Art. -Nr.: HY-146980

GLUT4-IN-2

Name: GLUT4-IN-2
Brand: MedChemExpress
SKU: HY-146980
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Availability: InStock
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GLUT4-IN-2 is a potent and selective GLUT4 inhibitor with IC₅₀s of 11.4 µM and 6.8 µM for GLUT1 and GLUT4, respectively. GLUT4-IN-2 induces cell apoptosis and cell cycle arrest at G0/G1phase. GLUT4-IN-2 shows potent antitumor activity.

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Reinheit : 99.17%
CAS. Nr.: 2454113-83-6
Formel: C₁₇H₁₁N₃O₄S₂
Molecular Weight:385.42

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

GLUT4-IN-2 Chemical Structure

CAS. Nr.: 2454113-83-6

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

^[1]

GLUT1

11.4 μM (IC₅₀)

GLUT4

6.8 μM (IC₅₀)

Alle GLUT Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
CCRF-CEM	CC₅₀	1.7 μM Compound: F18	Cytotoxicity against human CCRF-CEM cells assessed as reduction in cell viability measured after 48 hrs by Hoechst 33342/propidium iodide staining based imaging analysis Cytotoxicity against human CCRF-CEM cells assessed as reduction in cell viability measured after 48 hrs by Hoechst 33342/propidium iodide staining based imaging analysis	[PMID: 32634629]
HS27	CC₅₀	44 μM Compound: F18	Cytotoxicity against human HS27 cells assessed as reduction in cell viability measured after 48 hrs by Hoechst 33342/propidium iodide staining based imaging analysis Cytotoxicity against human HS27 cells assessed as reduction in cell viability measured after 48 hrs by Hoechst 33342/propidium iodide staining based imaging analysis	[PMID: 32634629]
K562	CC₅₀	91.9 μM Compound: F18	Cytotoxicity against human K562 cells assessed as reduction in cell viability measured after 48 hrs by Hoechst 33342/propidium iodide staining based imaging analysis Cytotoxicity against human K562 cells assessed as reduction in cell viability measured after 48 hrs by Hoechst 33342/propidium iodide staining based imaging analysis	[PMID: 32634629]
KCL-22	CC₅₀	15.3 μM Compound: F18	Cytotoxicity against human KCL-22 cells assessed as reduction in cell viability measured after 48 hrs by Hoechst 33342/propidium iodide staining based imaging analysis Cytotoxicity against human KCL-22 cells assessed as reduction in cell viability measured after 48 hrs by Hoechst 33342/propidium iodide staining based imaging analysis	[PMID: 32634629]
MDA-MB-231	CC₅₀	45.1 μM Compound: F18	Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability measured after 48 hrs by Hoechst 33342/propidium iodide staining based imaging analysis Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability measured after 48 hrs by Hoechst 33342/propidium iodide staining based imaging analysis	[PMID: 32634629]

In Vitro

GLUT4-IN-2 (compound F18) induces cell apoptosis and ell cycle arrest at G0/G1phase in CME cells^[1].
GLUT4-IN-2 (10 µM; 6 h) decreases the expression of mTOR and CDK2, but increases the expression of GRP78, and cleaved caspase 3 proteins ^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay^[1]

Cell Line:

CME, K562, KCL-22, MB-231, HS-27 cells
Concentration:

1-100 µM
Incubation Time:

48 h
Result:

Showed potent cytotoxicity with cytotoxic concentration 50% (CC₅₀) of 1.7, 91.9, 15.3, 45.1, 44.0 µM for CME, K562, KCL-22, MB-231, HS-27 cells, respectively.

Apoptosis Analysis^[1]

Cell Line:

CEM cells
Concentration:

1.7 µM
Incubation Time:

24 h
Result:

Induced cell apoptosis with the percentage of apoptotic cells in the late and early apoptosis region was 55.87% and 1.38%, respectively.

Cell Cycle Analysis^[1]

Cell Line:

CEM cells
Concentration:

10, 25, 50 µM
Incubation Time:

72 h
Result:

Induced cell cycle arrest at G0/G1phase in a dose-dependent manner.

Western Blot Analysis^[1]

Cell Line:

CEM cells
Concentration:

10 µM
Incubation Time:

6 h
Result:

Decreased the phosphorylation of mTOR and CDK2 proteins and increased the expression of GRP78, and cleaved caspase 3.

Cell Cytotoxicity Assay^[1]

Cell Line:

CEM cells
Concentration:

2.5-100 µM
Incubation Time:

48 h
Result:

Showed cytotoxicity with the IC₅₀s of 1.7, 187.2 µM for CEM, WBCs cells respectively.

In Vivo

GLUT4-IN-2 (50 mg/kg; i.p. on day 1–5, 8–12, 15–18) shows antitumor activity in CEM xenograft model^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

8–10 weeks, SCID mice (CEM xenograft tumor) ^[1]
Dosage:

50 mg/kg
Administration:

I.p.; administered on day 1-5, 8-12, 15-18
Result:

Showed potent antitumor activity in vivo.

Related Protocols :

Chemical Information

CAS. Nr. 2454113-83-6
Appearance Solid
Molecular Weight 385.42
Formel C₁₇H₁₁N₃O₄S₂
Color Off-white to light yellow
SMILES

O=C(NC1=NC2=CC=CC=C2S1)CN(C/3=O)C(SC3=C\C4=CC=CO4)=O
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (259.46 mM; ultrasonic and warming and heat to 80°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: 2.5 mg/mL (6.49 mM); Clear solution; Need ultrasonic

This protocol yields a clear solution of 2.5 mg/mL. If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (278 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Tilekar K,et al. 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. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.5946 mL	12.9729 mL	25.9457 mL	64.8643 mL
	5 mM	0.5189 mL	2.5946 mL	5.1891 mL	12.9729 mL
	10 mM	0.2595 mL	1.2973 mL	2.5946 mL	6.4864 mL
	15 mM	0.1730 mL	0.8649 mL	1.7297 mL	4.3243 mL
	20 mM	0.1297 mL	0.6486 mL	1.2973 mL	3.2432 mL
	25 mM	0.1038 mL	0.5189 mL	1.0378 mL	2.5946 mL
	30 mM	0.0865 mL	0.4324 mL	0.8649 mL	2.1621 mL
	40 mM	0.0649 mL	0.3243 mL	0.6486 mL	1.6216 mL
	50 mM	0.0519 mL	0.2595 mL	0.5189 mL	1.2973 mL
	60 mM	0.0432 mL	0.2162 mL	0.4324 mL	1.0811 mL
	80 mM	0.0324 mL	0.1622 mL	0.3243 mL	0.8108 mL
	100 mM	0.0259 mL	0.1297 mL	0.2595 mL	0.6486 mL

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GLUT4-IN-2

Alle GLUT Isoform-spezifische Produkte anzeigen