1. Epigenetics
  2. Epigenetic Reader Domain
    Histone Acetyltransferase

GSK 4027 

Cat. No.: HY-101027 Purity: 98.01% ee.: 99.26%
Handling Instructions

GSK 4027 is a chemical probe for the PCAF/GCN5 bromodomain with an pIC50 of 7.4±0.11 for PCAF in a time-resolved fluorescence resonance energy transfer (TR-FRET) assay.

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

GSK 4027 Chemical Structure

GSK 4027 Chemical Structure

CAS No. : 2079896-25-4

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 605 In-stock
Estimated Time of Arrival: December 31
5 mg USD 550 In-stock
Estimated Time of Arrival: December 31
10 mg USD 850 In-stock
Estimated Time of Arrival: December 31
25 mg USD 1750 In-stock
Estimated Time of Arrival: December 31
50 mg USD 2750 In-stock
Estimated Time of Arrival: December 31
100 mg USD 3950 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Other Forms of GSK 4027:

  • Biological Activity

  • Technical Information

  • Purity & Documentation

  • References

Description

GSK 4027 is a chemical probe for the PCAF/GCN5 bromodomain with an pIC50 of 7.4±0.11 for PCAF in a time-resolved fluorescence resonance energy transfer (TR-FRET) assay.

IC50 & Target

pIC50: 7.4±0.11 (PCAF)[1]

In Vitro

GSK 4027 is a PCAF/GCN5 bromodomain chemical probe. p300/CREB binding protein associated factor (PCAF/KAT2B) and general control nonderepressible 5 (GCN5/KAT2A) are multidomain proteins that have been implicated in retroviral infection, inflammation pathways, and cancer development. GSK 4027 also demonstrates potency toward BRD4 BD1 and BRD9 inTR-FRET assay with pIC50s of <4.3 and 5.1±0.08, respectively. The selectivity of GSK 4027 against the wider bromodomain family is assessed in the BROMOscan panel with pKi of 8.9 and 8.9 for PCAF and GCN5, respectively. GSK 4027 shows equipotent activity against PCAF and GCN5 with Ki of 1.4 nM for both bromodomains. As expected due to the encouraging measured artificial membrane permeability (500 nm/s), treatment of HEK293 cells with GSK 4027 displace full length PCAF from histone H3.3 with little drop-off from the biochemical assay and a pIC50 7.2 (IC50 60 nM)[1].

Solvent & Solubility
In Vitro: 

10 mM in DMSO

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6506 mL 13.2528 mL 26.5055 mL
5 mM 0.5301 mL 2.6506 mL 5.3011 mL
10 mM 0.2651 mL 1.3253 mL 2.6506 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Molecular Weight

377.28

Formula

C₁₇H₂₁BrN₄O

CAS No.

2079896-25-4

SMILES

BrC1=C(N[[email protected]@H]2C[[email protected]](C3=CC=CC=C3)CN(C)C2)C=NN(C)C1=O

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 4027
Cat. No.:
HY-101027
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GSK 4027

Cat. No.: HY-101027