Home Epigenetics Epigenetic Reader Domain inhibitor GSK 5959

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GSK 5959 Epigenetic Reader Domain inhibitor

Cat.No.S5916

GSK5959 is a potent and selective BRPF1 bromodomain inhibitor with an IC50 of 80 nM and exhibits >100-fold selectivity for BRPF1 over a panel of 35 other bromodomains, including BRPF2/3 and BET family bromodomains.
GSK 5959 Epigenetic Reader Domain inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 394.47

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: S591601 DMSO]6 mg/mL]false]Ethanol]3 mg/mL]false]Water]Insoluble]false Purity: 99.58%
99.58

Chemical Information, Storage & Stability

Molecular Weight 394.47 Formula

C22H26N4O3

 Storage (From the date of receipt) 3 years -20°C powder
CAS No. 901245-65-6 -- Storage of Stock Solutions

Synonyms N/A Smiles CN1C2=C(C=C(C(=C2)NC(=O)C3=CC=CC=C3OC)N4CCCCC4)N(C1=O)C

Solubility

In vitro
Batch:

DMSO : 6 mg/mL (15.21 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 3 mg/mL

Water : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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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.

Mechanism of Action

Targets/IC50/Ki
BRPF1 [1]
(TR-FRET)
7.1(pIC50)
BRPF2 [1]
(TR-FRET)
5.2(pIC50)
BRPF3 [1]
(TR-FRET)
4.5(pIC50)
In vitro
In the BROMOscan panel of 34 bromodomain binding assays, GSK5959 shows 10 nM BRPF1 inhibition, 90-fold selectivity over BRPF2, and over 500-fold selectivity over all members of the BET family[1].
References

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