2454113-83-6
2454113-83-6 structure
- Name: GLUT4-IN-2
- Chemical Name: GLUT4-IN-2
- CAS Number: 2454113-83-6
- Molecular Formula: C17H11N3O4S2
- Molecular Weight: 385.42
- Catalog: Signaling Pathways Apoptosis Apoptosis
- Create Date: 2022-07-28 12:05:02
- Modify Date: 2024-01-12 17:25:47
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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[1].
| Name | GLUT4-IN-2 |
|---|
| Description | 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[1]. |
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| Related Catalog | |
| Target |
GLUT1:11.4 μM (IC50) GLUT4:6.8 μM (IC50) |
| 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]. 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]. 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. |
| References |
| Molecular Formula | C17H11N3O4S2 |
|---|---|
| Molecular Weight | 385.42 |