GSK 4027
Based on 2 publication(s) in Google Scholar
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.
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- Purity: 98.22%
- CAS No.: 2079896-25-4
- 화학식: C17H21BrN4O
- 분자량:377.28
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biological Activity
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Chemical Information
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- References
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Publications Citing Use of MedChemExpress (MCE) GSK 4027
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Biological Activity
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GCN5/PCAF |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
60 nM
Compound: (R,R)-32; GSK4027
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Displacement of Halo-tagged histone H3.3 from NanoLuc-tagged full length human PCAF bromodomain expressed in HEK293 cells after 18 hrs by NanoBRET assay
Displacement of Halo-tagged histone H3.3 from NanoLuc-tagged full length human PCAF bromodomain expressed in HEK293 cells after 18 hrs by NanoBRET assay
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[PMID: 28002667] |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 2079896-25-4
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Appearance Solid
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분자량 377.28
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화학식 C17H21BrN4O
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Color Light yellow to yellow
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SMILES
BrC1=C(N[C@@H]2C[C@H](C3=CC=CC=C3)CN(C)C2)C=NN(C)C1=O
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (2)
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Journal Impact Factor
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Most Recent
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Nat Commun
Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. [Abstract]2026 Feb 12;17(1):1214. PMID: 41680175 -
용액&용해도
DMSO : 50 mg/mL (132.53 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
순도&문서
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Data Sheet (273 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
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- Español - ES (251 KB)
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- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.6506 mL | 13.2528 mL | 26.5055 mL | 66.2638 mL |
| 5 mM | 0.5301 mL | 2.6506 mL | 5.3011 mL | 13.2528 mL | |
| 10 mM | 0.2651 mL | 1.3253 mL | 2.6506 mL | 6.6264 mL | |
| 15 mM | 0.1767 mL | 0.8835 mL | 1.7670 mL | 4.4176 mL | |
| 20 mM | 0.1325 mL | 0.6626 mL | 1.3253 mL | 3.3132 mL | |
| 25 mM | 0.1060 mL | 0.5301 mL | 1.0602 mL | 2.6506 mL | |
| 30 mM | 0.0884 mL | 0.4418 mL | 0.8835 mL | 2.2088 mL | |
| 40 mM | 0.0663 mL | 0.3313 mL | 0.6626 mL | 1.6566 mL | |
| 50 mM | 0.0530 mL | 0.2651 mL | 0.5301 mL | 1.3253 mL | |
| 60 mM | 0.0442 mL | 0.2209 mL | 0.4418 mL | 1.1044 mL | |
| 80 mM | 0.0331 mL | 0.1657 mL | 0.3313 mL | 0.8283 mL | |
| 100 mM | 0.0265 mL | 0.1325 mL | 0.2651 mL | 0.6626 mL |
GSK 4027 Related Classifications
HY-101027 Related Classifications
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