Home Epigenetics Epigenetic Reader Domain inhibitor GSK 5959

GSK 5959

Catalog No.S5916

For research use only.

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

CAS No. 901245-65-6

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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 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].

Protocol (from reference)

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 394.47
Formula

C22H26N4O3
CAS No. 901245-65-6
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CN1C2=C(C=C(C(=C2)NC(=O)C3=CC=CC=C3OC)N4CCCCC4)N(C1=O)C

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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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.

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