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  2. Metabolic Enzyme/Protease
  3. Pyruvate Kinase
  4. TEPP-46

TEPP-46 (ML-265) 是一種有效，選擇性的丙酮酸激酶 M2 (pyruvate kinase M2; PKM2) 激活劑，AC50 值為 92 nM，對 PKM1，PKL 和 PKR 作用較小或沒有作用。

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TEPP-46 Chemical Structure

TEPP-46 Chemical Structure

CAS No. : 1221186-53-3

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規(guī)格 價格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥717
In-stock
1 mg ￥371
In-stock
5 mg ￥875
In-stock
10 mg ￥1320
In-stock
25 mg ￥1975
In-stock
50 mg ￥2700
In-stock
100 mg ￥4250
In-stock
500 mg 現(xiàn)貨 詢價
1 g   詢價  
5 g   詢價  

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Customer Review

MCE 顧客使用本產(chǎn)品發(fā)表的 39 篇科研文獻

WB
IF

    TEPP-46 purchased from MCE. Usage Cited in: Cell Rep. 2020 May 26;31(8):107690.  [Abstract]

    Analysis of enzymatic activity of PKM2. Protein level of PKM2 is analyzed using Western Blotting.

    TEPP-46 purchased from MCE. Usage Cited in: Cell Rep. 2020 May 26;31(8):107690.  [Abstract]

    Immunofluorescence of PKM2 in DCs. When added TEPP-46 to prevent the dissociation of PKM2 tetramers, LPS-induced accumulation of nuclear PKM2 as well as IL-12 expression is diminished.

    • 生物活性

    • 實驗參考方法

    • 純度 & 產(chǎn)品資料

    • 參考文獻

    生物活性

    TEPP-46 (ML-265) is a potent and selective pyruvate kinase M2 (PKM2) activator with an AC50 of 92 nM, showing little or no effect on PKM1, PKL and PKR[1].

    細胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    A549 IC50
    > 100 μM
    Compound: TEPP-46
    Cytotoxicity against human A549 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
    Cytotoxicity against human A549 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
    		[PMID: 34847663]
    C6 IC50
    81.8 μM
    Compound: TEPP-46
    Antiproliferative activity against rat C6 cells assessed as reduction in cell viability after 72 hrs by MTT assay
    Antiproliferative activity against rat C6 cells assessed as reduction in cell viability after 72 hrs by MTT assay
    		[PMID: 31977207]
    HCT-116 IC50
    89.91 μM
    Compound: TEPP-46
    Cytotoxicity against human HCT-116 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
    Cytotoxicity against human HCT-116 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
    		[PMID: 34847663]
    HepG2 IC50
    > 100 μM
    Compound: TEPP-46
    Cytotoxicity against human HepG2 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
    Cytotoxicity against human HepG2 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
    		[PMID: 34847663]
    HT-29 IC50
    > 100 μM
    Compound: TEPP-46
    Cytotoxicity against human HT-29 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
    Cytotoxicity against human HT-29 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
    		[PMID: 34847663]
    MDA-MB-231 IC50
    > 100 μM
    Compound: TEPP-46
    Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
    Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
    		[PMID: 34847663]
    NIH3T3 IC50
    56.58 μM
    Compound: TEPP-46
    Cytotoxicity against mouse 3T3 cells assessed as reduction in cell viability after 72 hrs by MTT assay
    Cytotoxicity against mouse 3T3 cells assessed as reduction in cell viability after 72 hrs by MTT assay
    		[PMID: 31977207]
    SF-126 IC50
    88.98 μM
    Compound: TEPP-46
    Antiproliferative activity against human SF126 cells assessed as reduction in cell viability after 72 hrs by MTT assay
    Antiproliferative activity against human SF126 cells assessed as reduction in cell viability after 72 hrs by MTT assay
    		[PMID: 31977207]
    SW480 IC50
    92.95 μM
    Compound: TEPP-46
    Cytotoxicity against human SW480 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
    Cytotoxicity against human SW480 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
    		[PMID: 34847663]
    U-118-MG IC50
    85 μM
    Compound: TEPP-46
    Antiproliferative activity against human U118MG cells assessed as reduction in cell viability after 72 hrs by MTT assay
    Antiproliferative activity against human U118MG cells assessed as reduction in cell viability after 72 hrs by MTT assay
    		[PMID: 31977207]
    U-251 IC50
    65.43 μM
    Compound: TEPP-46
    Antiproliferative activity against human U251 cells assessed as reduction in cell viability after 72 hrs by MTT assay
    Antiproliferative activity against human U251 cells assessed as reduction in cell viability after 72 hrs by MTT assay
    		[PMID: 31977207]
    U2OS IC50
    > 100 μM
    Compound: TEPP-46
    Cytotoxicity against human U2OS cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
    Cytotoxicity against human U2OS cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
    		[PMID: 34847663]
    U-87MG ATCC IC50
    86.3 μM
    Compound: TEPP-46
    Antiproliferative activity against human U87 cells assessed as reduction in cell viability after 72 hrs by MTT assay
    Antiproliferative activity against human U87 cells assessed as reduction in cell viability after 72 hrs by MTT assay
    		[PMID: 31977207]
    體外研究
    (In Vitro)

    TEPP-46 和 DASA-58 通過類似于內(nèi)源性激活劑 FBP 的機制激活 PKM2。用 TEPP-46 或 DASA-58 預(yù)處理細胞可防止過釩酸鹽誘導(dǎo)的 PKM2 活性抑制。TEPP-46 還會誘導(dǎo)細胞內(nèi)乙酰輔酶 A、乳酸、核糖磷酸和絲氨酸水平降低[1]。
    TEPP-46 抑制 LPS 誘導(dǎo)的 Hif-1α 和 IL-1β，以及一系列其他 Hif-1α 依賴性基因的表達。TEPP-46 處理顯著下調(diào) M1 標志物 Il12p40 和 Cxcl-10 的表達。使用 TEPP-46 激活 PKM2 可顯著抑制 FSL-1 和 CpG 誘導(dǎo)的 Il1b mRNA 表達。 TEPP-46 抑制 Mtb 誘導(dǎo)的 Il1b mRNA 水平，提高 Mtb 誘導(dǎo)的 Il10 mRNA 水平，對 Tnf 水平?jīng)]有影響[2]。

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    體內(nèi)研究
    (In Vivo)

    TEPP-46 具有良好的口服生物利用度，其清除率相對較低，半衰期長，且分布容積參數(shù)良好，這些參數(shù)預(yù)示著 TEPP-46 在腫瘤組織中的藥物暴露量較高。在 150 mg/kg 的劑量下，TEPP-46 能夠輕易地在 A549 異種移植腫瘤中實現(xiàn) PKM2 的最大活化[1]。

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

    372.46

    Formula

    C17H16N4O2S2
    CAS 號
    性狀

    固體

    顏色

    White to light yellow

    運輸條件

    Room temperature in continental US; may vary elsewhere.
    儲存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    溶解性數(shù)據(jù)
    細胞實驗： 

    DMSO 中的溶解度 : 50 mg/mL (134.24 mM; 超聲助溶; 吸濕的 DMSO 對產(chǎn)品的溶解度有顯著影響，請使用新開封的 DMSO)

    配制儲備液
    濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
    1 mM 2.6849 mL 13.4243 mL 26.8485 mL
    5 mM 0.5370 mL 2.6849 mL 5.3697 mL
    查看完整儲備液配制表

    * 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, 2 years; -20°C, 1 year。-80°C儲存時，請在2年內(nèi)使用， -20°C儲存時，請在1年內(nèi)使用。

    • 摩爾計算器

    • 稀釋計算器

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

    質(zhì)量
    =
    濃度
    ×
    體積
    ×
    分子量 *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    濃度 (start)

    C1

    ×
    體積 (start)

    V1

    =
    濃度 (final)

    C2

    ×
    體積 (final)

    V2

    動物實驗：

    請根據(jù)您的 實驗動物和給藥方式 選擇適當?shù)娜芙夥桨浮?

    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

    • 方案 一

      請依序添加每種溶劑： 5% DMSO    40% PEG300    5% Tween-80    50% Saline

      Solubility: ≥ 2.87 mg/mL (7.71 mM); 澄清溶液

    • 方案 二

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

      Solubility: ≥ 2.5 mg/mL (6.71 mM); 澄清溶液

      此方案可獲得 ≥ 2.5 mg/mL（飽和度未知）的澄清溶液。

      以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲備液加到 400 μL PEG300 中，混合均勻；再向上述體系中加入 50 μL Tween-80，混合均勻；然后再繼續(xù)加入 450 μL 生理鹽水 定容至 1 mL。

      生理鹽水的配制：將 0.9 g 氯化鈉，溶解于 ddH?O 并定容至 100 mL，可以得到澄清透明的生理鹽水溶液。

    以下溶解方案，請直接配制工作液。建議現(xiàn)用現(xiàn)配，在短期內(nèi)盡快用完。 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。

    • 方案 一

      請依序添加每種溶劑： 50% PEG300    50% Saline

      Solubility: 10 mg/mL (26.85 mM); 懸濁液; 超聲助溶

    • 方案 二

      請依序添加每種溶劑： 0.5% CMC-Na/saline water

      Solubility: 5 mg/mL (13.42 mM); 懸濁液; 超聲助溶

    動物溶解方案計算器
    請輸入動物實驗的基本信息：

    給藥劑量

    mg/kg

    動物的平均體重

    g

    每只動物的給藥體積

    μL

    動物數(shù)量

    只
    由于實驗過程有損耗，建議您多配一只動物的量
    請輸入您的動物體內(nèi)配方組成：
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    如果您的動物是免疫缺陷鼠或者體弱鼠，建議 DMSO 中的在最后工作液體系中的占比盡量不超過 2%。
    方案所需 助溶劑 包括：DMSO， ，均可在 MCE 網(wǎng)站選購。 ，Tween 80，均可在 MCE 網(wǎng)站選購。
    計算結(jié)果
    工作液所需濃度 : mg/mL
    儲備液配制方法 : mg 藥物溶于 μL  DMSO（母液濃度為 mg/mL）。
    您所需的儲備液濃度超過該產(chǎn)品的實測溶解度，以下方案僅供參考，如有需要，請與 MCE 中國技術(shù)支持聯(lián)系。
    動物實驗體內(nèi)工作液的配制方法 : 取 μL DMSO 儲備液，加入 μL 。 μL ，混合均勻至澄清，再加 μL Tween 80，混合均勻至澄清，再加 μL 生理鹽水。
    連續(xù)給藥周期超過半月以上，請謹慎選擇該方案。
    請確保第一步儲備液溶解至澄清狀態(tài)，從左到右依次添加助溶劑。您可采用超聲加熱 （超聲清洗儀，建議頻次 20-40 kHz），渦旋吹打等方式輔助溶解。
    純度 & 產(chǎn)品資料

    純度: 99.93%

    參考文獻
    Cell Assay
    [1]

    2,000 cells are seeded in 96-well plates 24 h prior to treatment start. CellTiter96? AQueous is used to assess cell viability following oxidant and PKM2 activator combination treatments. MTS: (3-(4,5-dimethylthiazol-2-yl)-5- (3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium).

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [1]

    H1299 parental and H1299 cells with constitutive expression of a mouse PKM1 cDNA (H1299-PKM1 cells) are propagated in RPMI supplemented with 10% fetal bovine serum, 2 mM glutamine, and hygromycin for transgene selection. Cells are harvested, resuspended in sterile PBS, and 5×105 cells are injected subcutaneously into nu/nu mice. Tumor growth is monitored by caliper measurement, the mice are sacrificed and tumors harvested after the time indicated. Tumors are weighed, divided and either flash-frozen in liquid nitrogen or fixed in formalin for later analysis.

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

    完整儲備液配制表

    * 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, 2 years; -20°C, 1 year。-80°C儲存時，請在2年內(nèi)使用， -20°C儲存時，請在1年內(nèi)使用。

    可選溶劑 濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.6849 mL 13.4243 mL 26.8485 mL 67.1213 mL
    5 mM 0.5370 mL 2.6849 mL 5.3697 mL 13.4243 mL
    10 mM 0.2685 mL 1.3424 mL 2.6849 mL 6.7121 mL
    15 mM 0.1790 mL 0.8950 mL 1.7899 mL 4.4748 mL
    20 mM 0.1342 mL 0.6712 mL 1.3424 mL 3.3561 mL
    25 mM 0.1074 mL 0.5370 mL 1.0739 mL 2.6849 mL
    30 mM 0.0895 mL 0.4475 mL 0.8950 mL 2.2374 mL
    40 mM 0.0671 mL 0.3356 mL 0.6712 mL 1.6780 mL
    50 mM 0.0537 mL 0.2685 mL 0.5370 mL 1.3424 mL
    60 mM 0.0447 mL 0.2237 mL 0.4475 mL 1.1187 mL
    80 mM 0.0336 mL 0.1678 mL 0.3356 mL 0.8390 mL
    100 mM 0.0268 mL 0.1342 mL 0.2685 mL 0.6712 mL
    Help & FAQs
    • Do most proteins show cross-species activity?

      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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    產(chǎn)品名稱：
    TEPP-46
    目錄號：
    HY-18657
    需求量：