GSK778
Based on 2 publication(s) in Google Scholar
GSK778 (iBET-BD1), a chemical probe, is a potent and selective BD1 bromodomain inhibitor of the BET proteins, with IC50s of 75 nM (BRD2 BD1), 41 nM (BRD3 BD1), 41 nM (BRD4 BD1), and 143 nM (BRDT BD1), respectively. GSK778 phenocopies the effects of pan-BET inhibitors in cancer models.
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- Purity: 99.14%
- CAS No.: 2451862-42-1
- 화학식: C30H33N5O3
- 분자량:511.61
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months
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) GSK778
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Biological Activity
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BRD2 BD1 75 nM (IC50) |
BRD3 BD1 41 nM (IC50) |
BRD4 BD1 41 nM (IC50) |
BRDT BD1 143 nM (IC50) |
GSK778 inhibits BRD BD2 with the IC50s of 3950 nM (BRD2 BD2), 1210 nM (BRD3 BD2), 5843 nM (BRD4 BD2), and 17451 nM (BRDT BD2), respectively[1].
GSK778 (0.01-10 μM; 72 hours) inhibits the proliferative activity of human primary CD4+ T cells and the production of effector cytokines including IFNγ, IL-17A and IL-22[1].
GSK778 (0.001-10 μM; 5 days) has a more pronounced effect on the growth and viability of MDA-453, MOLM-13, K562, MV4-11, THP-1, and MDA-MB-231 cells[1].
GSK778 (1000 nM; 72 hours) inhibits proliferation, induces a cell cycle arrest and apoptosis in MV4-11, MOLM13, MDA-MB-231 and MB453 cells[1].
GSK778 (1000 nM; 12 days) reduces the clonogenic capacity of primary human AML cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Human primary CD4+ T cell
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Concentration:0.001, 0.01, 0.1, 1, 10 μM
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Incubation Time:72 hours
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Result:Inhibited the proliferative activity of the cells and the production of effector cytokines.
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Cell Line:MDA-453, MOLM-13, K562, MV4-11, THP-1, and MDA-MB-231 cells
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Concentration:0.001, 0.01, 0.1, 1, 10 μM
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Incubation Time:5 days
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Result:Inhibited the growth and viability of human cancer cell lines.
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Cell Line:MV4-11, MOLM13, MDA-MB-231 and MB453 cells
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Concentration:1000 nM
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Incubation Time:72 hours
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Result:Inhibited cell proliferation and induced a cell cycle arrest and apoptosis.
GSK778 (15 mg/kg/BID; s.c. for 14 days) reduces the production of anti-keyhole limpet hemocyanin (KLH) IgM and is well tolerated[1].
GSK778 exhibits Cmax (85 ng/mL), Tmax (1.48 h) and AUC∞ (132 ng.h/mL) following oral administration (10 mg/kg) in mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:6-8 weeks female C57BL/6 mice are injected with MLL-AF9 cells[1]
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Dosage:15 mg/kg/BID
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Administration:I.p. injections for 30 days
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Result:Increased the survival rate of leukemia mice.
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Animal Model:Male CD1 mice[1]
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Dosage:10 mg/kg (Pharmacokinetic Analysis)
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Administration:P.o. administration
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Result:Cmax (85 ng/mL), Tmax (1.48 h); AUC∞ (132 ng.h/mL).
Chemical Information
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CAS No. 2451862-42-1
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Appearance Solid
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분자량 511.61
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화학식 C30H33N5O3
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Color White to light yellow
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SMILES
CC1=NOC(C)=C1C2=C(OC[C@@H]3CNCC3)C=C4C5=C(N=C(COC)N5[C@H](C)C6=CC=CC=C6)C=NC4=C2
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Synonyms
iBET-BD1
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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 1 year -20°C 6 months
Publications (2)
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Journal Impact Factor
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Most Recent
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ACS Nano
Nanopore Discrimination of Protein-Small-Molecule Drug Complexes at Near-Atomic Resolution. [Abstract]2026 May 12;20(18):13624-13635. PMID: 42046448 -
J Pharm Biomed Anal
An online rapid screening HPLC system establishing and applying discovered a new type of natural chemical ligand of the BRD4-BD1 from Hedyotis diffusa. [Abstract]2026 Apr 15:271:117336. PMID: 41512411
용액&용해도
DMSO : 41.67 mg/mL (81.45 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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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: ≥ 2.08 mg/mL (4.07 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.08 mg/mL (4.07 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.
순도&문서
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Data Sheet (288 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 1.9546 mL | 9.7731 mL | 19.5461 mL | 48.8653 mL |
| 5 mM | 0.3909 mL | 1.9546 mL | 3.9092 mL | 9.7731 mL | |
| 10 mM | 0.1955 mL | 0.9773 mL | 1.9546 mL | 4.8865 mL | |
| 15 mM | 0.1303 mL | 0.6515 mL | 1.3031 mL | 3.2577 mL | |
| 20 mM | 0.0977 mL | 0.4887 mL | 0.9773 mL | 2.4433 mL | |
| 25 mM | 0.0782 mL | 0.3909 mL | 0.7818 mL | 1.9546 mL | |
| 30 mM | 0.0652 mL | 0.3258 mL | 0.6515 mL | 1.6288 mL | |
| 40 mM | 0.0489 mL | 0.2443 mL | 0.4887 mL | 1.2216 mL | |
| 50 mM | 0.0391 mL | 0.1955 mL | 0.3909 mL | 0.9773 mL | |
| 60 mM | 0.0326 mL | 0.1629 mL | 0.3258 mL | 0.8144 mL | |
| 80 mM | 0.0244 mL | 0.1222 mL | 0.2443 mL | 0.6108 mL |
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