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

D574-0246 是一种 OXCT1 双重活性抑制剂，抑制 OXCT1 的酮解和琥珀酰转移酶活性。D574-0246 减少 HepG2 细胞中底物特异性 (LACTB K284) 和全局蛋白琥珀酰化，并降低 OXCT1 的酮解活性。D574-0246 抑制 HCC 细胞的存活率 (IC50：PLC 细胞为 16.49 μM，HepG2 细胞为 6.656 μM)。D574-0246 在携带 OXCT1 过表达 HepG2 异种移植瘤的裸鼠中发挥抗肿瘤疗效。D574-0246 可用于肝细胞癌 (HCC) 研究 。

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D574-0246

D574-0246 Chemical Structure

CAS No. : 1269110-12-4

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D574-0246 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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].

体外研究
(In Vitro)

D574-0246 (4 天) 降低 PLC 细胞的存活率，其 IC50 为 16.49 μM，降低 HepG2 细胞的存活率，其 IC50 为 6.656 μM[1]。
D574-0246 (1-10 μM) 以剂量依赖方式显著减少 HepG2 细胞中底物特异性 (LACTB K284) 和全局蛋白琥珀酰化[1]。
D574-0246 (1-10 μM) 显著降低 HepG2 细胞中 OXCT1 的酮解活性[1]。

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

D574-0246 相关抗体:
体内研究
(In Vivo)

D574-0246 (55 mg/kg，腹腔注射，每 3 天一次，共 8 次) 显著抑制携带 OXCT1 过表达 HepG2 异种移植瘤的裸鼠中肿瘤生长[1]。

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.
分子量

446.50

Formula

C24H26N6O3
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

D574-0246 相关分类

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  • Do most proteins show cross-species activity?

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Keywords:

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

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