GSK2981278
Based on 4 publication(s) in Google Scholar
GSK2981278 is a potent and selective RORγ inverse agonist. GSK2981278 inhibits activation of the il17 promoter and interferes RORγ-DNA binding.
For research use only. We do not sell to patients.
- Purity: 99.51%
- CAS No.: 1474110-21-8
- Formula: C25H35NO5S
- Molecular Weight:461.61
-
Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
-
Solvent & Solubility
- Purity & Documentation
- References
-
Help & FAQs
-
Immunology/Inflammation Compound Library
HY-L007
-
Metabolism/Protease Compound Library
HY-L012
-
Clinical Compound Library
HY-L026
-
Small Molecule Immuno-Oncology Compound Library
HY-L031
-
Drug Repurposing Compound Library
HY-L035
-
Transcription Factor-Targeted Library
HY-L090
-
Nuclear Receptor Compound Library
HY-L126
-
Heterocyclic Compound Library
HY-L138
-
Metabolic Enzyme Compound Library
HY-L146
-
Highly Selective Inhibitors Library
HY-L158
-
Bioactive Compound Library Max
HY-L181
-
MCE Bioactive Compound Library
HY-L001V
-
Drug Repurposing Compound Library Plus
HY-L035P
-
Clinical Compound Library Plus
HY-L026P
-
Bioactive Compound Library
HY-L001
-
Protein Kinase Compound Library
HY-L196
-
High-Throughput Bioactive Compound Library
HY-L205
Publications Citing Use of MedChemExpress (MCE) GSK2981278
More
Biological Activity
RORγ[1]
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| PBMC | IC50 |
20 nM
Compound: 14; GSK-2981278
|
Inhibition of SRC1 coactivator recruitment in human PBMC
Inhibition of SRC1 coactivator recruitment in human PBMC
|
[PMID: 30010338] |
| PBMC | IC50 |
63 nM
Compound: 14; GSK-2981278
|
Inhibition of IL-17 production in human PBMC
Inhibition of IL-17 production in human PBMC
|
[PMID: 30010338] |
GSK2981278 markedly and potently inhibits IL-17A and IL-22 protein secretion in a concentration dependent manner (IC50 = 3.2 nM) during 5 days of culture under Th17 skewing conditions[1].
GSK2981278 (0.3, 1, 3, 10, 30, 100, 300, 1000 pM; 5 day) potently and selectively inhibits IL-17 and IL-22 levels. Culture in the presence of ≥3 nM GSK2981278 led to a near-complete inhibition of IL-17A protein secretion[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:BALB/c JByRj Female Mice (8 week-old at study initiation; imiquimod (IMQ) mouse model) [1]
-
Dosage:1%
-
Administration:In ointment; topically; for three days
-
Result:Reduced skin redness and scaling, as well as decreased hyperplasia, as evidenced by a 23% reduction in epidermal thickness.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
-
CAS No. 1474110-21-8
-
Appearance Solid
-
Molecular Weight 461.61
-
Formula C25H35NO5S
-
Color White to off-white
-
SMILES
CC(C)CN(S(=O)(C1=CC=C(OCC2CCOCC2)C(CO)=C1)=O)C3=CC=C(CC)C=C3
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (4)
-
Journal Impact Factor
-
Most Recent
-
Sci Adv
Gut microbiota from patients with arteriosclerotic CSVD induces higher IL-17A production in neutrophils via activating RORγt. [Abstract]2021 Jan 22;7(4):eabe4827. PMID: 33523954 -
Brain Behav Immun
Double negative T cells promote surgery-induced neuroinflammation, microglial engulfment and cognitive dysfunction via the IL-17/CEBPβ/C3 pathway in adult mice. [Abstract]2025 Jan:123:965-981. PMID: 39491565 -
Antioxidants (Basel)
Melatonin Nuclear Receptors Mediate Green-and-Blue-Monochromatic-Light-Combinations-Inhibited B Lymphocyte Apoptosis in the Bursa of Chickens via Reducing Oxidative Stress and Nfκb Expression. [Abstract]2022 Apr 8;11(4):748. PMID: 35453433 -
Poultry Sci
Melatonin mediates monochromatic light-induced proliferation of T/B lymphocytes in the spleen via the membrane receptor or nuclear receptor. [Abstract]2020 Sep;99(9):4294-4302. PMID: 32867973
Solvent & Solubility
DMSO : ≥ 100 mg/mL (216.63 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)
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 (5.42 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.42 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 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:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%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.
Purity & Documentation
-
Data Sheet (280 KB)
-
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
-
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 | 2.1663 mL | 10.8317 mL | 21.6633 mL | 54.1583 mL |
| 5 mM | 0.4333 mL | 2.1663 mL | 4.3327 mL | 10.8317 mL | |
| 10 mM | 0.2166 mL | 1.0832 mL | 2.1663 mL | 5.4158 mL | |
| 15 mM | 0.1444 mL | 0.7221 mL | 1.4442 mL | 3.6106 mL | |
| 20 mM | 0.1083 mL | 0.5416 mL | 1.0832 mL | 2.7079 mL | |
| 25 mM | 0.0867 mL | 0.4333 mL | 0.8665 mL | 2.1663 mL | |
| 30 mM | 0.0722 mL | 0.3611 mL | 0.7221 mL | 1.8053 mL | |
| 40 mM | 0.0542 mL | 0.2708 mL | 0.5416 mL | 1.3540 mL | |
| 50 mM | 0.0433 mL | 0.2166 mL | 0.4333 mL | 1.0832 mL | |
| 60 mM | 0.0361 mL | 0.1805 mL | 0.3611 mL | 0.9026 mL | |
| 80 mM | 0.0271 mL | 0.1354 mL | 0.2708 mL | 0.6770 mL | |
| 100 mM | 0.0217 mL | 0.1083 mL | 0.2166 mL | 0.5416 mL |
GSK2981278 Related Classifications
HY-19770 Related Classifications
Powered by Bioz