| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| Other Sizes |
| Targets |
IC50: 0.32 μM (glutathione S-transferase, GST)[1]
Glutathione S‑transferase (GST) is a detoxification enzyme that binds glutathione (GSH). The GST‑FH class of compounds, including GST‑FH.1, generates false‑positive signals (frequent hitters, FH) in GST‑based binding assays due to non‑specific interactions with the enzyme‑substrate pair. The compound does not target a specific receptor but rather interferes with the GST‑GSH interaction, making it a tool for assay validation. |
|---|---|
| ln Vitro |
In vitro, GST-FH.1 is a GST‑FH compound that causes frequent false‑positive hits in assays measuring the GST‑GSH interaction. No specific IC₅0 value is reported for GST‑FH.1 itself in the search results; however, the related compound GST‑FH.4 inhibits GST with an IC₅0 of 0.32 microM. No cellular activity data are reported, as the compound is used in cell‑free biochemical systems.
|
| ln Vivo |
No in vivo activity data for GST-FH.1 are reported. The compound is not intended for use in animal models. It serves exclusively as an in vitro research tool for studying false‑positive interactions in GST‑based screening assays and has no therapeutic applications.
|
| Enzyme Assay |
No direct enzyme/receptor binding assays are applicable. GST‑FH.1 is used as a control to generate false‑positive signals. For interaction studies, GST is immobilized on a solid support (e.g., glutathione‑Sepharose beads), and the compound is incubated with the beads in the presence of GSH. The amount of compound bound is detected by absorbance or fluorescence to assess non‑specific binding. No specific IC₅0 is reported.
|
| Cell Assay |
GST-FH.1 is not evaluated in cellular assays. Its use is limited to cell‑free GST pull‑down or enzymatic assays. For validation purposes, the compound can be added to lysates containing GST‑tagged proteins to assess non‑specific binding, but no specific protocols are described.
|
| Animal Protocol |
GST-FH.1 is not used in animal experiments. The compound is a research reagent for in vitro biochemical studies only. No in vivo animal protocols are described.
|
| ADME/Pharmacokinetics |
GST-FH.1 (C1₅H13N3O3S, MW = 315.35, purity ≥90% by HPLC) is a solid powder. For storage, the powder should be kept at -20degC for up to 3 years, sealed, and protected from light. For in vitro use, stock solutions in DMSO (e.g., 20 mg/mL) can be stored at -80degC for up to 1 year. The compound is not formulated for in vivo use.
|
| Toxicity/Toxicokinetics |
No specific toxicity data for GST-FH.1 are reported. As a research‑grade compound, it is not intended for human or veterinary use. Standard laboratory safety precautions for handling chemicals should be followed. No LD₅0 or formal toxicology studies are available.
|
| References | |
| Additional Infomation |
GST-FH.1 is a research‑grade GST‑FH compound used to study false‑positive “frequent hitter” interactions in GST‑based assays. The GST‑FH class of compounds was described in the literature by Brenke et al. (J Biomol Screen, 2016). The compound is for research use only and has not entered clinical trials or received regulatory approval.
|
| Molecular Formula |
C15H13N3O3S
|
|---|---|
| Molecular Weight |
315.35
|
| Exact Mass |
315.068
|
| CAS # |
920115-54-4
|
| PubChem CID |
22433254
|
| Appearance |
Solid powder
|
| Hydrogen Bond Donor Count |
1
|
| Rotatable Bond Count |
2
|
| Heavy Atom Count |
22
|
| Complexity |
498
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
CN1C2=C(C=C(C=C2)NC(=O)C3=CC=CS3)N(C(=O)C1=O)C
|
| InChi Key |
SLDCODWMMHDLEV-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C15H13N3O3S/c1-17-10-6-5-9(16-13(19)12-4-3-7-22-12)8-11(10)18(2)15(21)14(17)20/h3-8H,1-2H3,(H,16,19)
|
| Chemical Name |
N-(1,4-dimethyl-2,3-dioxoquinoxalin-6-yl)thiophene-2-carboxamide
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| 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 | 3.1711 mL | 15.8554 mL | 31.7108 mL | |
| 5 mM | 0.6342 mL | 3.1711 mL | 6.3422 mL | |
| 10 mM | 0.3171 mL | 1.5855 mL | 3.1711 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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