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

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.

For research use only. We do not sell to patients.

Antitumor agent-214

Antitumor agent-214 Chemical Structure

CAS No. : 1911631-77-0

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Antitumor agent-214 Related Antibodies

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

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Description

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

 

In Vitro

Antitumor agent-214 (Compound 3f) exhibits cytotoxic activity against HCT-116 cells (IC50 = 3.56 μM), MCF-7 cells (IC50 = 4.08 μM), A549 cells (IC50 = 12.70 μM), HeLa cells (IC50 = 8.37 μM), HT-29 cells (IC50 = 6.18 μM) and MD-MBA-231 cells (IC50 = 10.62 μM), with lower cytotoxicity against non-cancerous cells MCF-10AMCF-10A (IC50 = 9.81 μM) [1].
Antitumor agent-214 (1.78-7.12 μM; 24 h) causes a dose-dependent accumulation of HCT-116 cells in the sub-G1 phase, indicating induction of apoptosis[1].
Antitumor agent-214 (3.56 μM, 7.12 μM; 24 h) induces apoptosis in HCT-116 cells as confirmed by Annexin V-FITC/PI dual staining (HY-K1073), with the apoptosis rate equivalent to that induced by Staurosporine (HY-15141), and shows weaker apoptotic effect on MCF-10A cells[1].
Antitumor agent-214 (3.56 μM, 7.12 μM; 24 h) induces apoptosis in HCT-116 cells as demonstrated by AO-EB double staining, with the proportion of orange fluorescent apoptotic cells increasing dose-dependently[1].
Antitumor agent-214 (3.56 μM, 7.12 μM; 24 h) increases mitochondrial superoxide production in HCT-116 cells as detected by MitoSOX Red (HY-D1055) staining[1].
Antitumor agent-214 (7.12 μM; 24 h) induces depolarization of mitochondrial transmembrane potential in HCT-116 cells as shown by JC-1 (HY-15534) staining[1].
Antitumor agent-214 (7.12 μM; 4-12 h) promotes the cleavage of PARP1, caspase 3, caspase 7 and caspase 9 in HCT-116 cells as analyzed by WB, with significant accumulation of cleaved proteins at 12 h[1].

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

Antitumor agent-214 Related Antibodies

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.
Molecular Weight

336.34

Formula

C19H16N2O4
CAS No.
SMILES

O=C1NC(/C=C/C(C2=CC(OC)=CC=C2OC)=O)=NC3=C1C=CC=C3
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Purity & Documentation
References
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Antitumor agent-214 Related Classifications

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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:

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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