Home Epigenetics Epigenetic Reader Domain inhibitor GSK620 For research use only.

GSK620

GSK620 is a pan-BD2 inhibitor, which shows an anti-inflammatory phenotype in human whole blood with excellent broad selectivity, developability, and in vivo oral pharmacokinetics.

GSK620 Chemical Structure

GSK620 Chemical Structure

CAS No. 2088410-46-0

Purity & Quality Control

GSK620 Related Products

Signaling Pathway

Epigenetic Reader Domain Signaling Pathways

Epigenetic Reader Domain Signaling Pathway

Biological Activity

Description GSK620 is a pan-BD2 inhibitor, which shows an anti-inflammatory phenotype in human whole blood with excellent broad selectivity, developability, and in vivo oral pharmacokinetics.
Targets
BD2 [1]
In vitro
In vitro

GSK620 is highly selective for the BET-BD2 family of proteins, with >200-fold selectivity over all other bromodomains. GSK620 is capable of reducing the MCP-1 response in a concentration-dependent manner, providing strong evidence that GSK620 is indeed engaging BD2 in cells.[1]
Cell Research Cell lines human whole blood, hepatocytes
Concentrations 0.5 μM
Incubation Time 60 min, 120 min
Method

GSK620 is diluted in 100% DMSO to give a range of appropriate concentrations at 140× the required final assay concentration, of which 1 μL is added to a 96 well tissue culture plate. Then 130 μL of human whole blood, collected into sodium heparin anticoagulant (1 unit/mL final) is added to each well and plates are incubated at 37℃ (5% CO2) for 30 min before the addition of 10 μL of 2.8 μg/mL LPS, diluted in complete RPMI 1640 (final concentration 200 ng/mL), to give a total volume of 140 μL per well. After further incubation for 24 h at 37℃, 140 μL of PBS is added to each well. The plates are sealed, shaken for 10 min, and then centrifuged (2500 rpm × 10 min). Finally, 100 μL of the supernatant is removed and MCP-1 levels assayed immediately by immunoassay.
In Vivo
In vivo

GSK620 is a potent and selective pan-BD2 inhibitor with excellent in vivo PK properties and excellent developability properties, with the exception of moderate FaSSIF solubility driven by its highly crystalline nature.[1]
Animal Research Animal Models Male Wistar Han rats, male Beagle dog
Dosages 0.5 mg/kg, 1 mg/kg, 3 mg/kg
Administration IV, Oral gavage

Chemical Information & Solubility

Molecular Weight 325.36 Formula

C18H19N3O3
CAS No. 2088410-46-0 SDF --
Smiles CNC(=O)C1=CC(=CN(CC2=CC=CC=C2)C1=O)C(=O)NC3CC3
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 65 mg/mL ( (199.77 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
Batch:

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In vivo Formulation Calculator

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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.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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