| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg | |||
| Other Sizes |
| Targets |
Targets: GLUT4 (glucose transporter type 4, IC50=6.8 uM) and GLUT1 (IC50=11.4 uM). By inhibiting GLUT4, the compound disrupts insulin-stimulated glucose uptake into cells, impacting glucose homeostasis and potentially providing therapeutic benefits in cancer, insulin resistance, and type 2 diabetes.
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| ln Vitro |
GLUT4-IN-2 (compound F18) causes cell cycle arrest and death in CME cells during the G0/G1 phase [1]. GLUT4-IN-2 (10 µM; 6 hours) enhances the expression of GRP78 and cleaved caspase 3 protein but decreases the expression of mTOR and CDK2 [1].
In vitro, GLUT4-IN-2 (10 uM; 6 h) decreases the expression of mTOR and CDK2, but increases the expression of GRP78 and cleaved caspase-3 proteins. It shows potent cytotoxicity with CC50 values of 1.7 uM (CME), 91.9 uM (K562), 15.3 uM (KCL-22), 45.1 uM (MB-231), and 44.0 uM (HS-27) cells. |
| ln Vivo |
In a CEM xenograft model, GLUT4-IN-2 (50 mg/kg; i.p. on days 1–5, 8–12, 15–18) demonstrated antitumor activity [1].
In vivo, GLUT4-IN-2 (50 mg/kg; IP) exhibits potent in vivo anti-tumor activity in an 8-10 week old SCID mouse xenograft model of CEM cells, when administered on days 1-5, 8-12, and 15-18. Further detailed efficacy data is pending full publication. |
| Enzyme Assay |
For cell-free assays: recombinant GLUT1 and GLUT4 transporter proteins are immobilized on liposomes or reconstituted into proteoliposomes. The compound is incubated with the transporters and a fluorescent glucose analog (e.g., 2-NBDG). Inhibition of glucose uptake is measured by fluorescence intensity. IC50 values are calculated from dose-response curves.
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| Cell Assay |
Cell Viability Assay[1]
Cell Types: CME, K562, KCL-22, MB-231, HS-27 Cell Tested Concentrations: 1-100 µM Incubation Duration: 48 hrs (hours) Experimental Results: Demonstrated effective cytotoxicity with a cytotoxic concentration of 50 % (CC50) CME, K562, KCL-22, MB-231, and HS-27 cells are 1.7, 91.9, 15.3, 45.1, and 44.0 µM, respectively. Apoptosis analysis [1] Cell Types: CEM Cell Tested Concentrations: 1.7 µM Incubation Duration: 24 h Experimental Results: Cell apoptosis was induced, and the proportions of apoptotic cells in late and early apoptotic areas were 55.87% and 1.38% respectively. Cell cycle analysis[1] Cell Types: CEM Cell Tested Concentrations: 10, 25, 50 µM Incubation Duration: 72 hrs (hours) Experimental Results: Induces cell cycle arrest in G0/G1 phase in a dose-dependent manner. Western Blot Analysis[1] Cell Types: CEM Cell Tested Concentrations: 10 µM Incubation Duration: 6 hrs (hours) Experimental Results: diminished phosphorylation of mTOR and CDK2 proteins, increased expression of GRP78 and cleaved caspase 3. Cytotoxicity assay[1] Cell Types: CEM Cell Tested Concentrations: 2.5-100 µM Incubat For cell assays: cancer cell lines (CME, K562, KCL-22, MB-231, HS-27) are treated with GLUT4-IN-2 (1-100 uM; 48 h). Cell viability is assessed by MTT or CCK-8 assay. Apoptosis is measured by Annexin V/PI flow cytometry. Cell cycle arrest is analyzed by propidium iodide staining and flow cytometry. |
| Animal Protocol |
Animal/Disease Models: 8-10 weeks, SCID (severe combined immunodeficient) mouse (CEM xenograft tumors) [1]
Doses: 50 mg/kg Route of Administration: intraperitoneal (ip) injection; administered on days 1-5, 8-12, 15-18 Experimental Results: Displayed potent in vivo antitumor activity. For in vivo animal studies: an 8-10 week old SCID mouse xenograft model bearing CEM cells is treated with GLUT4-IN-2 (50 mg/kg; IP) on days 1-5, 8-12, and 15-18. Tumor volume is measured with calipers, and body weight is monitored to assess tolerability. |
| ADME/Pharmacokinetics |
PK properties of GLUT4-IN-2: The compound has a molecular weight of 385.42 and is soluble in DMSO (80 mg/mL). For in vivo studies, it is formulated in 10% DMSO + 90% corn oil (3.3 mg/mL, 8.56 mM) for IP injection. No formal PK parameters (t1/2, Cmax, AUC) have been reported.
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| Toxicity/Toxicokinetics |
No toxicity data have been published for GLUT4-IN-2 in peer-reviewed literature. Based on its GLUT4 inhibition mechanism, potential metabolic side effects may include altered glucose homeostasis and hypoglycemia. No acute toxicity or LD50 studies have been reported to date.
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| References | |
| Additional Infomation |
GLUT4-IN-2 is a research compound not yet approved for clinical use. It serves as a valuable chemical probe for studying the role of glucose transporters in cancer metabolism and tumor proliferation. It has potential as a lead compound for developing antimetabolic therapies for cancer and metabolic disorders.
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| Molecular Formula |
C17H11N3O4S2
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|---|---|
| Molecular Weight |
385.416940927505
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| Exact Mass |
385.019
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| CAS # |
2454113-83-6
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| PubChem CID |
162673506
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| Appearance |
Off-white to light yellow solid powder
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| LogP |
3.2
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
26
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| Complexity |
642
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| Defined Atom Stereocenter Count |
0
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| SMILES |
S1C(=CC2=CC=CO2)C(=O)N(CC(NC2=NC3=CC=CC=C3S2)=O)C1=O
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| InChi Key |
NWXKGGNFDDOYOU-MDWZMJQESA-N
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| InChi Code |
InChI=1S/C17H11N3O4S2/c21-14(19-16-18-11-5-1-2-6-12(11)25-16)9-20-15(22)13(26-17(20)23)8-10-4-3-7-24-10/h1-8H,9H2,(H,18,19,21)/b13-8+
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| Chemical Name |
N-(1,3-benzothiazol-2-yl)-2-[(5E)-5-(furan-2-ylmethylidene)-2,4-dioxo-1,3-thiazolidin-3-yl]acetamide
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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 (~259.5 mM; with ultrasonication and warming by heating to 80°C)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (6.49 mM) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), Clear solution; with ultrasonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 900 μL of corn oil and mix well. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5946 mL | 12.9729 mL | 25.9457 mL | |
| 5 mM | 0.5189 mL | 2.5946 mL | 5.1891 mL | |
| 10 mM | 0.2595 mL | 1.2973 mL | 2.5946 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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