1. Epigenetics
  2. Epigenetic Reader Domain
  3. GSK-5959

GSK-5959 

Cat. No.: HY-18665 Purity: 98.29%
Handling Instructions

GSK-5959 is a potent, selective and cell permeable BRPF1 bromodomain inhibitor with an IC50 of ~ 80 nM.

For research use only. We do not sell to patients.

GSK-5959 Chemical Structure

GSK-5959 Chemical Structure

CAS No. : 901245-65-6

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Free Sample (0.5-1 mg)   Apply Now  
10 mM * 1 mL in DMSO USD 66 In-stock
Estimated Time of Arrival: December 31
5 mg USD 60 In-stock
Estimated Time of Arrival: December 31
10 mg USD 100 In-stock
Estimated Time of Arrival: December 31
50 mg USD 290 In-stock
Estimated Time of Arrival: December 31
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Description

GSK-5959 is a potent, selective and cell permeable BRPF1 bromodomain inhibitor with an IC50 of ~ 80 nM[1].

IC50 & Target

IC50: 80 nM (BRPF1)[1].

In Vitro

GSK-5959 (3a) also displays selectivity over the closely related family members, BRPF2 (100-fold) and BRPF3 (>1000-fold)[2].
GSK-5959 (3a) exhibits an EC50 = 0.98 μM) in cellular NanoBRET assay[2].
GSK-5959 has no effect on TRIM24 SUMOylation[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

394.47

Formula

C₂₂H₂₆N₄O₃

CAS No.
SMILES

O=C(NC1=C(N2CCCCC2)C=C(N3C)C(N(C)C3=O)=C1)C4=CC=CC=C4OC

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 13 mg/mL (32.96 mM; Need ultrasonic and warming)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5350 mL 12.6752 mL 25.3505 mL
5 mM 0.5070 mL 2.5350 mL 5.0701 mL
10 mM 0.2535 mL 1.2675 mL 2.5350 mL
*Please refer to the solubility information to select the appropriate solvent.
References
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Keywords:

GSK-5959GSK5959GSK 5959Epigenetic Reader DomainBRPF1BRPF2BRD1BRPF3bromodomainepigeneticsInhibitorinhibitorinhibit

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GSK-5959
Cat. No.:
HY-18665
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