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GSK2606414 PERK inhibitor

Name: GSK2606414
Brand: Selleck Chemicals
SKU: S7307
Availability: InStock
Rating: 5 (100 reviews)

Cat.No.S7307

GSK2606414 is an orally available, potent, and selective PERK inhibitor with IC50 of 0.4 nM, displaying at least 100-fold selectivity over the other EIF2AKs assayed. This compound impairs GANT-61 induced autophagy in NB cells with MYCN amplification. It exacerbates ER stress-induced apoptosis in HCT116 cells while reduces the apoptosis in SIL1 KD HeLa cells.

Chemical Structure

Molecular Weight: 451.44

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Quality Control

Batch: Purity: 99.92%

99.92

Related Targets	Bcl-2 Caspase PD-1/PD-L1 Ferroptosis p53 Apoptosis related Synthetic Lethality STAT TNF-alpha Ras
Other PERK Inhibitors	GSK2656157 ISRIB (trans-isomer) Azoramide CCT020312 BTdCPU Sal003 AMG PERK 44 MK-28

Solubility in DMSO or Water

In vitro
Batch:

DMSO : 90 mg/mL (199.36 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 19 mg/mL

Water : Insoluble

The solubility data above are all experimental results (not literature values).

DMSO : 90 mg/mL (199.36 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 19 mg/mL

Water : Insoluble

The solubility data above are all experimental results (not literature values).

DMSO : 200 mg/mL (443.02 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 21 mg/mL

Water : Insoluble

The solubility data above are all experimental results (not literature values).

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	4.500mg/ml (9.97mM)	Taking the 1 mL working solution as an example, add 50 μL of 90 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5% DMSO 1 45% PEG 300 2 ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	1.000mg/ml (2.22mM)	Taking the 1 mL working solution as an example, add 50 μL of 20 mg/ml clarified DMSO stock solution to 450 μL PEG 300, mix evenly to clarify it; then continue to add 500 μL ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	10.000mg/ml (22.15mM)	Taking the 1 mL working solution as an example, add 50 μL of 200 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.900mg/ml (1.99mM)	Taking the 1 mL working solution as an example, add 50 μL of 18 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Search directly for a cell line, or select a cell line to find matched working concentrations

GSK2606414 is a potent inhibitor of PERK, GCN2, RIPK1 (< 1000 nM), c-kit (< 1000 nM), AuroraBkinase (< 1000 nM), BRK (< 1000 nM), MAP3K10 (< 1000 nM), c-MER (< 1000 nM), DDR2 (< 1000 nM), MYLK2 (< 1000 nM), IKBKE (1000 nM), TRKC (1000 nM), MAP3K11 (1000 nM), RET (1000 nM), LCK (1000 nM), NEK4 (1000 nM), MAP4K5 (1000 nM), MAP3K9 (1000 nM), TRKA (1000 nM), AXL (1000 nM), TRKB (1000 nM), YES1 (1000 nM), WNK2 (1000 nM). GSK2606414 exhibits the greatest inhibitory potency toward PERK.

Mechanism of Action

Information	GSK2606414 is a specific PERK inhibitor. It affects the PERK/eIF2α/ATF4/CHOP and ISR signaling pathways by blocking PERK and eIF2α phosphorylation, effectively inhibiting ER stress-induced apoptosis, oxidative stress, and extracellular matrix deposition.
Primary Applications and Mechanism of Action

Chemical Information, Storage & Stability

Molecular Weight	451.44	Formula	C₂₄H₂₀F₃N₅O	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	1337531-36-8	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	CN1C=C(C2=C(N=CN=C21)N)C3=CC4=C(C=C3)N(CC4)C(=O)CC5=CC(=CC=C5)C(F)(F)F

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Handling Instructions

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GSK2606414 PERK inhibitor

Molecular Weight: 451.44

Quality Control

Solubility in DMSO or Water

Molarity Calculator

In vivo Formulation Calculator (Clear solution)

Working Concentrations for Cell Culture Treatment

Search directly for a cell line, or select a cell line to find matched working concentrations

Selectivity & Specificity

Mechanism of Action

Chemical Information, Storage & Stability

Tech Support