[CAS NO. 2079896-25-4] GSK 4027
PRODUCTS SPECIFICATIONS [2079896-25-4]
DESCRIPTION [2079896-25-4]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 377.28 |
| Molecular Formula | C17H21BrN4O |
| SMILES | BrC1=C(N[C@@H]2C[C@H](C3=CC=CC=C3)CN(C)C2)C=NN(C)C1=O |
Summary
GSK 4027 is a chemical probe for the PCAF / GCN5 bromodomain with an pIC 50 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 pIC 50 s 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 pK i of 8.9 and 8.9 for PCAF and GCN5, respectively. GSK 4027 shows equipotent activity against PCAF and GCN5 with K i 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 pIC 50 7.2 (IC 50 60 nM) [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
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
DMSO : 50 mg/mL ( 132.53 mM ; Need ultrasonic)
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 |
