Home Epigenetics Epigenetic Reader Domain inhibitor GSK 5959 For research use only.

GSK 5959

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 Chemical Structure

GSK 5959 Chemical Structure

CAS No. 901245-65-6

Purity & Quality Control

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

GSK 5959 Related Products

Signaling Pathway

Epigenetic Reader Domain Signaling Pathways

Epigenetic Reader Domain Signaling Pathway

Biological Activity

Description 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.
Targets
BRPF1 [1]
(TR-FRET)		 BRPF2 [1]
(TR-FRET)		 BRPF3 [1]
(TR-FRET)
7.1(pIC50) 5.2(pIC50) 4.5(pIC50)
In vitro
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].

Chemical Information & Solubility

Molecular Weight 394.47 Formula

C22H26N4O3
CAS No. 901245-65-6 SDF --
Smiles CN1C2=C(C=C(C(=C2)NC(=O)C3=CC=CC=C3OC)N4CCCCC4)N(C1=O)C
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 6 mg/mL ( (15.21 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 3 mg/mL

Water : Insoluble


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In vivo
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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.

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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

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