| CAS NO: | 2079896-25-4 |
| 包装 | 价格(元) |
| 10mM (in 1mL DMSO) | 电议 |
| 5mg | 电议 |
| 10mg | 电议 |
| 25mg | 电议 |
| 50mg | 电议 |
| 100mg | 电议 |
| Cas No. | 2079896-25-4 |
| Canonical SMILES | BrC1=C(N[C@@H]2C[C@H](C3=CC=CC=C3)CN(C)C2)C=NN(C)C1=O |
| 分子式 | C17H21BrN4O |
| 分子量 | 377.28 |
| 溶解度 | DMSO : 50 mg/mL (132.53 mM) |
| 储存条件 | Store at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
| 产品描述 | 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. 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]. [1]. Humphreys PG, et al. Discovery of a Potent, Cell Penetrant, and Selective p300/CBP-Associated Factor (PCAF)/General Control Nonderepressible 5 (GCN5) Bromodomain Chemical Probe. J Med Chem. 2017 Jan 26;60(2):695-709. |
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