2. Apoptosis Epigenetics Cell Cycle/DNA Damage
  3. Caspase PARP Apoptosis
  4. Antitumor agent-214

Antitumor agent-214 是具有抗癌活性的查尔酮类似物。Antitumor agent-214 可诱导肿瘤细胞周期阻滞和凋亡 (apoptosis)，破坏线粒体代谢稳态，上调 caspase-3、caspase-7 及 caspase-9，下调 PARP1。Antitumor agent-214 可用于结直肠癌、乳腺癌、肺癌、宫颈癌的抗肿瘤相关研究

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Antitumor agent-214

Antitumor agent-214 Chemical Structure

CAS No. : 1911631-77-0

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Antitumor agent-214 相关抗体

Top Publications Citing Use of Products

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Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

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PARP PARP1 PARP2 PARP3 PARP4 TNKS1/PARP5A TNKS2/PARP5B PARP7 PARP10 PARP14 PARP15 PARP12 PARP16

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Antitumor agent-214 is a chalcone analogue with anti-tumor activity. Antitumor agent-214 induces cell cycle arrest and apoptosis in tumor cells, disrupts mitochondrial metabolism, and upregulates the expression of caspase 3, caspase 7 and caspase 9, downregulates PARP1. Antitumor agent-214 can be used for anti-tumor research related to colorectal cancer, breast cancer, lung cancer, and cervical cancer[1].

IC50 & Target

Caspase 3

 

Caspase-7

 

Caspase-9

 

PARP-1

 

体外研究
(In Vitro)

Antitumor agent-214 (Compound 3f) 对 HCT-116 细胞 (IC50 = 3.56 μM)、MCF-7 细胞 (IC50 = 4.08 μM)、A549 细胞 (IC50 = 12.70 μM)、HeLa 细胞 (IC50 = 8.37 μM)、 HT-29 细胞 (IC50 = 6.18 μM) 和 MD-MBA-231 细胞 (IC50 = 10.62 μM) 具有细胞毒性，对非癌细胞 MCF-10A 的细胞毒性较低 (IC50 = 9.81 μM)[1]。
Antitumor agent-214 (1.78-7.12 μM; 24 h) 导致 HCT-116 细胞亚 G1 期细胞剂量依赖性积累，表明其诱导细胞凋亡[1]。
Antitumor agent-214 (3.56 μM, 7.12 μM; 24 h) 经 Annexin V-FITC/PI 双染色法证实可诱导 HCT-116 细胞凋亡，7.12 μM 时的凋亡率与星形孢菌素 (Staurosporine) 相当，且对 MCF-10A 细胞的凋亡诱导作用较弱[1]。
Antitumor agent-214 (3.56 μM, 7.12 μM; 24 h) 经 AO-EB 双染色证实可诱导 HCT-116 细胞凋亡，橙色荧光凋亡细胞比例呈剂量依赖性增加[1]。
Antitumor agent-214 (3.56 μM, 7.12 μM; 24 h) 经 MitoSOX Red 染色检测，可诱导 HCT-116 细胞线粒体超氧化物生成增加[1]。
Antitumor agent-214 (7.12 μM; 24 h) 经 JC-1 (HY-15534) 染色显示，可导致 HCT-116 细胞线粒体膜电位去极化[1]。
Antitumor agent-214 (7.12 μM; 4-12 h) 可促进 HCT-116 细胞中 PARP1、caspase 3、caspase 7 和 caspase 9 的切割， 12 h 时切割蛋白显著积累[1]。

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

Antitumor agent-214 相关抗体:

Cell Viability Assay[1]

Cell Line: HCT-116, MCF-7, A549, HeLa, HT-29, MD-MBA-231, MCF-10A cells
Concentration: 0-20 μM
Incubation Time: 72 h
Result: Exhibited potent anti-proliferative activity on all tested cancer cell lines, with IC50 values of 3.56 μM (HCT-116), 4.08 μM (MCF-7), 12.70 μM (A549), 8.37 μM (HeLa), 6.18 μM (HT-29), 10.62 μM (MD-MBA-231), and showed certain selectivity between tumor cells and normal MCF-10A cells (IC50=9.81 μM).

Cell Cycle Analysis[1]

Cell Line: HCT-116 cells
Concentration: 1.78 μM, 3.56 μM, 7.12 μM
Incubation Time: 24 h
Result: Induced a significant dose-dependent accumulation of cells in the sub-G1 phase, while had no marked effect on the distribution of cells in G0/G1, S and G2/M phases.

Apoptosis Analysis[1]

Cell Line: HCT-116 cells
Concentration: 3.56 μM, 7.12 μM
Incubation Time: 24 h
Result: Induced apoptosis in a dose-dependent manner, the percentage of apoptotic cells induced by antitumor agent-214 was equivalent to that induced by the positive control staurosporine (STS).

Apoptosis Analysis[1]

Cell Line: MCF-10A cells
Concentration: 9.81 μM, 19.62 μM
Incubation Time: 24 h
Result: Induced apoptosis in a dose-dependent manner, the percentage of apoptotic cells induced by antitumor agent-214 was only 54% of that induced by STS, showing lower apoptosis-inducing potency in normal cells than in cancer cells.

Western Blot Analysis[1]

Cell Line: HCT-116 cells
Concentration: 7.12 μM
Incubation Time: 4 h, 8 h, 12 h
Result: Time-dependently increased the protein levels of cleaved PARP1, cleaved caspase 3, cleaved caspase 7 and cleaved caspase 9, activating the caspase cascade of the mitochondrial death pathway.
分子量

336.34

Formula

C19H16N2O4
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

Antitumor agent-214 相关分类

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Keywords:

Antitumor agent-2141911631-77-0Antitumor agent214Antitumor agent 214CaspasePARPApoptosispoly ADP ribose polymerase Anti-tumordisrupts mitochondrial metabolismcell cycle arrest and apoptosisupregulates the expression of caspase 3caspase 7 and caspase 9colorectal cancerbreast cancertriple-negative breast cancer (TNBC)lung cancercervical carcinomaHCT-116 cellsMCF-7 cellsA549 cellsHeLa cellsHT-29 cellsMD-MBA-231 cellsMCF-10A cellsInhibitorinhibitorinhibit

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