2. Apoptosis
  3. Apoptosis
  4. (±)-Forbesione

(±)-Forbesione 是 Forbesione (HY-N7892) 的消旋体，是一种潜在的细胞凋亡诱导 (apoptosis) 剂。(±)-Forbesione 可抑制癌细胞增。(±)-Forbesione 可用于癌症的相关研究。

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(±)-Forbesione

(±)-Forbesione Chemical Structure

CAS No. : 667914-50-3

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(±)-Forbesione 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

(±)-Forbesione, a potential apoptosis inducer, is a racemate of Forbesione (HY-N7892). (±)-Forbesione inhibits proliferation of cancer cells. (±)-Forbesione can be used for cancer research[1].

体外研究
(In Vitro)

(±)-Forbesione (24 小时) 对 HepG2、A549 和 U251 细胞表现出低微摩尔级的抗增殖活性，其 IC50 值分别为 4.07 μM、3.58 μM 和 8.57 μM[1]。

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

(±)-Forbesione 相关抗体:

Cell Cycle Analysis[1]

Cell Line: Ham-1 cholangiocarcinoma cells
Concentration: 0.5 µM; 1 µM; 2 µM; 4 µM; 8 µM
Incubation Time: 24 h
Result: Induced concentration-dependent S-phase cell cycle arrest (P<0.01).
Reduced the proportion of cells in the G0/G1 (P<0.05) and G2/M (P<0.05) phases.
Increased the percentage of cells in the sub-G1 fraction (apoptotic cells) significantly in a concentration-dependent manner (P<0.01).

Apoptosis Analysis[1]

Cell Line: Ham-1 cholangiocarcinoma cells
Concentration: 2 µM; 4 µM; 8 µM; 16 µM
Incubation Time: 24 h
Result: Induced bright green, condensed, and fragmented chromatin, which are hallmarks of apoptosis, in treated cells, while untreated cells showed uniformly green-stained, normal nuclei.

Apoptosis Analysis[1]

Cell Line: Ham-1 cholangiocarcinoma cells
Concentration: 2 µM; 4 µM; 8 µM; 16 µM; 32 μM
Incubation Time: 6, 24, 48 h
Result: Increased the percentage of apoptotic cells in a concentration- and time-dependent manner.
Resulted in 50.75% (P<0.01), 55.57% (P<0.001), and 64.43% (P<0.001) apoptotic cells at 6, 24, and 48 h respectively when treated with 32 µM.

Western Blot Analysis[1]

Cell Line: Ham-1 cholangiocarcinoma cells
Concentration: 2 µM; 4 µM; 8 µM
Incubation Time: 24 h
Result: Significantly decreased protein expression of cyclin E (P<0.01), cyclin A (P<0.05), and cyclin-dependent kinase 2 (Cdk2) (P<0.01).
Significantly increased protein expression of p21 (P<0.05) and p27 (P<0.05) compared to control cells.\nIncreased protein expression of Fas (P<0.05), Fas-associated death domain (FADD) (P<0.05), and activated caspase-3 (P<0.05) in the death receptor pathway.
Decreased protein expression of procaspase-8 (P<0.05) and procaspase-3 (P<0.01) in the death receptor pathway.
Increased protein expression of B-cell lymphoma-2-like protein 4 (Bax) (P<0.05), activated caspase-9 (P<0.05), and activated caspase-3 (P<0.05) in the mitochondrial pathway.
Decreased protein expression of B-cell lymphoma-2 (Bcl-2) (P<0.05), procaspase-9 (P<0.05), and procaspase-3 (P<0.01) in the mitochondrial pathway.
Increased protein expression of activated caspase-12 (P<0.05), activated caspase-9 (P<0.05), and activated caspase-3 (P<0.05) in the endoplasmic reticulum pathway.
Decreased protein expression of procaspase-12 (P<0.05), procaspase-9 (P<0.05), and procaspase-3 (P<0.01) in the endoplasmic reticulum pathway.\nSignificantly decreased protein expression of NF-κB/p65 (P<0.01) compared to control cells.
Significantly increased protein expression of inhibitor of κB-α (IκB-α) (P<0.05) compared to control cells.\nSignificantly decreased protein expression of cytokeratin 19 (CK19) (P<0.01) compared to control cells.
Significantly decreased protein expression of proliferating cell nuclear antigen (PCNA) (P<0.05) compared to control cells.

Apoptosis Analysis[3]

Cell Line: human cholangiocarcinoma KKU-100 cells
Concentration: 0.25 µM; 0.5 µM; 1 µM; 2 μM; 1 μM (combined with 0.025 μM Doxorubicin)
Incubation Time: 48 h
Result: Increased apoptosis in KKU-100 cells in a dose-dependent manner, with the highest single-agent dose (2 μM) inducing ~32% apoptotic cells.
Induced ~75% apoptotic cells when combined with 0.025 μM Doxorubicin, which was significantly higher than either single agent alone.

Western Blot Analysis[3]

Cell Line: human cholangiocarcinoma KKU-100 cells
Concentration: 0.25 μM; 0.5 μM; 1 μM (single agent); 0.25 μM + 0.006 μM Doxorubicin (C1); 0.5 μM + 0.012 μM Doxorubicin (C2); 1 μM + 0.025 μM Doxorubicin (C3)
Incubation Time: 48 h
Result: Decreased Bcl-2 expression (0.27-fold at 1 μM) and increased Bax expression (2.06-fold at 1 μM) as a single agent, leading to a Bax/Bcl-2 ratio of 1.63; the C3 combination further decreased Bcl-2 to 0.10-fold and increased Bax to 3.24-fold, resulting in a Bax/Bcl-2 ratio of 12.00.
Decreased survivin (0.35-fold at 1 μM), procaspase-9 (0.70-fold at 1 μM), and procaspase-3 (0.76-fold at 1 μM) while increasing activated caspase-9 (42.00-fold at 1 μM) and activated caspase-3 (42.00-fold at 1 μM) as a single agent; the C3 combination enhanced these effects, reducing procaspase-9 and procaspase-3 to 0-fold and increasing activated caspase-9 and caspase-3 to 64.00-fold and 54.00-fold, respectively.
Increased IκB-α (1.15-fold at 1 μM) and decreased pIκB-α (0.14-fold at 1 μM) and NF-κB/p65 (0.12-fold at 1 μM) as a single agent; the C3 combination further increased IκB-α to 1.21-fold and decreased pIκB-α and NF-κB/p65 to 0.01-fold each.
Decreased MRP1 expression (0.71-fold at 1 μM) as a single agent, while the C3 combination reduced MRP1 to 0.34-fold, a significantly greater effect than single-agent treatment.
体内研究
(In Vivo)
Animal Model: Syrian hamsters (male, 6-8 weeks old, intradermal injection of 2.5×105 Ham-1 cholangiocarcinoma cells)[1]
Dosage: 50 mg/kg
Administration: p.o.; daily; 4 weeks
Result: Reduced tumor volume (P<0.01) and mean tumor weight from 0.54 g (control) to 0.27 g (P<0.001).
Significantly decreased relative CK19 mRNA expression in tumor tissues (P<0.05).
Significantly increased relative Bax, Apaf-1, caspase-9, and caspase-3 mRNA expression in tumor tissues (P<0.05).
Significantly decreased expression of CK19 (P=0.036), PCNA (P=0.032), cyclin A (P=0.028), and Bcl-2 (P=0.039) in tumor tissues via immunohistochemical analysis.
Significantly increased expression of Bax (P=0.039), caspase-9 (P=0.028), and caspase-3 (P=0.039) in tumor tissues via immunohistochemical analysis.
Increased body weight (P<0.001), food intake (P<0.001), and water intake (P<0.05) in treated hamsters.
Caused no significant histopathological changes in liver, kidney, or stomach, and no changes in serum liver (ALT, ALP) or kidney (BUN, creatinine) function markers.
分子量

464.55

Formula

C28H32O6
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

(±)-Forbesione 相关分类

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  • 稀释计算器

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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:

(±)-Forbesione667914-50-3ApoptosisHepG2 cellsapoptosisU251 cellsA549 cellscancerInhibitorinhibitorinhibit

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