1. Cell Cycle/DNA Damage Epigenetics Metabolic Enzyme/Protease
  2. Sirtuin Methionine Adenosyltransferase (MAT) Indoleamine 2,3-Dioxygenase (IDO)
  3. 3-TYP

3-TYP 是一种 SIRT3 抑制剂 (IC50: ~377 μM),也是甲硫氨酸氨肽酶 2 和吲哚胺 2,3-双加氧酶的抑制剂。3-TYP 可能存在许多需要检查的脱靶点,例如 NAD 依赖性酶,包括脱氢酶。

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3-TYP Chemical Structure

3-TYP Chemical Structure

CAS No. : 120241-79-4

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10 mM * 1 mL in DMSO ¥660
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5 mg ¥600
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10 mg ¥1000
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50 mg ¥3000
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100 mg ¥4900
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Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 49 篇科研文献

WB

    3-TYP purchased from MCE. Usage Cited in: Nat Immunol. 2023 Jan;24(1):162-173.  [Abstract]

    A485 (10 μM; 24 h) leads to the downregulation of H3K9bhb and CPS1 in BHB-treated CD8+ TM cells; however, the use of 3-TYP (10 μM; 24 h) or Trichostatin A (TSA; 5 nM; 24 h) result in the increase of H3K9bhb and CPS1.

    3-TYP purchased from MCE. Usage Cited in: Cell Physiol Biochem. 2017;44(6):2212-2227.  [Abstract]

    MEK, ERK1/2 and IκBα phosphorylation and their total protein expression are detected by Western blot. Cardiac myocytes are stimulated by Ang II for 48h after treatment with Sesamin (10 mM) or 3-TYP (50 μM).

    查看 Sirtuin 亚型特异性产品:

    查看 Indoleamine 2,3-Dioxygenase (IDO) 亚型特异性产品:

    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    3-TYP is an inhibitor of SIRT3 (IC50: ~377 μM) and an inhibitor of Methionine Adenosyltransferase (MAT) 2 and Indoleamine 2,3-Dioxygenase (IDO). There may be many off-target sites for 3-TYP that need to be examined, such as NAD-dependent enzymes, including dehydrogenases[1][2][3].

    IC50 & Target[3]

    SIRT3

    377 μM (IC50)

    Methionine Aminopeptidase 2

     

    体外研究
    (In Vitro)

    3-TYP 抑制褪黑激素增强的 SIRT3 活性,但不影响 SIRT3 蛋白表达。3-TYP 预处理可逆转褪黑激素对镉 (Cd) 诱导的线粒体衍生 O2- 产生和自噬性细胞死亡的保护作用。3-TYP 显著减弱褪黑激素诱导的暴露于 Cd 的 HepG2 细胞中去乙酰化 SOD2 表达和 SOD2 活性的增加[1]

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    体内研究
    (In Vivo)

    3-TYP (50 mg/kg,ip) 对 LVEF、LVFS、梗塞面积、血清 LDH 水平、细胞凋亡和氧化应激没有显著影响。与对照组相比,3-TYP 对 gp91phox、Nrf2、NQO 1、Bax、Bcl-2、Caspase-3 和 cleaved Caspase-3 表达水平的影响很小。3-TYP 显著降低 SIRT3 活性并增加 SOD2 的乙酰化,但不影响 SIRT3 表达。3-TYP 通过在再灌注 24 小时后降低 LVEF 和 LVFS 来减弱褪黑激素的心脏保护作用。与 IR+Mel 组相比,3-TYP 还增加了梗死面积、血清 LDH 水平和细胞凋亡率[2]

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    分子量

    146.15

    Formula

    C7H6N4

    CAS 号
    性状

    固体

    颜色

    White to off-white

    运输条件

    Room temperature in continental US; may vary elsewhere.

    储存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    溶解性数据
    In Vitro: 

    DMSO 中的溶解度 : 125 mg/mL (855.29 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

    Ethanol 中的溶解度 : 16.67 mg/mL (114.06 mM; 超声助溶)

    H2O 中的溶解度 : 1 mg/mL (6.84 mM; 超声助溶 (<60°C))

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 6.8423 mL 34.2114 mL 68.4229 mL
    5 mM 1.3685 mL 6.8423 mL 13.6846 mL
    查看完整储备液配制表

    * 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。-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。

    * 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

    • 摩尔计算器

    • 稀释计算器

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    质量
    =
    浓度
    ×
    体积
    ×
    分子量 *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    浓度 (start)

    C1

    ×
    体积 (start)

    V1

    =
    浓度 (final)

    C2

    ×
    体积 (final)

    V2

    In Vivo:

    请根据您的 实验动物和给药方式 选择适当的溶解方案。

    以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:
    ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用
    以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

    • 方案 一

      请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.08 mg/mL (14.23 mM); 澄清溶液

      此方案可获得 ≥ 2.08 mg/mL(饱和度未知)的澄清溶液。

      1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;再向上述体系中加入 50 μL Tween-80,混合均匀;然后再继续加入 450 μL 生理盐水 定容至 1 mL

      生理盐水的配制:将 0.9 g 氯化钠,溶解于 ddH₂O 并定容至 100 mL,可以得到澄清透明的生理盐水溶液。
    • 方案 二

      请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.08 mg/mL (14.23 mM); 澄清溶液

      此方案可获得 ≥ 2.08 mg/mL(饱和度未知)的澄清溶液。

      1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中,混合均匀。

      20% SBE-β-CD in Saline 的配制(4°C,储存一周):2 g SBE-β-CD(磺丁基醚 β-环糊精)粉末定容于 10 mL 的生理盐水中,完全溶解至澄清透明。
    动物溶解方案计算器
    请输入动物实验的基本信息:

    给药剂量

    mg/kg

    动物的平均体重

    g

    每只动物的给药体积

    μL

    动物数量

    由于实验过程有损耗,建议您多配一只动物的量
    请输入您的动物体内配方组成:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    如果您的动物是免疫缺陷鼠或者体弱鼠,建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
    方案所需 助溶剂 包括:DMSO ,均可在 MCE 网站选购。 Tween 80,均可在 MCE 网站选购。
    计算结果
    工作液所需浓度 : mg/mL
    储备液配制方法 : mg 药物溶于 μL  DMSO(母液浓度为 mg/mL)。
    您所需的储备液浓度超过该产品的实测溶解度,以下方案仅供参考,如有需要,请与 MCE 中国技术支持联系。
    动物实验体内工作液的配制方法 : 取 μL DMSO 储备液,加入 μL  μL ,混合均匀至澄清,再加 μL Tween 80,混合均匀至澄清,再加 μL 生理盐水
    连续给药周期超过半月以上,请谨慎选择该方案。
    请确保第一步储备液溶解至澄清状态,从左到右依次添加助溶剂。您可采用超声加热 (超声清洗仪,建议频次 20-40 kHz),涡旋吹打等方式辅助溶解。
    纯度 & 产品资料

    纯度: 99.90%

    参考文献
    Cell Assay
    [1]

    Cell viability is analyzed using Cell Counting Kit-8. Briefly, 1×104 cells are inoculated into 96-well plates. After being treated, 90 μL of medium and 10 μL of CCK-8 solution are added to each well. The cells are then incubated at 37°C for 2 h. After incubation, the absorption at 450 nm is measured using an Infinite™ M200 Microplate Reader. The results are expressed as a percentage of the control. The cell death is also evaluated using the trypan blue assay. HepG2 cells are plated in the 6-well plates (5×105 cells per well) and incubated for 24 h. After being treated with Cd or melatonin, the cells are detached with 300 μL trypsin-EDTA solution. The mixture of detached cells is centrifugated at 300 g for 5 min. Then, the residue is combined with 800 μL trypan blue solution and dispersed. After 3 min staining, cells are counted using an automated cell counter. The dead cells are stained with the blue color. Cell mortality (%) is expressed as percentage of the dead cell number/the total cell number.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [2]

    In brief, male C57BL/6 mice are anesthetized with 2% isoflurane, and myocardial ischemia is produced by temporarily exteriorizing the heart via a left thoracic incision and placing a 6-0 silk suture slipknot around the left anterior descending coronary artery. After 30 minutes of myocardial ischemia, the slipknot is released, and the myocardium is reperfused for 3 hour (for western blot analysis and oxidative stress measurement) or 24 hour (for cardiac function, apoptotic index and infarct size determination). Sham-operated mice undergo the same surgical procedures except the suture placed under the left coronary artery is not tied. Ten minutes before reperfusion, mice are randomized to receive either vehicle (1% ethanol) or melatonin (20 mg/kg) by intraperitoneal injection. C57BL/6 mice are randomly divided into the following groups: (i) Sham group: mice underwent the sham operation and are treated with vehicle (1% ethanol); (ii) Mel group: mice are treated with melatonin (20 mg/kg via intraperitoneal injection); (iii) IR+V group: mice underwent the MI/R operation and are treated with vehicle (1% ethanol); (iv) IR+Mel group: mice underwent the MI/R operation and are treated with melatonin (20 mg/kg via intraperitoneal injection 10 minutes before reperfusion); (v) IR+Mel+3-TYP group: mice are pretreated with 3-TYP (3-TYP is intraperitoneally injected at a dose of 50 mg/kg every 2 days for a total of three doses prior to the MI/R surgery), subjected to the MI/R operation, and treated with melatonin (20 mg/kg via intraperitoneal injection 10 minutes before reperfusion); and (vi) IR+3-TYP group: mice are pretreated with 3-TYP and then subjected to the MI/R operation.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    参考文献

    完整储备液配制表

    * 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。-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。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    H2O / Ethanol / DMSO 1 mM 6.8423 mL 34.2114 mL 68.4229 mL 171.0571 mL
    5 mM 1.3685 mL 6.8423 mL 13.6846 mL 34.2114 mL
    Ethanol / DMSO 10 mM 0.6842 mL 3.4211 mL 6.8423 mL 17.1057 mL
    15 mM 0.4562 mL 2.2808 mL 4.5615 mL 11.4038 mL
    20 mM 0.3421 mL 1.7106 mL 3.4211 mL 8.5529 mL
    25 mM 0.2737 mL 1.3685 mL 2.7369 mL 6.8423 mL
    30 mM 0.2281 mL 1.1404 mL 2.2808 mL 5.7019 mL
    40 mM 0.1711 mL 0.8553 mL 1.7106 mL 4.2764 mL
    50 mM 0.1368 mL 0.6842 mL 1.3685 mL 3.4211 mL
    60 mM 0.1140 mL 0.5702 mL 1.1404 mL 2.8510 mL
    80 mM 0.0855 mL 0.4276 mL 0.8553 mL 2.1382 mL
    100 mM 0.0684 mL 0.3421 mL 0.6842 mL 1.7106 mL

    * 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

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      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    目录号:
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