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D574-0246 is a dual-active inhibitor of OXCT1, targeting the enzyme's keto-dehydrogenase and succinyl-transferase activities. It reduces substrate-specific (LACTB K284) and global protein succinylation in HepG2 cells and lowers the ketolytic activity of OXCT1. The compound decreases the viability of HCC cells with an IC50 of 16.49 μM in PLC cells and 6.656 μM in HepG2 cells. In nude mice with HepG2 xenograft tumors overexpressing OXCT1, D574-0246 demonstrates anti-tumor effects. It is applicable for studies on hepatocellular carcinoma (HCC).
| Pack Size | Price | USA Stock | Global Stock | Quantity |
|---|---|---|---|---|
| 10 mg | Inquiry | 10-14 weeks | 10-14 weeks | |
| 50 mg | Inquiry | 10-14 weeks | 10-14 weeks |
| Description | D574-0246 is a dual-active inhibitor of OXCT1, targeting the enzyme's keto-dehydrogenase and succinyl-transferase activities. It reduces substrate-specific (LACTB K284) and global protein succinylation in HepG2 cells and lowers the ketolytic activity of OXCT1. The compound decreases the viability of HCC cells with an IC50 of 16.49 μM in PLC cells and 6.656 μM in HepG2 cells. In nude mice with HepG2 xenograft tumors overexpressing OXCT1, D574-0246 demonstrates anti-tumor effects. It is applicable for studies on hepatocellular carcinoma (HCC). |
| In vitro | D574-0246 decreases the survival rate of PLC cells with an IC50 of 16.49 μM and reduces the viability of HepG2 cells with an IC50 of 6.656 μM. At concentrations of 1-10 μM, D574-0246 significantly diminishes substrate-specific (LACTB K284) and global protein succinylation in HepG2 cells in a dose-dependent manner. Additionally, D574-0246 (1-10 μM) significantly reduces the ketoacid transferase activity of OXCT1 in HepG2 cells. |
| In vivo | Administered as an intraperitoneal injection at a dosage of 55 mg/kg every three days for a total of eight treatments, D574-0246 significantly inhibits tumor growth in nude mice xenografted with HepG2 cells overexpressing OXCT1. |
| Synonyms | iOXCT1 |
| Molecular Weight | 446.51 |
| Formula | C24H26N6O3 |
| Cas No. | 1269110-12-4 |
| Smiles | O=C(NC1=CC=C2OCOC2=C1)N3CCN(C4=NC(=NC(=C4)C)NC5=CC=C(C=C5)C)CC3 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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