TCL6148
TCL6148 is a ferroptosis inducer targeting GOT1, with a KD of 25.84 μM for GOT1. TCL6148 inhibits the viability of renal cell carcinoma 786-O and A498 cells, with IC50 values of 7.896 μM and 7.468 μM, respectively. TCL6148 induces ferroptosis by increasing Fe2+, ROS and lipid peroxidation, reducing GSH and inhibiting the GOT1/GPX4 pathway; it also inhibits proliferation and migration of RCC cells, enhances cellular sensitivity to Sunitinib (HY-10255A) and suppresses the growth of RCC xenograft tumors. TCL6148 can be used in research on renal cell carcinoma and ferroptosis.
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- Formule: C113H168N26O27S2
- Masse moléculaire:2386.83
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
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Activité biologique
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GOT1 25.84 μM (Kd) |
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Cell Line
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Type | Value | Description | References |
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| 786-0 | IC50 |
7.896 μM
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TCL6148 inhibits 786-O cell viability after 24 h exposure.
TCL6148 inhibits 786-O cell viability after 24 h exposure.
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40379184 |
| A498 | IC50 |
7.468 μM
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TCL6148 inhibits A498 cell viability after 24 h exposure.
TCL6148 inhibits A498 cell viability after 24 h exposure.
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40379184 |
| HK-2 | IC50 |
210.5 μM
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TCL6148 shows markedly lower cytotoxicity toward normal human renal tubular epithelial HK-2 cells.
TCL6148 shows markedly lower cytotoxicity toward normal human renal tubular epithelial HK-2 cells.
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40379184 |
TCL6148 (0.78-50 μM) binds to purified GOT1 protein, with a Kd value of 25.84 μM[1].
TCL6148 (10 μM; 24 h) significantly suppresses GOT enzymatic activity in 786-O and A498 renal cell carcinoma (RCC) cells[1].
TCL6148 (0-50 μM; 24 h) potently inhibits the viability of 786-O (IC50 = 7.896 μM) and A498 (IC50 = 7.468 μM) renal cell carcinoma cells in a dose-dependent manner, while it shows extremely low cytotoxicity against normal HK-2 renal cells after 24 h of treatment (IC50 = 210.5 μM)[1].
TCL6148 (2-10 μM; 24 h) inhibits the migration of 786-O and A498 renal cell carcinoma (RCC) cells in a dose-dependent manner, exhibiting significant inhibitory effects after treatment with 10 μM for 24 h[1].
TCL6148 (2-10 μM; 24 h) inhibits the proliferation of 786-O and A498 renal cell carcinoma (RCC) cells in a dose-dependent manner, and the proportion of EdU-positive cells decreases by approximately 40% after treatment with 10 μM for 24 h[1].
TCL6148 (2 μM; 24 h) enhances the sensitivity of 786-O and A498 cells to Sunitinib, reducing the IC50 values of Sunitinib from 9.216 μM and 11.12 μM to 4.049 μM and 4.414 μM, respectively, and further inhibits cell migration and proliferation[1].
TCL6148 (2-10 μM; 24 h) induces ferroptosis in 786-O and A498 renal cell carcinoma cells in a dose-dependent manner by increasing intracellular Fe2+ accumulation, ROS production and lipid peroxidation, while decreasing GSH levels after 24 h of treatment[1].
Treatment with TCL6148 (2-10 μM; 24 h) downregulates the protein expression levels of GOT1 and GPX4 in a dose-dependent manner in 786-O and A498 renal cell carcinoma (RCC) cells[1].
TCL6148 (2 μM) enhances Sunitinib-induced ferroptosis in RCC cells, increasing the relative Fe2+ levels from 1.93 to 2.79 in 786-O cells and from 1.72 to 2.25 in A498 cells. Meanwhile, it further elevates ROS and MDA levels, reduces GSH levels, and further downregulates GOT1 and GPX4[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:human RCC cell lines 786-O, A498, and normal human renal tubular epithelial cells HK-2
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Concentration:0-50 μM
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Incubation Time:24 h
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Result:Reduced RCC cell viability in a dose-dependent manner, with IC50 values of 7.896 μM for 786-O, 7.468 μM for A498, and 210.5 μM for HK-2 cells.
Maintained HK-2 cell viability at 93.64% at 10 μM.
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Cell Line:human RCC cell lines 786-O and A498
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Concentration:2-10 μM
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Incubation Time:24 h
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Result:Suppressed RCC cell migration in a dose-dependent manner.
Decreased the relative migration rate of both cell lines to <20% compared to untreated controls at 10 μM.
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Cell Line:human RCC cell lines 786-O and A498
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Concentration:2-10 μM
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Incubation Time:24 h
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Result:Reduced the proportion of EdU-positive cells in a dose-dependent manner.
Decreased the percentage of EdU-positive cells by approximately 40% compared to untreated controls at 10 μM.
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Cell Line:human RCC cell lines 786-O and A498
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Concentration:2-10 μM
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Incubation Time:24 h
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Result:Downregulated protein expression levels of both GOT1 and GPX4 in a dose-dependent manner, with the most significant reduction observed at 10 μM.
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Cell Line:human RCC cell lines 786-O and A498
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Concentration:2 μM (TCL6148; combined with sunitinib at concentrations to determine IC50)
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Incubation Time:24 h
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Result:Reduced the IC50 of sunitinib from 9.216 μM to 4.049 μM in 786-O cells, and from 11.12 μM to 4.414 μM in A498 cells, indicating enhanced sunitinib sensitivity.
TCL6148 (15 mg/kg; once every 3 days; for 30 days) reduces the expression of GOT1 and GPX4 in 786-O xenograft tumor tissues, and the downregulation of GOT1 and GPX4 is more pronounced when TCL6148 is combined with Sunitinib (20 mg/kg)[1]
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c nude mice[1]
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Dosage:15 mg/kg; 15 mg/kg (in combination with 20 mg/kg sunitinib)
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Administration:s.c.; every three days; 30 days
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Result:Significantly reduced tumor volume compared to the control group.
Showed good tolerance, with no significant changes in body weight observed throughout the experiment.
Decreased expression levels of GOT1 and GPX4 in tumor tissues.
Further suppressed tumor growth when combined with sunitinib compared to either treatment alone.
Caused a more pronounced reduction in GOT1 and GPX4 expression when combined with sunitinib compared to either treatment alone.
Chemical Information
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Masse moléculaire 2386.83
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Formule C113H168N26O27S2
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Sequence
Met-Cys-Leu-Ser-Phe-Arg-Phe-Ser-Phe-Glu-Leu-Ala-Val-Thr-Pro-Leu-Gln-Phe-Leu-His
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Sequence Shortening
MCLSFRFSFELAVTPLQFLH
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
TCL6148 Related Classifications
HY-P11929 Related Classifications
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