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
- Molecular Weight:
- 377.28
- MDL Number:
- MFCD31692324
- MOL File:
- 2079896-25-4.mol
GSK4027 price More Price(10)
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| Cayman Chemical | 23421 | GSK4027 | 2079896-25-4 | 1mg | $44 | 2024-03-01 | Buy |
| Cayman Chemical | 23421 | GSK4027 | 2079896-25-4 | 10mg | $257 | 2024-03-01 | Buy |
| Cayman Chemical | 23421 | GSK4027 | 2079896-25-4 | 5mg | $140 | 2024-03-01 | Buy |
| AK Scientific | 3339EJ | 4-Bromo-2-methyl-5-[[(3R,5R)-1-methyl-5-phenylpiperidin-3-yl]amino]pyridazin-3-one | 2079896-25-4 | 5mg | $253 | 2021-12-16 | Buy |
| Biosynth Carbosynth | BG166671 | GSK 4027 | 2079896-25-4 | 10mg | $285 | 2021-12-16 | Buy |
GSK4027 Chemical Properties,Uses,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
GSK4027 Suppliers
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| TargetMol Chemicals Inc. | +1-781-999-5354 +1-00000000000 | marketing@targetmol.com | United States | 19892 | 58 |
| Aladdin Scientific | +1-+1(833)-552-7181 | sales@aladdinsci.com | United States | 52927 | 58 |
| BOC Sciences | 16314854226 | info@bocsci.com | United States | 9926 | 65 |
| Hangzhou Synstar pharmaceutical Technology CO.,Ltd | 0571-85361029 | synstar518@163.com | China | 1991 | 58 |
| ChemeGen(Shanghai) Biotechnology Co.,Ltd. | 18818260767 | sales@chemegen.com | China | 11289 | 58 |
| Shanghai hongqu biomedical technology co. LTD | 88888888888 | hongquchem@qq.com | China | 5132 | 58 |
| Kaifeng Mingren Pharmaceutical Co.,LTD | 0371-65741762 | sales@hasunny.com | China | 2380 | 58 |
| Shanghai Yifei Biotechnology Co. , Ltd. | 021-65675885 18964387627 | customer_service@efebio.com | China | 8740 | 58 |
| RD International Technology Co., Limited | 18024082417 | market@ubiochem.com | China | 9155 | 58 |
| TargetMol Chemicals Inc. | 15002134094 | marketing@targetmol.cn | China | 28118 | 58 |