GLUT4-IN-2 is a potent and specific GLUT4 inhibitor (antagonist) with IC50s of 11.4 µM and 6.8 µM for GLUT1 and GLUT4, respectively. GLUT4-IN-2 causes apoptosis and cell cycle arrest in the G0/G1 phase. GLUT4-IN-2 displays potent anti-tumor effects.

Physicochemical Properties

Molecular Formula	C17H11N3O4S2
Molecular Weight	385.416940927505
Exact Mass	385.019
CAS #	2454113-83-6
PubChem CID	162673506
Appearance	Off-white to light yellow solid powder
LogP	3.2
Hydrogen Bond Donor Count	1
Hydrogen Bond Acceptor Count	7
Rotatable Bond Count	4
Heavy Atom Count	26
Complexity	642
Defined Atom Stereocenter Count	0
SMILES	S1C(=CC2=CC=CO2)C(=O)N(CC(NC2=NC3=CC=CC=C3S2)=O)C1=O
InChi Key	NWXKGGNFDDOYOU-MDWZMJQESA-N
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+
Chemical Name	N-(1,3-benzothiazol-2-yl)-2-[(5E)-5-(furan-2-ylmethylidene)-2,4-dioxo-1,3-thiazolidin-3-yl]acetamide
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)

Biological Activity

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].
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].
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
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.
References	[1]. Structure guided design and synthesis of furyl thiazolidinedione derivatives as inhibitors of GLUT 1 and GLUT 4, and evaluation of their anti-leukemic potential. Eur J Med Chem. 2020 Sep 15;202:112603.

Solubility Data

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

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 (e.g. IP/IV/IM/SC) Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline) *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). 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)] *Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin → 500 μL Saline) Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO → 100 μLPEG300 → 200 μL castor oil → 650 μL Saline) Injection Formulation 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (i.e. 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline) Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH → 900 μL Corn oil) Injection Formulation 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH → 400 μLPEG300 → 50 μL Tween 80 → 450 μL 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). Oral Formulation 3: Dissolved in PEG400 Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose Oral Formulation 6: Mixing with food powders Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.  (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.