| Size | Price | Stock | Qty |
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| 1mg |
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| Other Sizes |
| Targets |
(S)-GSK852 is a diastereomer of GSK852, which is a highly potent and selective inhibitor of the second bromodomain (BD2) of BET (Bromo and Extra-Terminal domain) family proteins. BET proteins (BRD2, BRD3, BRD4, BRDT) are epigenetic readers that regulate gene expression. By inhibiting BD2, (S)-GSK852 can modulate the transcription of genes involved in inflammation and cancer.
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| ln Vitro |
No specific in vitro activity data was found for (S)-GSK852. The parent compound, GSK852, is a BET inhibitor targeting the second bromodomain (BD2), with a pIC50 of 7.9. The (S)-diastereomer likely has different or reduced activity compared to GSK852. It is likely used as a negative control to determine the stereospecificity of the biological effects observed with GSK852.
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| ln Vivo |
No specific in vivo data was found for (S)-GSK852. GSK852 is a selective BD2 inhibitor with a pIC50 of 7.9, and such inhibitors have shown efficacy in models of inflammatory diseases. The (S)-diastereomer might be used as a tool compound to determine if the in vivo effects of GSK852 are stereospecific or due to off-target effects. By comparing the two, researchers can draw more definitive conclusions about BD2 target engagement.
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| Enzyme Assay |
Standard BRD4 BD2 binding assay: Recombinant BRD4 BD2 protein is incubated with a fluorescently labeled BET ligand. The test compound, (S)-GSK852, is added at a range of concentrations. The binding interaction is measured by a fluorescence polarization (FP) or time-resolved fluorescence resonance energy transfer (TR-FRET) assay. This allows for the determination of the IC50 or Ki for the diastereomer at the BD2 domain. This value can then be compared to that of the potent GSK852.
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| Cell Assay |
Standard cell-based assay for BET inhibition: A luciferase reporter cell line containing a NF-kappaB or c-Myc response element can be used. Cells are plated and treated with (S)-GSK852 and GSK852. After 4-6 hours, the luciferase signal, which correlates with transcriptional activity, is measured. The ability of the test compounds to suppress the reporter signal is compared to confirm the target-specific activity of the active enantiomer.
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| Animal Protocol |
No specific animal protocol was found. To study the stereospecificity of a BET BD2 inhibitor in a mouse model of acute inflammation, (S)-GSK852 and GSK852 would be administered to mice following an LPS challenge. For example, 8-10 week old C57BL/6 mice would be administered an oral dose (e.g., 30 mg/kg) of the test compound or vehicle. After 1 hour, the mice would be injected with LPS (e.g., 10 mg/kg). Plasma levels of TNF-alpha would be measured 1.5 hours after LPS injection. The active diastereomer would suppress TNF-alpha, whereas (S)-GSK852 would not.
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| ADME/Pharmacokinetics |
No specific PK data was found. As a diastereomer of a potent BET inhibitor, (S)-GSK852 is expected to have a similar PK profile to the active parent compound. It is a small molecule with a favorable molecular weight (406.47 Da) for oral absorption. The compound would be expected to be metabolized by the liver and have a short to moderate half-life.
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| Toxicity/Toxicokinetics |
No specific toxicity data was found. As a selective BET BD2 inhibitor, its toxicity is expected to be lower than that of first-generation BET inhibitors, which caused significant thrombocytopenia and gastrointestinal issues. By selectively targeting BD2, the toxicities related to BD1 inhibition are avoided. However, the safety profile of the (S)-diastereomer is not known.
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| References | |
| Additional Infomation |
(S)-GSK852 (CAS: 2305919-51-9) has a molecular formula of C24H26N2O4 and a molecular weight of 406.47. It is a diastereomer of GSK852, which is a BET inhibitor that targets BD2 with a pIC50 of 7.9. This product is for research use only.
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| Molecular Formula |
C24H26N2O4
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| Molecular Weight |
406.47
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| CAS # |
2305919-51-9
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| Related CAS # |
GSK852;2305842-30-0
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| Appearance |
White to off-white solid powder
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~246.02 mM; with ultrasonication)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4602 mL | 12.3010 mL | 24.6021 mL | |
| 5 mM | 0.4920 mL | 2.4602 mL | 4.9204 mL | |
| 10 mM | 0.2460 mL | 1.2301 mL | 2.4602 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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