GSK2801

Catalog No.S7231

GSK2801 Chemical Structure

Molecular Weight(MW): 371.45

GSK2801 is a selective bromodomains BAZ2A/B inhibitor with KD of 257 nM and 136 nM, respectively.

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Biological Activity

Description GSK2801 is a selective bromodomains BAZ2A/B inhibitor with KD of 257 nM and 136 nM, respectively.
Targets
BAZ2B [1]
()
BAZ2A [1]
()
136 nM(Kd) 257 nM(Kd)
In vitro

In U2OS cells transfected with mutant BAZ2A (N1873F), GSK2801 (1 μM) accelerates FRAP half-recovery time by displacing BAZ2A from chromatin. [1]

In vivo In male CD1 mice, GSK2801 (30 mg/kg, p.o. and i.p.) has reasonable in vivo exposure after oral dosing, modest clearance, and reasonable plasma stability. [1]

Protocol

Animal Research:[1]
+ Expand
  • Animal Models: Male CD1 mice
  • Formulation: 0.5% CMC+1% Tween 80.
  • Dosages: 30 mg/kg
  • Administration: i.p., p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 74 mg/mL warmed (199.21 mM)
Ethanol 7 mg/mL warmed (18.84 mM)
Water Insoluble
In vivo Add solvents individually and in order:
0.5% CMC+1% Tween 80
30mg/mL

* 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 371.45
Formula

C20H21NO4S

CAS No. 1619994-68-1
Storage powder
Synonyms N/A

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

Mass (g) = Concentration (mol/L) × Volume (L) × 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 MSDS / COA (available on product pages).

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Dilution Calculator

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

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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 MSDS / 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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Epigenetic Reader Domain Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID