GSK2606414

Name: GSK2606414
Brand: MedChemExpress
SKU: HY-18072
Rating: 5.0 (121 reviews)

製品番号: HY-18072 純度: 99.91%: Data Sheet SDS COA 取扱説明書
FAQs
Technical Support

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.

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。

CAS 番号 : 1337531-36-8

容量	価格（税別）	在庫状況	数量

>無料サンプル (0.1 - 0.2 mg)		今すぐ申し込む
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 130	在庫あり	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 130	在庫あり	Estimated Time of Arrival: December 31
Solid
5 mg	$119	在庫あり	Estimated Time of Arrival: December 31
10 mg	$156	在庫あり	Estimated Time of Arrival: December 31
25 mg	$280	在庫あり	Estimated Time of Arrival: December 31
50 mg	$420	在庫あり	Estimated Time of Arrival: December 31
100 mg	$648	在庫あり	Estimated Time of Arrival: December 31
250 mg	$1040	在庫あり	Estimated Time of Arrival: December 31
500 mg	$1407	在庫あり	Estimated Time of Arrival: December 31
1 g	$1900	在庫あり	Estimated Time of Arrival: December 31
5 g		お問い合わせ
10 g		お問い合わせ

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* アイテムを追加する前、数量をご選択ください

This product is a controlled substance and not for sale in your territory.

カスタマーレビュー

Based on 121 publication(s) in Google Scholar

顧客検証

Cell Proliferation/Viability Assay

: GSK2606414 purchased from MedChemExpress. 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 MedChemExpress. Usage Cited in: Microbiol Spectr. 2022 Dec 21;10(6):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 MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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.

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製品説明

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)

Cellular Effect

Cell Line	Type	Value	Description	References
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]
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]
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
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
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]

体外実験

GSK2606414 inhibits PERK activation in cells^[1].

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

体内実験

GSK2606414 (50 and 150 mg/kg, p.o.) inhibits the growth of a human tumor xenograft in mice^[1].

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

分子量

451.44

分子式

C₂₄H₂₀F₃N₅O

CAS 番号

1337531-36-8

Appearance

Solid

Color

White to off-white

SMILES

NC1=C2C(N(C)C=C2C3=CC4=C(N(C(CC5=CC=CC(C(F)(F)F)=C5)=O)CC4)C=C3)=NC=N1

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

4°C, protect from light

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

溶剤 & 溶解度

体外:

DMSO : 90.91 mg/mL (201.38 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	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
10 mM	0.2215 mL	1.1076 mL	2.2151 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

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

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

一般には略語で表示されます：C₁V₁ = C₂V₂

濃度 _（開始）

体積 _（開始）

濃度 _（終了）

体積 _（終了）

体内:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.54 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (5.54 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 5% DMSO 40% PEG300 5% Tween-80 50% Saline
Solubility: ≥ 2.5 mg/mL (5.54 mM); Clear solution

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 0.5% HPMC/0.2% Tween-80 in Saline water
Solubility: 3.33 mg/mL (7.38 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

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

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

純度とドキュメンテーション

純度: 99.91%

Select Batch:

データシート (282 KB) SDS (392 KB)

COA (259 KB) LCMS (93 KB)

取扱説明書 (2659 KB)

参考文献

[1]. Axten JM, et al. Discovery of 7-methyl-5-(1-{[3-(trifluoromethyl)phenyl]acetyl}-2,3-dihydro-1H-indol-5-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine (GSK2606414), a potent and selective first-in-class inhibitor of protein kinase R (PKR)-like endoplasmic reticulu [Content Brief]

[2]. Zhang M, et al. Inhibiting the Plasmodium eIF2α Kinase PK4 Prevents Artemisinin-Induced Latency. Cell Host Microbe. 2017 Dec 13;22(6):766-776.e4. [Content Brief]

動物実験
^[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.

MedChemExpress (MCE) はこれらの方法の精度を確認していません。こちらは参照専用です。

参考文献

[1]. Axten JM, et al. Discovery of 7-methyl-5-(1-{[3-(trifluoromethyl)phenyl]acetyl}-2,3-dihydro-1H-indol-5-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine (GSK2606414), a potent and selective first-in-class inhibitor of protein kinase R (PKR)-like endoplasmic reticulu [Content Brief]

[2]. Zhang M, et al. Inhibiting the Plasmodium eIF2α Kinase PK4 Prevents Artemisinin-Induced Latency. Cell Host Microbe. 2017 Dec 13;22(6):766-776.e4. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	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

GSK2606414 Related Classifications

Molarity Calculator
Dilution Calculator

The molarity calculator equation

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

質量		濃度		体積		分子量 *
	=		×		×

The dilution calculator equation

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

一般には略語で表示されます：C₁V₁ = C₂V₂

濃度 _（開始）	×	体積 _（開始）	=	濃度 _（終了）	×	体積 _（終了）
	×		=		×
C1		V1		C2		V2

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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GSK2606414

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•関連スクリーニングライブラリ:

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参考文献

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GSK2606414 関連抗体

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

GSK2606414 Related Classifications

Molarity Calculator

Dilution Calculator

The molarity calculator equation

The dilution calculator equation

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