GSK8814
Based on 1 publication(s) in Google Scholar
GSK8814 is a potent and selective ATAD2 bromodomain chemical probe and inhibitor (IC50 = 0.059 μM), with a binding constant pKd = 8.1 and a pKi = 8.9 in BROMOscan. GSK8814 binds to ATAD2 and BRD4 BD1 with pIC50s of 7.3 and 4.6, respectively. GSK8814 shows 500-fold selectivity for ATAD2 over BRD4 BD1. GSK8814 can be researched for cancer associated with ATAD2 bromodomain.
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- Purity: 99.80%
- CAS No.: 1997369-78-4
- 화학식: C28H35F2N5O3
- 분자량:527.61
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보관:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) GSK8814
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Biological Activity
제품 설명
IC50 & Target
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ATAD2 8.9 (pKi) |
ATAD2 8 nM (Ki) |
BRD4 BD1 4.6 (pIC50) |
In Vitro
GSK8814 (Compound 16) (10 nM-1 μM) results in dose-dependent displacement[1].
GSK8814 (20 μM) has effects on colony formation and inhibits genes involved in cell cycle and division at high compound concentrations in LNCaP cells (IC50 = 2.7 μM)[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. 1997369-78-4
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Appearance Solid
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분자량 527.61
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화학식 C28H35F2N5O3
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Color Light yellow to yellow
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SMILES
O=C1NC2=C(N[C@H]3[C@H](OCC4CCC(F)(F)CC4)CNC[C@@H]3OC)N=CC(C5=CC(C)=CN=C5)=C2C=C1C
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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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
In Vitro:
DMSO : 100 mg/mL (189.53 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
순도&문서
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Data Sheet (276 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
[1]. Bamborough P, et al. A Chemical Probe for the ATAD2 Bromodomain. Angew Chem Int Ed Engl. 2016 Sep 12;55(38):11382-6. [Content Brief]
[2]. Bamborough P, et al. Aiming to Miss a Moving Target: Bromo and Extra Terminal Domain (BET) Selectivity in Constrained ATAD2 Inhibitors. J Med Chem. 2018 Sep 27;61(18):8321-8336. [Content Brief]
[3]. Yao, D., et al., (2023). Fragment-based design, synthesis and biological evaluation of theophylline derivatives as ATAD2 inhibitors in BT-549 cells. Journal of enzyme inhibition and medicinal chemistry, 38(1), 2242601. [Content Brief]
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.8953 mL | 9.4767 mL | 18.9534 mL | 47.3835 mL |
| 5 mM | 0.3791 mL | 1.8953 mL | 3.7907 mL | 9.4767 mL | |
| 10 mM | 0.1895 mL | 0.9477 mL | 1.8953 mL | 4.7383 mL | |
| 15 mM | 0.1264 mL | 0.6318 mL | 1.2636 mL | 3.1589 mL | |
| 20 mM | 0.0948 mL | 0.4738 mL | 0.9477 mL | 2.3692 mL | |
| 25 mM | 0.0758 mL | 0.3791 mL | 0.7581 mL | 1.8953 mL | |
| 30 mM | 0.0632 mL | 0.3159 mL | 0.6318 mL | 1.5794 mL | |
| 40 mM | 0.0474 mL | 0.2369 mL | 0.4738 mL | 1.1846 mL | |
| 50 mM | 0.0379 mL | 0.1895 mL | 0.3791 mL | 0.9477 mL | |
| 60 mM | 0.0316 mL | 0.1579 mL | 0.3159 mL | 0.7897 mL | |
| 80 mM | 0.0237 mL | 0.1185 mL | 0.2369 mL | 0.5923 mL | |
| 100 mM | 0.0190 mL | 0.0948 mL | 0.1895 mL | 0.4738 mL |
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