mg/kg, i.p.) increases O-GlcNAc levels in brain, liver, and knee of the C57BL/6 mice in a dose-dependent manner[2].


分子量：248.30


性狀：Solid


Formula：C9H16N2O4S


CAS 號：1009816-48-1


運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.


儲存方式

Powder-20°C3 years

4°C2 years
In solvent-80°C6 months

-20°C1 month


溶解性數(shù)據(jù)


In Vitro: 

H2O : ≥ 50 mg/mL (201.37 mM)

DMSO : ≥ 45 mg/mL (181.23 mM)

* "≥" means soluble, but saturation unknown.

配制儲備液
濃度溶劑體積質(zhì)量1 mg5 mg10 mg
1 mM4.0274 mL20.1369 mL40.2739 mL
5 mM0.8055 mL4.0274 mL8.0548 mL
10 mM0.4027 mL2.0137 mL4.0274 mL
*

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；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 儲存時，請在 6 個月內(nèi)使用，-20°C 儲存時，請在 1 個月內(nèi)使用。

In Vivo:

以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液，再依次添加助溶劑：

——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(dāng)保存；體內(nèi)實驗的工作液，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.


    請依序添加每種溶劑： PBS

    Solubility: 50 mg/mL (201.37 mM); Clear solution; Need ultrasonic


  • 2.


    請依序添加每種溶劑： 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (8.38 mM); Clear solution


  • 3.


    請依序添加每種溶劑： 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (8.38 mM); Clear solution


  • 4.


    請依序添加每種溶劑： 10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (8.38 mM); Clear solution



參考文獻(xiàn)

[1]. Yuzwa SA, et al. Increasing O-GlcNAc slows neurodegeneration and stabilizes tau against aggregation. Nat Chem Biol. 2012 Feb 26;8(4):393-9. [Content Brief]

[2]. Andrés-Bergós J, et al. The increase in O-linked N-acetylglucosamine protein modification stimulates chondrogenic differentiation both in vitro and in vivo. J Biol Chem. 2012 Sep 28;287(40):33615-28.  [Content Brief]

[3]. Ding N, et al. Thiamet-G-mediated inhibition of O-GlcNAcase sensitizes human leukemia cells to microtubule-stabilizing agent NSC 125973. Biochem Biophys Res Commun. 2014 Oct 24;453(3):392-7.  [Content Brief]



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