2. Metabolic Enzyme/Protease
  3. Mitochondrial Metabolism
  4. D574-0246

D574-0246 is a dual-activity inhibitor of OXCT1, inhibiting both the ketolytic and succinyltransferase activities of OXCT1. D574-0246 reduces substrate-specific (LACTB K284) and global protein succinylation and decreases OXCT1 ketolytic activity in HepG2 cells. D574-0246 inhibits the viability of HCC cells (IC50: 16.49 μM in PLC cells, 6.656 μM in HepG2 cells). D574-0246 exerts anti-tumor efficacy in nude mice bearing OXCT1-overexpressing HepG2 xenograft tumors. D574-0246 can be used for the study of hepatocellular carcinoma (HCC).

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D574-0246

D574-0246 Chemical Structure

CAS No. : 1269110-12-4

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Description

D574-0246 is a dual-activity inhibitor of OXCT1, inhibiting both the ketolytic and succinyltransferase activities of OXCT1. D574-0246 reduces substrate-specific (LACTB K284) and global protein succinylation and decreases OXCT1 ketolytic activity in HepG2 cells. D574-0246 inhibits the viability of HCC cells (IC50: 16.49 μM in PLC cells, 6.656 μM in HepG2 cells). D574-0246 exerts anti-tumor efficacy in nude mice bearing OXCT1-overexpressing HepG2 xenograft tumors. D574-0246 can be used for the study of hepatocellular carcinoma (HCC)[1].

In Vitro

D574-0246 (4 days) reduces the viability of PLC cells with an IC50 of 16.49 μM and HepG2 cells with an IC50 of 6.656 μM[1].
D574-0246 (1-10 μM) significantly reduces both substrate-specific (LACTB K284) and global protein succinylation in HepG2 cells in a dose-dependent manner[1].
D574-0246 (1-10 μM) significantly decreases the ketolytic activity of OXCT1 in HepG2 cells[1].

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

D574-0246 Related Antibodies
In Vivo

D574-0246 (55 mg/kg, i.p., once every 3 days for 8 times) significantly inhibits tumor growth in nude mice bearing OXCT1-overexpressing HepG2 xenograft tumors[1].

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

Animal Model: HepG2 cells with OXCT1 overexpression or knockout (2 × 106) were subcutaneously implanted into the flanks of 5-week-old male BALB/c nude mice[1]
Dosage: 55 mg/kg
Administration: i.p., once every 3 days for 8 times
Result: Inhibited tumor growth in nude mice bearing OXCT1-overexpressing HepG2 xenograft tumors, while exerting no significant inhibitory effect on tumor growth in nude mice with OXCT1-knockout HepG2 xenograft tumors.
Reduced both global protein succinylation levels and LACTB K284-specific succinylation levels in OXCT1-overexpressing tumor tissues.
Showed no significant changes in body weight.
Caused no significant abnormalities in serum levels of aspartate aminotransferase (AST), alanine aminotransferase (ALT), and alkaline phosphatase (ALP) in nude mice.
Induced no obvious morphological changes in major organs (liver, kidney, and spleen) of nude mice.
Molecular Weight

446.50

Formula

C24H26N6O3
CAS No.
Appearance

Solid

Color

White to light yellow

SMILES

CC1=CC=C(C=C1)NC2=NC(N3CCN(CC3)C(NC4=CC=C5OCOC5=C4)=O)=CC(C)=N2
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Purity & Documentation
References
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D574-0246 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

D574-02461269110-12-4iOXCT1iOXCT 1iOXCT-1Mitochondrial Metabolismhepatocellular carcinomaHepG2 cellsPLC cellsInhibitorinhibitorinhibit

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