1. Epigenetics
  2. Epigenetic Reader Domain

GSK-5959 

Cat. No.: HY-18665 Purity: 98.42%
Handling Instructions

GSK-5959 is a potent, selective and cell permeable BRPF1 bromodomain inhibitor with IC50 ~ 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

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 132 In-stock
Estimated Time of Arrival: December 31
5 mg USD 120 In-stock
Estimated Time of Arrival: December 31
10 mg USD 192 In-stock
Estimated Time of Arrival: December 31
50 mg USD 900 In-stock
Estimated Time of Arrival: December 31
100 mg   Get quote  
200 mg   Get quote  

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  • Biological Activity

  • Technical Information

  • Purity & Documentation

  • References

Description

GSK-5959 is a potent, selective and cell permeable BRPF1 bromodomain inhibitor with IC50 ~ 80 nM. Exhibits >100-fold selectivity for BRPF1 over a panel of 35 other bromodomains, including BRPF2/3 and BET family bromodomains. IC50 value: 80 nM Target: BRPF1 in vitro: GSK-5959 inhibits BRPF1 interaction with histone H3. A cellular protein interaction assay measuring the displacement of NanoLuc-tagged BRPF1 bromodomain from Halotagged histone H3 is employed to demonstrate GSK-5959 is cell permeability and disruption of chromatin binding with IC50 of 0.98 μM. GSK-5959 is used at 10 μM final concentration in various in vitro assays.

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
Molecular Weight

394.47

Formula

C₂₂H₂₆N₄O₃

CAS No.

901245-65-6

SMILES

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

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
GSK-5959
Cat. No.:
HY-18665
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GSK-5959

Cat. No.: HY-18665