| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
GS-87 targets glycogen synthase kinase 3 (GSK3), specifically the GSK3α and GSK3β isoforms. It has IC50 values of 415 nM for GSK3α and 521 nM for GSK3β. By inhibiting GSK3, GS-87 activates downstream signaling pathways, including MAPK signaling, which leads to the differentiation of AML cells. It modulates key GSK3 target proteins involved in cell proliferation and differentiation.
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| ln Vitro |
In vitro, GS-87 is a highly specific and potent GSK3 inhibitor. It inhibits GSK3α with an IC50 of 415 nM and GSK3β with an IC50 of 521 nM. The compound induces differentiation of acute myeloid leukemia (AML) cell lines. It is more effective at modulating key GSK3 target proteins than Lithium and SB415285.
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| ln Vivo |
In vivo, GS-87 has the potential to act as a differentiation agent for non-promyelocytic AML research. As an inhibitor of GSK3, it is expected to modulate key signaling pathways involved in cell proliferation and differentiation. However, specific in vivo efficacy data and detailed animal study results are not extensively reported in the available literature.
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| Enzyme Assay |
In vitro enzyme assays for GS-87 typically involve kinase activity assays using purified recombinant GSK3α and GSK3β enzymes. The compound is incubated with the enzyme, ATP, and a specific peptide substrate. The phosphorylation of the substrate is measured using techniques such as radioactive (33P-ATP) or luminescence-based detection methods. IC50 values are determined from dose-response curves.
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| Cell Assay |
In vitro cellular assays for GS-87 are performed using acute myeloid leukemia (AML) cell lines. Cells are cultured in appropriate media and treated with various concentrations of the compound. Cell differentiation is assessed by measuring the expression of differentiation markers (e.g., CD11b, CD14) using flow cytometry. Cell proliferation and viability are also assessed using standard assays like MTT or CellTiter-Glo.
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| Animal Protocol |
In vivo animal studies with GS-87 would typically be conducted in mouse models of AML to evaluate its efficacy as a differentiation agent. The compound would be administered orally or intraperitoneally, and its effects on tumor growth, differentiation of leukemic cells, and overall survival would be assessed. However, specific protocols are not detailed in the available literature.
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| ADME/Pharmacokinetics |
The pharmacokinetic properties of GS-87 are not extensively reported. It has a molecular weight of 337.36. Its solubility in DMSO and other properties are not detailed in the available literature. Specific parameters such as oral bioavailability, half-life, and tissue distribution are not available.
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| Toxicity/Toxicokinetics |
The toxicity profile of GS-87 is not extensively reported in the available literature. As a research compound, it is for research use only and not for human therapeutic use. Standard toxicity studies would be required to assess its safety for potential therapeutic applications. No specific toxicity data are detailed.
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| References | |
| Additional Infomation |
GS-87 (GS87) is a highly specific and potent GSK3 inhibitor with IC50s of 415 nM (GSK3α) and 521 nM (GSK3β). It induces differentiation of AML cell lines by activating GSK3-dependent MAPK signaling. The compound has potential as a differentiation agent for non-promyelocytic AML research. It is available for research purposes only.
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| Molecular Formula |
C16H11N5O2S
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|---|---|
| Molecular Weight |
337.355840921402
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| Exact Mass |
337.063
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| CAS # |
919936-70-2
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| PubChem CID |
17408143
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.47±0.1 g/cm3 (20 °C, 760 mmHg)
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| Boiling Point |
572.5±60.0 °C (760 mmHg)
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| LogP |
3.473
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
24
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| Complexity |
393
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| Defined Atom Stereocenter Count |
0
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| SMILES |
N1=C(SCC2ON=C(C3C=CC=CC=3)N=2)OC(C2C=CN=CC=2)=N1
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| InChi Key |
HNTUWEZDVRVSFY-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C16H11N5O2S/c1-2-4-11(5-3-1)14-18-13(23-21-14)10-24-16-20-19-15(22-16)12-6-8-17-9-7-12/h1-9H,10H2
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| Chemical Name |
2-[(3-phenyl-1,2,4-oxadiazol-5-yl)methylsulfanyl]-5-pyridin-4-yl-1,3,4-oxadiazole
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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 | 2.9642 mL | 14.8210 mL | 29.6419 mL | |
| 5 mM | 0.5928 mL | 2.9642 mL | 5.9284 mL | |
| 10 mM | 0.2964 mL | 1.4821 mL | 2.9642 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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