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GSK620

GSK620
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Purity:99.88%
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GSK620

Catalog No. T9020Cas 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.GSK620 is highly selective for the BET-BD2 family of proteins, with >200-fold selectivity over all other bromodomains. GSK620 shows an anti-inflammatory phenotype in human whole blood.
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Pack SizePriceAvailabilityQuantity
1 mg$33In Stock
5 mg$76In Stock
10 mg$122In Stock
25 mg$247In Stock
50 mg$396In Stock
100 mg$589In Stock
500 mg$1,280In Stock
1 mL x 10 mM (in DMSO)$84In Stock
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Product Introduction

Bioactivity
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.GSK620 is highly selective for the BET-BD2 family of proteins, with >200-fol
In vitro
GSK620 showed an anti-inflammatory phenotype in human whole blood, confirming it cellular target engagement.?Human blood samples are stimulated with LPS, which produces a strong immune response. The monocyte chemattractant protein 1 (MCP-1/CCL2) is measured. This is a chemokine which recruits monocytes, memory T cells, and dendritic cells to sites of inflammation. GSK620 reduces the MCP-1 response in a concentration-dependent manner with (an expected) ~1 log drop off in potency relative to the biochemical BRD4 BD2 potencies observed
Chemical Properties
Molecular Weight325.36
FormulaC18H19N3O3
Cas No.2088410-46-0
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year
Solubility Information
DMSO: 45 mg/mL (138.31 mM)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM3.0735 mL15.3676 mL30.7352 mL153.6759 mL
5 mM0.6147 mL3.0735 mL6.1470 mL30.7352 mL
10 mM0.3074 mL1.5368 mL3.0735 mL15.3676 mL
20 mM0.1537 mL0.7684 mL1.5368 mL7.6838 mL
50 mM0.0615 mL0.3074 mL0.6147 mL3.0735 mL
100 mM0.0307 mL0.1537 mL0.3074 mL1.5368 mL

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