1. Cell Cycle/DNA Damage Metabolic Enzyme/Protease
  2. PDI
  3. Dicentrinone

Dicentrinone 是一种具有口服活性的 PDI 抑制剂,其 IC50 值为 43.95 μM。Dicentrinone 可直接与 PDI 结合,抑制细胞增殖并降低癌细胞存活率。Dicentrinone 可通过抑制白细胞迁移、血浆渗出和足爪水肿,以及清除自由基来发挥抗炎和抗氧化作用。Dicentrinone 可用于肝癌、风湿病和关节炎的相关研究。

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Dicentrinone

Dicentrinone Chemical Structure

CAS No. : 16408-78-9

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Dicentrinone is an orally active PDI inhibitor with an IC50 value of 43.95 μM. Dicentrinone directly binds to PDI and suppresses cell proliferation and reduces cancer cell viability. Dicentrinone elicits anti-inflammatory and antioxidant effects by suppressing leukocyte migration, plasma leakage and paw edema, and scavenging free radicals. Dicentrinone can be used in the research of hepatoma, rheumatism and arthritis[1][2][3].

体外研究
(In Vitro)

Dicentrinone (compound 1) (1-100 μM; 48 h) 可强效抑制 HepG2 细胞增殖,其 CC50 为 20.70 μM[1]
Dicentrinone (3-300 μM; 1 h) 可抑制纯化的牛 PDI 活性,其 IC50 为 56.70 μM[1]
Dicentrinone (56.70 μM; 48 h) 可通过抑制 PDI 特异性抑制 HepG2 细胞活力,因为与 PDI siRNA 联合处理不会增强其细胞毒性作用[1]
Dicentrinone (72 h) 对 MCF-7、HCT116、HepG2、HL-60 或 MRC-5 细胞的生长无抑制作用,孵育 72 h 后的 IC50 >10 μM[2]

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

Cell Proliferation Assay[1]

Cell Line: human hepatoma HepG2 cells
Concentration: log0, log0.5, log1, log1.5, log2 μM
Incubation Time: 48 h
Result: Reduced HepG2 cell viability in a dose-dependent manner: at 1 μM, cell viability was 75.29%; at 10 μM, cell viability was 59.98%; at 50 μM, cell viability was 11.79%.
Calculated the 50% cytotoxic concentration (CC50) as 20.70 μM.

Cell Viability Assay[1]

Cell Line: human hepatoma HepG2 cells
Concentration: 56.70 μM
Incubation Time: 48 h (siRNA transfection prior to treatment)
Result: Reduced the cell number index to 0.54 in the siCtl group compared to untreated siCtl cells.
Showed no further reduction of cell number index when co-treated with siPDI compared to siPDI alone.
体内研究
(In Vivo)

Dicentrinone (100 mg/kg;口服) 可显著抑制 Carrageenan 诱导的瑞士小鼠足肿胀,且在造模后 2 h 和 4 h 均有该效应[3]
Dicentrinone (100 mg/kg;口服) 可在瑞士小鼠气囊炎症模型中抑制 Carrageenan 诱导的白细胞迁移达 69.1%,抑制血浆渗出达 50.4%[3]
Dicentrinone (100 mg/kg;口服) 可显著抑制雄性小鼠关节腔注射酵母聚糖诱导的关节肿胀与滑膜白细胞募集浸润[3]

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

分子量

335.31

Formula

C19H13NO5

CAS 号
结构分类
初始来源
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
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  • 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.

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Dicentrinone
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HY-N19464
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