GSK5959 --- BRPF1 Bromodomain Inhibitor

Catalog No. size PriceQuantity
M60239-2S 2 mg solid $129
M60239-10S 10mg solid $536
M60239-100S 100mg solid $1,620


GSK5959 is a potent, selective and cell permeable BRPF1 bromodomain inhibitor with IC50 ~ 80 nM. It has >100-fold selectivity for BRPF1 over a panel of 35 other bromodomains, including BRPF2/3 and BET family bromodomains. A cellular protein interaction assay measuring the displacement of NanoLuc-tagged BRPF1 bromodomain from Halotagged histone H3.3 was employed to demonstrate GSK5959’s cell permeability and disruption of chromatin binding with IC50 ~0.98 µM.

Product information

CAS Number: 901245-65-6

Molecular Weight: 394.47

Formula: C22H26N4O3



GSK 5959

Chemical Name: N-(1,3-dimethyl-2-oxo-6-(piperidin-1-yl)-2,3-dihydro-1H-benzo[d]imidazol-5-yl)-2-methoxybenzamide

Smiles: COC1=CC=CC=C1C(=O)NC1=CC2=C(C=C1N1CCCCC1)N(C)C(=O)N2C


InChi: InChI=1S/C22H26N4O3/c1-24-18-13-16(23-21(27)15-9-5-6-10-20(15)29-3)17(26-11-7-4-8-12-26)14-19(18)25(2)22(24)28/h5-6,9-10,13-14H,4,7-8,11-12H2,1-3H3,(H,23,27)

Technical Data

Appearance: Solid Power.

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO up to 10 mM

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

How to use

In Vitro:

GSK5959 was used at 10 µM final concentration in various in vitro assays. GSK-5959 (3a) also displays selectivity over the closely related family members, BRPF2 (100-fold) and BRPF3 (>1000-fold). GSK-5959 (3a) exhibits an EC50 = 0.98 μM) in cellular NanoBRET assay. GSK-5959 has no effect on TRIM24 SUMOylation.


  1. Demont EH, et al. 1,3-Dimethyl Benzimidazolones Are Potent, Selective Inhibitors of the BRPF1 Bromodomain. (2014) ACS Med Chem Lett. 5(11):1190-5.
  2. Wylie S.Palmer, et al. Development of small molecule inhibitors of BRPF1 and TRIM24 bromodomains Discovery Today: Technologies Volume 19, March 2016, Pages 65-71.
  3. Srikanth Appikonda, et al. Cross-talk between chromatin acetylation and SUMOylation of tripartite motif-containing protein 24 (TRIM24) impacts cell adhesionJ Biol Chem. 2018 May 11;293(19):7476-7485.

Products are for research use only. Not for human use.


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