GSK1324726A
Based on 6 publication(s) in Google Scholar
GSK1324726A is a novel, potent, and selective inhibitor of BET proteins with high affinity to BRD2 (IC50=41 nM), BRD3 (IC50=31 nM), and BRD4 (IC50=22 nM).
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- Purity : 99.92%
- CAS No.: 1300031-52-0
- 화학식: C25H23ClN2O3
- 분자량:434.91
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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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용액&용해도
- Protocol
- 순도&문서
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) GSK1324726A
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Customer Validation & Images
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WB
Biological Activity
제품 설명
IC50 & Target
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BRD4 BD2 |
BRD4 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| LOUCY | EC50 |
0.7 μM
Compound: 4; GSK1324726A
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Cytotoxicity against human Loucy cells assessed as reduction in cell viability after 5 days by CellTiter-Glo assay
Cytotoxicity against human Loucy cells assessed as reduction in cell viability after 5 days by CellTiter-Glo assay
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[PMID: 29170024] |
In Vitro
A panel of neuroblastoma cell lines are treated with GSK1324726A (I-BET726), and observed potent growth inhibition and cytotoxicity in most cell lines irrespective of MYCN copy number or expression level. All neuroblastoma cell lines tested exhibit potent growth inhibition, with a median growth IC50 value (gIC50; inhibitor concentration resulting in 50% growth inhibition) equal to 75 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1300031-52-0
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Appearance Solid
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분자량 434.91
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화학식 C25H23ClN2O3
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Color White to light yellow
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SMILES
ClC1=CC=C(N[C@H]2C3=C(C=CC(C4=CC=C(C(O)=O)C=C4)=C3)N(C(C)=O)[C@@H](C)C2)C=C1
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Synonyms
I-BET726
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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 (6)
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Journal Impact Factor
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Most Recent
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Proc Natl Acad Sci U S A
2019 Feb 19;116(8):2961-2966. PMID: 30718431 -
J Med Chem
Impact of Target Warhead and Linkage Vector on Inducing Protein Degradation: Comparison of Bromodomain and Extra-Terminal (BET) Degraders Derived from Triazolodiazepine (JQ1) and Tetrahydroquinoline (I-BET726) BET Inhibitor Scaffolds. [Abstract]2018 Jan 25;61(2):504-513. PMID: 28595007
GSK1324726A purchased from MedChemExpress. Usage Cited in: J Med Chem. 2018 Jan 25;61(2):504-513. [Abstract]
Protein degradation profile of VHL-based BET degraders. Sub-confluent HeLa cells are treated for 24 h with varying concentration of test compounds JQ1(Compound 3), I-BET726 (Compound 4). Protein extracts are separated by SDS-PAGE and then analyzed by Western blot. Proteins Brd4, Brd3, Brd2 and β-actin are probed for JQ1and I-BET726 with specific antibodies.
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Bioorg Med Chem
Exploiting a water network to achieve enthalpy-driven, bromodomain-selective BET inhibitors. [Abstract]2018 Jan 1;26(1):25-36. PMID: 29170024 -
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용액&용해도
In Vitro:
DMSO : ≥ 46 mg/mL (105.77 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.75 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
순도&문서
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Data Sheet (281 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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Handling Instructions (2659 KB)
References
[1]. Wyce A, et al. BET inhibition silences expression of MYCN and BCL2 and induces cytotoxicity in neuroblastoma tumor models. PLoS One. 2013 Aug 23;8(8):e72967. [Content Brief]
[2]. Gosmini R, et al. The discovery of I-BET726 (GSK1324726A), a potent tetrahydroquinoline ApoA1 up-regulator and selective BET bromodomain inhibitor. J Med Chem. 2014 Oct 9;57(19):8111-31. [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, 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 |
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| DMSO | 1 mM | 2.2993 mL | 11.4966 mL | 22.9933 mL | 57.4832 mL |
| 5 mM | 0.4599 mL | 2.2993 mL | 4.5987 mL | 11.4966 mL | |
| 10 mM | 0.2299 mL | 1.1497 mL | 2.2993 mL | 5.7483 mL | |
| 15 mM | 0.1533 mL | 0.7664 mL | 1.5329 mL | 3.8322 mL | |
| 20 mM | 0.1150 mL | 0.5748 mL | 1.1497 mL | 2.8742 mL | |
| 25 mM | 0.0920 mL | 0.4599 mL | 0.9197 mL | 2.2993 mL | |
| 30 mM | 0.0766 mL | 0.3832 mL | 0.7664 mL | 1.9161 mL | |
| 40 mM | 0.0575 mL | 0.2874 mL | 0.5748 mL | 1.4371 mL | |
| 50 mM | 0.0460 mL | 0.2299 mL | 0.4599 mL | 1.1497 mL | |
| 60 mM | 0.0383 mL | 0.1916 mL | 0.3832 mL | 0.9581 mL | |
| 80 mM | 0.0287 mL | 0.1437 mL | 0.2874 mL | 0.7185 mL | |
| 100 mM | 0.0230 mL | 0.1150 mL | 0.2299 mL | 0.5748 mL |
GSK1324726A Related Classifications
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