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

GSK2606414 是可渗透细胞且有口服活性的蛋白激酶 R 样内质网 (ER) 激酶 (PERK) 抑制剂，IC50值为 0.4 nM。

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GSK2606414 Chemical Structure

GSK2606414 Chemical Structure

CAS No. : 1337531-36-8

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规格 价格 是否有货 数量
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
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Customer Review

GSK2606414 相关抗体

Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 82 篇科研文献

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: 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: 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: 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

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    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)

    细胞效力
    (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]
    体外研究
    (In Vitro)

    GSK2606414 抑制细胞中的 PERK 激活[1]。

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

    GSK2606414 相关抗体:
    体内研究
    (In Vivo)

    GSK2606414（50 和 150 mg/kg，口服）可抑制小鼠体内人类肿瘤异种移植瘤的生长[1]。

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

    451.44

    Formula

    C24H20F3N5O
    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

    4°C, protect from light

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

    溶解性数据
    细胞实验： 

    DMSO 中的溶解度 : ≥ 100 mg/mL (221.51 mM; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

    * "≥" means soluble, but saturation unknown.

    配制储备液
    浓度 溶剂体积 质量 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 (protect from light)。-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。

    • 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

    动物实验：

    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: ≥ 2.5 mg/mL (5.54 mM); 澄清溶液

      此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。

      以 1 mL 工作液为例，取 100 μL 25.0 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: 2.5 mg/mL (5.54 mM); 悬浊液; 超声助溶

      此方案可获得 2.5 mg/mL的均匀悬浊液，悬浊液可用于口服和腹腔注射。

      以 1 mL 工作液为例，取 100 μL 25.0 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。

      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。

    以下溶解方案，请直接配制工作液。建议现用现配，在短期内尽快用完。 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： 0.5% HPMC/0.2% Tween-80 in Saline water

      Solubility: 3.33 mg/mL (7.38 mM); 悬浊液; 超声助溶

    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

    只
    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）。

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

    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: 99.91%

    COA (203 KB) LCMS (94 KB)

    产品使用指南 (1538 KB)
    参考文献
    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.
    参考文献

    GSK2606414 相关分类

    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 (protect from light)。-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
    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.

    Keywords:

    GSK26064141337531-36-8GSK 2606414GSK-2606414PERKAutophagyApoptosisProtein kinase R-like endoplasmic reticulum kinasePKR-like endoplasmic reticulum kinaseInhibitorinhibitorinhibit

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