Home Epigenetics Epigenetic Reader Domain inhibitor GSK2801

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GSK2801 Epigenetic Reader Domain inhibitor

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

GSK2801 Epigenetic Reader Domain inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 371.45

Purity & Quality Control

Batch: S723101 DMSO]74 mg/mL]false]Ethanol]7 mg/mL]false]Water]Insoluble]false Purity: 99.98%
99.98

Related Products

Signaling Pathway

Epigenetic Reader Domain Signaling Pathways

Epigenetic Reader Domain Signaling Pathway

Mechanism of Action

Targets
BAZ2B [1] BAZ2A [1]
136 nM(Kd) 257 nM(Kd)

In vitro
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 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]
Animal Research Animal Models Male CD1 mice
Dosages 30 mg/kg
Administration i.p., p.o.

References
  • https://pubmed.ncbi.nlm.nih.gov/25799074/

Chemical Information

Molecular Weight 371.45 Formula

C20H21NO4S
CAS No. 1619994-68-1 SDF Download SDF
Synonyms N/A
Smiles CCCOC1=CC2=C(C=C(N2C=C1)C(=O)C)C3=CC=CC=C3S(=O)(=O)C

Storage and Stability

Storage (From the date of receipt)

In vitro
Batch:

DMSO : 74 mg/mL ( (199.21 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 7 mg/mL

Water : Insoluble


Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

Preparing Stock Solutions

Molarity Calculator

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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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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.

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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