GSK620

For research use only.

Catalog No.S9685

GSK620 Chemical Structure

CAS No. 2088410-46-0

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.

Purity & Quality Control

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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

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]

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]

Protocol

Cell Research:

[1]

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  • 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.


    (Only for Reference)
Animal Research:

[1]

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  • Animal Models: Male Wistar Han rats, male Beagle dog
  • Dosages: 0.5 mg/kg, 1 mg/kg, 3 mg/kg
  • Administration: IV, Oral gavage
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 65 mg/mL (199.77 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 325.36
Formula

C18H19N3O3

CAS No. 2088410-46-0
Storage powder
in solvent
Synonyms N/A

In vivo Formulation Calculator (Clear solution)

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

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

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*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and SDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

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* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / COA (available online).

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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

Tel: +1-832-582-8158 Ext:3

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID