1. Apoptosis
  2. Apoptosis
  3. Antitumor agent-83

Antitumor agent-83 是一种促凋亡蛋白 BAX 的激活剂,对肿瘤细胞有显著的抗增殖作用。Antitumor agent-83 通过诱导 BAX 的构象激活介导细胞凋亡 (Apoptosis),对 A549 细胞周期有抑制作用。Antitumor agent-83 具有良好的体外代谢稳定性和 CYP 谱。

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Antitumor agent-83

Antitumor agent-83 Chemical Structure

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Antitumor agent-83 is an activator of pro-apoptotic protein BAX and has significant anti-proliferation effect on tumor cells. Antiumor agent-83 mediates cell Apoptosis by inducing the conformational activation of BAX and has inhibitory effect on A549 cell cycle. Antiumor agent-83 has good metabolic stability and CYPs spectrum in vitro[1].

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
A549 GI50
2.15 μM
Compound: 6d
Antiproliferative activity against human A549 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay
Antiproliferative activity against human A549 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay
[PMID: 36680883]
HCT-116 GI50
3.31 μM
Compound: 6d
Antiproliferative activity against human HCT-116 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay
Antiproliferative activity against human HCT-116 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay
[PMID: 36680883]
K562 GI50
1.41 μM
Compound: 6d
Antiproliferative activity against human K562 cells expressing BAX assessed as cell growth inhibition incubated for 72 hrs by trypan blue cell counting analysis
Antiproliferative activity against human K562 cells expressing BAX assessed as cell growth inhibition incubated for 72 hrs by trypan blue cell counting analysis
[PMID: 36680883]
MDA-MB-231 GI50
3.98 μM
Compound: 6d
Antiproliferative activity against human MDA-MB-231 cells expressing BAX assessed as cell growth inhibition incubated for 72 hrs by MTT assay
Antiproliferative activity against human MDA-MB-231 cells expressing BAX assessed as cell growth inhibition incubated for 72 hrs by MTT assay
[PMID: 36680883]
MV4-11 GI50
2.84 μM
Compound: 6d
Antiproliferative activity against human MV4-11 cells expressing BAX assessed as cell growth inhibition incubated for 72 hrs by trypan blue cell counting analysis
Antiproliferative activity against human MV4-11 cells expressing BAX assessed as cell growth inhibition incubated for 72 hrs by trypan blue cell counting analysis
[PMID: 36680883]
NCI-H1581 GI50
2.15 μM
Compound: 6d
Antiproliferative activity against human NCI-H1581 cells expressing BAX assessed as cell growth inhibition incubated for 72 hrs by MTT assay
Antiproliferative activity against human NCI-H1581 cells expressing BAX assessed as cell growth inhibition incubated for 72 hrs by MTT assay
[PMID: 36680883]
PC-3 GI50
2.5 μM
Compound: 6d
Antiproliferative activity against human PC-3 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay
Antiproliferative activity against human PC-3 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay
[PMID: 36680883]
THP-1 GI50
2.18 μM
Compound: 6d
Antiproliferative activity against human THP-1 cells expressing BAX assessed as cell growth inhibition incubated for 72 hrs by trypan blue cell counting analysis
Antiproliferative activity against human THP-1 cells expressing BAX assessed as cell growth inhibition incubated for 72 hrs by trypan blue cell counting analysis
[PMID: 36680883]
体外研究
(In Vitro)

Antitumor agent-83 (Compound 6d) (5-40 µM;24 h) 对 BAX 有激活作用并介导细胞凋亡,以剂量依赖的方式促进细胞色素 C 的释放[1]
Antitumor agent-83 对 A549、HCT-116、PC-3、H1581、MDA-MB-231、K562、MV4-11 和 THP-1 肿瘤细胞有显著的抗增殖作用,GI50 值分别为 2.15 µM、3.31 µM、2.50 µM、2.15 µM、3.98 µM、1.41 µM、2.84 µM、2.18 µM[1]
Antitumor agent-83 (1-5 µM;24、48 和 72 h) 以剂量和时间依赖的方式显著降低 A549 细胞的生存能力[1]
Antitumor agent-83 (5 µM 和 10 µM;48 h) 以剂量依赖性的方式促进 A549 细胞凋亡[1]
Antitumor agent-83 (2.5 µM 和 5 µM;48 h) 以剂量依赖性方式导致 G0/G1 期细胞周期阻滞[1]

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

Western Blot Analysis[1]

Cell Line: A549 cells.
Concentration: 5, 10, 20 and 40 µM.
Incubation Time: 24 h.
Result: Significantly up-regulated the expression level of BAX, activated the conformation of BAX and caused the release of cytochrome c.

Cell Viability Assay[1]

Cell Line: A549 cells.
Concentration: 1, 2, 3, 4 and 5 µM.
Incubation Time: 24, 48 and 72h.
Result: Showed inhibitory effect on the growth of A549 cells and exhibited greatest impact on the viability of A549 cells (5 µM; 72 h).

Apoptosis Analysis[1]

Cell Line: A549 cells.
Concentration: 5 and 10 µM.
Incubation Time: 48 h.
Result: Showed active effect on the apoptosis of A549 cells with cell apoptosis were 15.43 % and 73.40 % at the concentration of 5 µM and 10 µM, respectively.

Cell Cycle Analysis[1]

Cell Line: A549 cells.
Concentration: 2.5 and 5 µM.
Incubation Time: 48 h.
Result: Exhibited inhibitory effect on A549 cell cycle.
分子量

494.59

Formula

C29H30N6O2

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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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.

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产品名称:
Antitumor agent-83
目录号:
HY-152468
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