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  2. Cell Cycle/DNA Damage Autophagy Apoptosis
  3. PERK Autophagy Apoptosis
  4. GSK2606414

GSK2606414 是可滲透細(xì)胞且有口服活性的蛋白激酶 R 樣內(nèi)質(zhì)網(wǎng) (ER) 激酶 (PERK) 抑制劑，IC50值為 0.4 nM。

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GSK2606414 Chemical Structure

GSK2606414 Chemical Structure

CAS No. : 1337531-36-8

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規(guī)格 價(jià)格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥1092
In-stock
2 mg ￥700
In-stock
5 mg ￥1100
In-stock
10 mg ￥1500
In-stock
25 mg ￥2800
In-stock
50 mg ￥4200
In-stock
100 mg 現(xiàn)貨 詢價(jià)
200 mg   詢價(jià)  
500 mg   詢價(jià)  

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Customer Review

MCE 顧客使用本產(chǎn)品發(fā)表的 90 篇科研文獻(xiàn)

WB
IF
Cell Viability Assay

    GSK2606414 purchased from MCE. Usage Cited in: NPJ Parkinsons Dis. 2023 Mar 7;9(1):35.  [Abstract]

    Co-application of 100?nM GSK2606414 or 100?nM KIRA8 with 10?nM thapsigargin for 48?h significantly mitigate thapsigargin-induced cell death of both the Ctrl and iKO (inducible knockout) midbrain DAergic neurons of mice.

    GSK2606414 purchased from MCE. Usage Cited in: Microbiol Spectr. 2022 Nov 15;e0328222.  [Abstract]

    GSK2606414 (10 μM; 24 h) or C16 (1 μM; 24 h) substantially decreases MGF110-7L-induced phosphorylation of PERK, PKR, and eIF2a in 3D4/21 cells (transfected with an empty Flag vector or a MGF110-7LFlag-expressing vector).

    GSK2606414 purchased from MCE. Usage Cited in: Antimicrob Agents Chemother. 2018 Oct 24;62(11). pii: e01442-18.  [Abstract]

    Extracellular tachyzoites are treated with 1 μM Thapsigargin in the presence of different concentrations of GSK2606414 (PERKi) as indicated or incubated with vehicle (DMSO) for 1 hour.

    GSK2606414 purchased from MCE. Usage Cited in: Neuroscience. 2018 Apr 1;375:34-48.  [Abstract]

    Western blot analysis of p-eIF2α in axotomized DRG spot cultures pretreated with or without GSK2606414 (10?μM) 30?min prior to axotomy. Cells are collected 1?h after axotomy.

    GSK2606414 purchased from MCE. Usage Cited in: PLoS One. 2018 Apr 9;13(4):e0194310.  [Abstract]

    HeLa cells are treated with Tun in the absence or presence of PERK kinase inhibitor GSK2606414 (1 μM) with DMSO as the control. Total cell lysates are prepared, normalized for total protein and immunoblotting of indicated proteins ASB7, CHOP and ATF4 for 6 h in HeLa cells.

    GSK2606414 purchased from MCE. Usage Cited in: Cell Host Microbe. 2017 Dec 13;22(6):766-776.e4.  [Abstract]

    Effects of GSK2606414 on the levels of Plasmodium eIF2a phosphorylation 24 hr after 75 mg/kg GSK2606414 treatment of mice infected with asynchronized P. berghei ANKA (A) and 48 hr after 2 mM GSK2606414 treatment of asynchronized P. falciparum 3D7 parasites in culture (B).

    GSK2606414 purchased from MCE. Usage Cited in: Biochem Biophys Res Commun. 2016 Nov 11;480(2):166-172.  [Abstract]

    An inhibitor of PERK, GSK2606414, is examined. Treatment and immunostaining are performed as per. Note that large CD63 and Rab7 positive vesicles appeared during ER stress when cells are pre-treated with GSK2606414.

    • 生物活性

    • 實(shí)驗(yàn)參考方法

    • 純度 & 產(chǎn)品資料

    • 參考文獻(xiàn)

    生物活性

    GSK2606414 is a cell-permeable and orally available protein kinase R-like endoplasmic reticulum (ER) kinase (PERK) inhibitor with an IC50 of 0.4 nM.

    IC50 & Target[1]

    EIF2AK3 (PERK)

    0.4 nM (IC50)

    EIF2AK1 (HRI)

    420 nM (IC50)

    EIF2AK2 (PKR)

    696 nM (IC50)

    細(xì)胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    A549 IC50
    < 0.03 μM
    Compound: 38, GSK2606414
    Inhibition of thapsigargin-induced autophosphorylation of PERK in human A549 cells after 2 hrs by Western blotting
    Inhibition of thapsigargin-induced autophosphorylation of PERK in human A549 cells after 2 hrs by Western blotting
    		[PMID: 22827572]
    A549 IC50
    < 0.03 μM
    Compound: 1, GSK2606414
    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]
    Caco-2 IC50
    0.25 μM
    Compound: GSK2606414
    Determination of IC50 values for inhibition of SARS-CoV-2 induced cytotoxicity of Caco-2 cells after 48 hours by high content imaging
    Determination of IC50 values for inhibition of SARS-CoV-2 induced cytotoxicity of Caco-2 cells after 48 hours by high content imaging
    		10.21203/rs.3.rs-23951/v1
    Caco-2 CC50
    70.35 μM
    Compound: GSK2606414
    Toxicity against Caco-2 cells determined at 48 hours by intracellular ATP concentration using the CellTiter-Glo Luminescent Cell Viability Assay
    Toxicity against Caco-2 cells determined at 48 hours by intracellular ATP concentration using the CellTiter-Glo Luminescent Cell Viability Assay
    		10.21203/rs.3.rs-23951/v1
    L929 IC50
    0.4 nM
    Compound: 40; GSK'414
    Anti-neprotic activity in mouse L929 cells assessed as reduction in TNF-induced necroptosis and measured every 1 hr by SYTOX Green dye based fluorescence assay
    Anti-neprotic activity in mouse L929 cells assessed as reduction in TNF-induced necroptosis and measured every 1 hr by SYTOX Green dye based fluorescence assay
    		[PMID: 31622096]
    MEF IC50
    7.3 nM
    Compound: 40; GSK'414
    Anti-neprotic activity in mouse MEF cells assessed as reduction in TNF-induced necroptosis and measured every 1 hr in presence of z-VAD by SYTOX Green dye based fluorescence assay
    Anti-neprotic activity in mouse MEF cells assessed as reduction in TNF-induced necroptosis and measured every 1 hr in presence of z-VAD by SYTOX Green dye based fluorescence assay
    		[PMID: 31622096]
    體外研究
    (In Vitro)

    GSK2606414 抑制細(xì)胞中的 PERK 激活[1]。

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

    GSK2606414（50 和 150 mg/kg，口服）可抑制小鼠體內(nèi)人類(lèi)腫瘤異種移植瘤的生長(zhǎng)[1]。

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

    451.44

    Formula

    C24H20F3N5O
    CAS 號(hào)
    性狀

    固體

    顏色

    White to off-white

    運(yùn)輸條件

    Room temperature in continental US; may vary elsewhere.
    儲(chǔ)存方式

    4°C, protect from light

    *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

    溶解性數(shù)據(jù)
    細(xì)胞實(shí)驗(yàn)： 

    DMSO 中的溶解度 : 90.91 mg/mL (201.38 mM; 超聲助溶; 吸濕的 DMSO 對(duì)產(chǎn)品的溶解度有顯著影響，請(qǐng)使用新開(kāi)封的 DMSO)

    配制儲(chǔ)備液
    濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
    1 mM 2.2151 mL 11.0757 mL 22.1513 mL
    5 mM 0.4430 mL 2.2151 mL 4.4303 mL
    查看完整儲(chǔ)備液配制表

    * 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 (protect from light)。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用。

    • 摩爾計(jì)算器

    • 稀釋計(jì)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(dòng)物實(shí)驗(yàn)：

    請(qǐng)根據(jù)您的 實(shí)驗(yàn)動(dòng)物和給藥方式 選擇適當(dāng)?shù)娜芙夥桨浮?

    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(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的方式助溶

    • 方案 一

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

      Solubility: ≥ 2.5 mg/mL (5.54 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(chǔ)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(qǐng)依序添加每種溶劑： 10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: 2.5 mg/mL (5.54 mM); 懸濁液; 超聲助溶

      此方案可獲得 2.5 mg/mL的均勻懸濁液，懸濁液可用于口服和腹腔注射。

      以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲(chǔ)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(qǐng)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(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的方式助溶。

    • 方案 一

      請(qǐng)依序添加每種溶劑： 0.5% HPMC/0.2% Tween-80 in Saline water

      Solubility: 3.33 mg/mL (7.38 mM); 懸濁液; 超聲助溶

    動(dòng)物溶解方案計(jì)算器
    請(qǐng)輸入動(dòng)物實(shí)驗(yàn)的基本信息：

    給藥劑量

    mg/kg

    動(dòng)物的平均體重

    g

    每只動(dòng)物的給藥體積

    μL

    動(dòng)物數(shù)量

    只
    由于實(shí)驗(yàn)過(guò)程有損耗，建議您多配一只動(dòng)物的量
    請(qǐng)輸入您的動(dòng)物體內(nèi)配方組成：
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    如果您的動(dòng)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(guò) 2%。
    方案所需 助溶劑 包括：DMSO， ，均可在 MCE 網(wǎng)站選購(gòu)。 ，Tween 80，均可在 MCE 網(wǎng)站選購(gòu)。
    計(jì)算結(jié)果
    工作液所需濃度 : mg/mL
    儲(chǔ)備液配制方法 : mg 藥物溶于 μL  DMSO（母液濃度為 mg/mL）。

    *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

    您所需的儲(chǔ)備液濃度超過(guò)該產(chǎn)品的實(shí)測(cè)溶解度，以下方案僅供參考，如有需要，請(qǐng)與 MCE 中國(guó)技術(shù)支持聯(lián)系。
    動(dòng)物實(shí)驗(yàn)體內(nèi)工作液的配制方法 : 取 μL DMSO 儲(chǔ)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(guò)半月以上，請(qǐng)謹(jǐn)慎選擇該方案。
    請(qǐng)確保第一步儲(chǔ)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: 99.91%

    參考文獻(xiàn)
    Animal Administration
    [1]

    Exponentially growing BxPC3 tumor cells (10×106 cells/mouse) from cell culture are implanted subcutaneously into the right flank of female nude mice. Sixteen days after implantation, mice with -200 mm3 tumors are randomized into various treatment groups (n=8 mice/group). Animals are orally treated with vehicle (0.5% hydoxypropylmethylcellulose, 0.1% Tween 80 in water, pH 4.8), compound at 50 or 150 mg/kg, b.i.d. for 21 days. Tumor volume is measured twice weekly with calipers and calculated. Results are represented as percent inhibition on completion of dosing, which is 100[1-(average growth of drug-treated population)/(average growth of vehicle-treated control population)]. Statistical analysis is performed using a two-tailed t test.

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

    完整儲(chǔ)備液配制表

    * 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 (protect from light)。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)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 2.2151 mL 11.0757 mL 22.1513 mL 55.3783 mL
    5 mM 0.4430 mL 2.2151 mL 4.4303 mL 11.0757 mL
    10 mM 0.2215 mL 1.1076 mL 2.2151 mL 5.5378 mL
    15 mM 0.1477 mL 0.7384 mL 1.4768 mL 3.6919 mL
    20 mM 0.1108 mL 0.5538 mL 1.1076 mL 2.7689 mL
    25 mM 0.0886 mL 0.4430 mL 0.8861 mL 2.2151 mL
    30 mM 0.0738 mL 0.3692 mL 0.7384 mL 1.8459 mL
    40 mM 0.0554 mL 0.2769 mL 0.5538 mL 1.3845 mL
    50 mM 0.0443 mL 0.2215 mL 0.4430 mL 1.1076 mL
    60 mM 0.0369 mL 0.1846 mL 0.3692 mL 0.9230 mL
    80 mM 0.0277 mL 0.1384 mL 0.2769 mL 0.6922 mL
    100 mM 0.0222 mL 0.1108 mL 0.2215 mL 0.5538 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：
    GSK2606414
    目錄號(hào)：
    HY-18072
    需求量：