GSK4027
- Product Name
- GSK4027
- CAS No.
- 2079896-25-4
- Chemical Name
- GSK4027
- Synonyms
- GSK4207;GSK4027;3(2H)-Pyridazinone, 4-bromo-2-methyl-5-[[(3R,5R)-1-methyl-5-phenyl-3-piperidinyl]amino]-
- CBNumber
- CB93339890
- Molecular Formula
- C17H21BrN4O
- Formula Weight
- 377.28
- MOL File
- 2079896-25-4.mol
GSK4027 Property
- Boiling point:
- 450.3±55.0 °C(Predicted)
- Density
- 1.45±0.1 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- DMSO:50.0(Max Conc. mg/mL);132.53(Max Conc. mM)
- form
- A crystalline solid
- pka
- 9.58±0.10(Predicted)
N-Bromosuccinimide Price
- Product number
- 23421
- Product name
- GSK4027
- Packaging
- 1mg
- Price
- $44
- Updated
- 2024/03/01
- Product number
- 23421
- Product name
- GSK4027
- Packaging
- 10mg
- Price
- $257
- Updated
- 2024/03/01
- Product number
- 23421
- Product name
- GSK4027
- Packaging
- 5mg
- Price
- $140
- Updated
- 2024/03/01
- Product number
- 3339EJ
- Product name
- 4-Bromo-2-methyl-5-[[(3R,5R)-1-methyl-5-phenylpiperidin-3-yl]amino]pyridazin-3-one
- Packaging
- 5mg
- Price
- $253
- Updated
- 2021/12/16
- Product number
- BG166671
- Product name
- GSK 4027
- Packaging
- 10mg
- Price
- $285
- Updated
- 2021/12/16
GSK4027 Chemical Properties,Usage,Production
Description
GSK4027 is a potent and selective chemical probe for the PCAF/GCN5 bromodomain. GSK4027 has PCAF TR-FRET pIC50 = 7.4 ; PCAF BROMOscan pKi = 8.9; GCN5 BROMOscan pKi = 8.9; PCAF NanoBRET pIC50 =7.2; BRD4 BD1 TR-FRET pIC50 < 4.3. GSK4027 shows high potency for the PCAF/GCN5 bromodomain, high solubility, cellular target engagement, and ≥18000-fold selectivity over the BET family, together with ≥70-fold selectivity over the wider bromodomain families. 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.
in vitro
Herein, this study reports GSK4027 as a chemical probe for the PCAF/GCN5 bromodomain, together with GSK4028 as an enantiomeric negative control._x000D_ _x000D_ Reference: J Med Chem. 2017 Jan 26;60(2):695-709. https://pubmed.ncbi.nlm.nih.gov/28002667/
target
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.
GSK4027 Preparation Products And Raw materials
Raw materials
Preparation Products
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