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  2. Cell Cycle/DNA Damage Autophagy Apoptosis
  3. PERK Autophagy Apoptosis
  4. GSK2656157

GSK2656157 是選擇性，ATP競爭性的 PERK 抑制劑，IC50 值為 0.9 nM。

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GSK2656157 Chemical Structure

GSK2656157 Chemical Structure

CAS No. : 1337532-29-2

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規(guī)格 價格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥770
In-stock
1 mg ￥409
In-stock
5 mg ￥700
In-stock
10 mg ￥1200
In-stock
50 mg ￥2550
In-stock
100 mg ￥4200
In-stock
200 mg   詢價  
500 mg   詢價  

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Customer Review

MCE 顧客使用本產(chǎn)品發(fā)表的 46 篇科研文獻

WB

    GSK2656157 purchased from MCE. Usage Cited in: J Steroid Biochem Mol Biol. 2021, 105893.

    Pretreatment with GSK2656157 (1?μM) alleviated the NEFA-induced increase in protein abundance and mRNA levels of PERK, eIF2α, ATF4, and CHOP vis a vis treatment with 1.2?mM NEFA alone.

    GSK2656157 purchased from MCE. Usage Cited in: Oxid Med Cell Longev. 2020 Jul 27;2020:8291413.  [Abstract]

    GSK2656157 not only inhibits the expression of p-PERK, but also reduces the expression of NRF2 in the nucleus (n-NRF2) and total NRF2 (t-NRF2) proteins.

    GSK2656157 purchased from MCE. Usage Cited in: J Neuroinflammation. 2017 May 11;14(1):104.  [Abstract]

    GSK2656157 treatment suppresses PERK autophosphorylation and TXNIP expression; STF083010 treatment inhibits IRE1α endonuclease activity and TXNIP expression. Representative Western blot and densitometric quantification of protein band optical densities for p-PERK, p-eIF2α/eIF2α, ATF-5, ChREBP, splicing XBP1 (sXBP1) and TXNIP. TXNIP expression is downregulated by GSK2656157 and STF083010 treatment.

    GSK2656157 purchased from MCE. Usage Cited in: Int J Mol Sci. 2017 Apr 18;18(4). pii: E854.  [Abstract]

    GSK2656157 treatment suppresses TXNIP expression and the number of TUNEL-positive cells. TXNIP expression is significantly suppressed by the GSK2656157 (300 μg) treatment.

    • 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

    GSK2656157 is a selective and ATP-competitive inhibitor of protein kinase R (PKR)-like endoplasmic reticulum kinase (PERK) with an IC50 of 0.9 nM.

    IC50 & Target[1]

    EIF2AK3 (PERK)

    0.9 nM (IC50)

    EIF2AK1 (HRI)

    460 nM (IC50)

    BRK

    905 nM (IC50)

    EIF2AK2 (PKR)

    905 nM (IC50)

    MEKK3

    954 nM (IC50)

    Aurora B

    1259 nM (IC50)

    KHS

    1764 nM (IC50)

    LCK

    2344 nM (IC50)

    MLK2

    2796 nM (IC50)

    MEKK3

    2847 nM (IC50)

    ALK5

    3020 nM (IC50)

    MLCK2

    3039 nM (IC50)

    EIF2AK4(GCN2)

    3162 nM (IC50)

    c-MER

    3431 nM (IC50)

    PI3Kγ

    3802 nM (IC50)

    WNK3

    5951 nM (IC50)

    LRRK2

    6918 nM (IC50)

    ROCK1

    7244 nM (IC50)

    MSK1

    8985 nM (IC50)

    NEK1

    9807 nM (IC50)

    AXL

    9808 nM (IC50)

    JAK2

    24547 nM (IC50)

    細胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    A549 IC50
    0.03 μM
    Compound: 6, GSK2656157
    Inhibition of thapsigargin-induced autophosphorylation of PERK in human A549 cells preincubated for 1 hr followed by thapsigargin-induction measured after 1 hr by Western blotting analysis
    Inhibition of thapsigargin-induced autophosphorylation of PERK in human A549 cells preincubated for 1 hr followed by thapsigargin-induction measured after 1 hr by Western blotting analysis
    		[PMID: 24900593]
    體外研究
    (In Vitro)

    GSK2656157 在 BxPC3 胰腺腫瘤細胞系中抑制 PERK 激活并減少下游底物磷酸化-eIF2α、ATF4 和 CHOP，IC50 范圍為 10-30 nM .在 UPR 誘導前暴露于 1 μM GSK2656157 的細胞能夠阻斷這種對蛋白質(zhì)從頭合成的影響[1]。
    GSK2656157 激活另一種 eIF2α 激酶，以補償 HT1080 細胞中 PERK 活性的損失。GSK2656157 抑制 HT1080 細胞的生長[2]。
    GSK2656157 抑制 LPS 誘導的 IL-1β 產(chǎn)生、LPS 誘導的 Caspase 1 激活和 LPS 誘導的 eIF-2α 磷酸化，但不抑制 LPS 誘導的 TNF-α 產(chǎn)生[3]。

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

    GSK2656157 (1.5-150 mg/kg，口服) 導致磷酸化 PERK Thr980 的劑量依賴性抑制，在 50 和 150 mg/kg 時抑制超過 80%。GSK2656157 (50-150 mg/kg，口服) 導致人腫瘤異種移植模型中腫瘤生長的劑量依賴性抑制[1]。

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

    416.45

    Formula

    C23H21FN6O
    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 1 year
    -20°C 6 months
    溶解性數(shù)據(jù)
    細胞實驗： 

    DMSO 中的溶解度 : 8.33 mg/mL (20.00 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 2.4012 mL 12.0062 mL 24.0125 mL
    5 mM 0.4802 mL 2.4012 mL 4.8025 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，避免反復凍融造成的產(chǎn)品失效。
    儲備液的保存方式和期限：-80°C, 1 year; -20°C, 6 months。-80°C儲存時，請在1年內(nèi)使用， -20°C儲存時，請在6個月內(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： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 0.5 mg/mL (1.20 mM); 澄清溶液

      此方案可獲得 ≥ 0.5 mg/mL（飽和度未知）的澄清溶液。

      以 1 mL 工作液為例，取 100 μL 5.0 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。
    • 方案 二

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

      Solubility: ≥ 0.5 mg/mL (1.20 mM); 澄清溶液

      此方案可獲得 ≥ 0.5 mg/mL（飽和度未知）的澄清溶液。

      以 1 mL 工作液為例，取 100 μL 5.0 mg/mL 的澄清 DMSO 儲備液加到 900 μL 20% 的 SBE-β-CD 生理鹽水水溶液 中，混合均勻。

      2 g SBE-β-CD（磺丁基醚 β-環(huán)糊精）粉末定容于 10 mL 的生理鹽水中，完全溶解至澄清透明。

    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： 0.5% HPMC/0.2% Tween-80 in Saline water

      Solubility: 4.17 mg/mL (10.01 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: 99.66%

    參考文獻
    Kinase Assay
    [1]

    BxPC3 (human pancreatic adenocarcinoma) or LL/2 (murine lung carcinoma) cells are treated with DMSO or various concentrations of GSK2656157 for 1 hour, followed by addition of 5 μg/mL tunicamycin or 1 μM thapsigargin for an additional 6 hours to induce endoplasmic reticulum-stress. Cells are lysed in cold radioimmunoprecipitation assay (RIPA) buffer [150 mM NaCl, 50 mM Tris-Cl pH 7.5, 0.25% sodium deoxycholate, 1% NP-40, protease inhibitors, and 100 mM sodium orthovanadate]. Clarified lysates are resolved by SDS-PAGE and transferred to nitrocellulose membrane using NuPAGE system. Blots are incubated with antibodies to total PERK, p-eIF-2α Ser51, total eIF-2α, ATF4, and CHOP. IRDye700DX-labeled goat anti-mouse immunoglobulin G (IgG), IRDye800-CW donkey anti-goat IgG, and IRDye800-CW goat anti-rabbit IgG are used as secondary antibodies. Proteins are detected on the Odyssey Infrared Imager.

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

    BxPC3 cells are treated with DMSO or 1 μM GSK2656157 for 1 hour before adding 5 μg/mL tunicamycin for an additional hour. Cells are metabolically labeled with 125 μCi 35S-methionine for the subsequent 1 hour. Cells are lysed in cold RIPA buffer and lysates are resolved by SDS-PAGE, followed by exposure to a phosphorimager screen. Control cells are also pretreated with 100 μM cyclohexamide for 1 hour followed by metabolic labeling. Radioisotope incorporation is quantitated using ImageQuant 5.2 software.

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

    Exponentially growing HPAC (5×106?cells/mouse), Capan-2 (10×106?cells/mouse), or NCI-H929 (1×6 cells/mouse) cells are implanted subcutaneously into the right flank of 8- to 12-week-old female SCID mice. Similarly, 10×106?BxPC3 cells per mouse are implanted in female nude mice. When the tumors reached approximately 200 mm3?in size, the animals are weighed, and block randomized according to tumor size into treatment groups of 8 mice each. Mice are dosed orally with the formulating vehicle or GSK2656157. Mice are weighed and tumors measured by calipers twice weekly. Tumor volumes are calculated. The percentage of tumor growth inhibition is calculated on each day of tumor measurement using the formula: 100× [1 ? (average growth of the compound-treated tumors/average growth of vehicle-treated control tumors)].

    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，避免反復凍融造成的產(chǎn)品失效。
    儲備液的保存方式和期限：-80°C, 1 year; -20°C, 6 months。-80°C儲存時，請在1年內(nèi)使用， -20°C儲存時，請在6個月內(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 2.4012 mL 12.0062 mL 24.0125 mL 60.0312 mL
    5 mM 0.4802 mL 2.4012 mL 4.8025 mL 12.0062 mL
    10 mM 0.2401 mL 1.2006 mL 2.4012 mL 6.0031 mL
    15 mM 0.1601 mL 0.8004 mL 1.6008 mL 4.0021 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：
    GSK2656157
    目錄號：
    HY-13820
    需求量：