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BOC Sciences
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16314854226 |
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Product Name:GSK4027 CAS:2079896-25-4 Purity:95% Package:1G;10G;100G Remarks:GSK4027 is a potent and selective inhibitor of p300/CBP-associated factor (PCAF)/general control nonderepressible 5 (GCN5) bromodomain (Ki = 1.4 nM; IC50 = 60 nM in a chromatin engagement assay).
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ChemeGen(Shanghai) Biotechnology Co.,Ltd.
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18818260767 |
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sales@chemegen.com |
Products Intro: |
Product Name:GSK 4027 CAS:2079896-25-4 Purity:98% Package:10 mg;50 mg;100 mg;500 mg;1 g;5 g;10 g
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| GSK4027 Basic information |
Product Name: | GSK4027 | Synonyms: | GSK4027;GSK4207;3(2H)-Pyridazinone, 4-bromo-2-methyl-5-[[(3R,5R)-1-methyl-5-phenyl-3-piperidinyl]amino]- | CAS: | 2079896-25-4 | MF: | C17H21BrN4O | MW: | 377.28 | EINECS: | | Product Categories: | | Mol File: | 2079896-25-4.mol | ![GSK4027 Structure](CAS/20200515/GIF/2079896-25-4.gif) |
| GSK4027 Chemical Properties |
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) |
| GSK4027 Usage And Synthesis |
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_
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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 |
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