1. Cell Cycle/DNA Damage Cytoskeleton Metabolic Enzyme/Protease Apoptosis
  2. Microtubule/Tubulin Carbonic Anhydrase Apoptosis MDM-2/p53
  3. Anticancer agent 314

Anticancer agent 314 is a multi-target anticancer agent with tubulin polymerization inhibitory activity (IC50 = 6.35 μM) and human carbonic anhydrase IX (Ki = 27.1 nM) and XII (Ki 20.9 = nM) inhibitory activity. Anticancer agent 314 binds to the colchicine-binding pocket of tubulin and inhibits tumor-associated carbonic anhydrase isoforms via zinc coordination within enzyme active sites. Anticancer agent 314 induces G2/M phase cell cycle arrest, apoptosis via p53-dependent signaling, and broad-spectrum antiproliferative activity across multiple cancer cells. Anticancer agent 314 can be used for the research of cancer, such as leukemia, melanoma, ovarian cancer.

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

Anticancer agent 314

Anticancer agent 314 Chemical Structure

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Description

Anticancer agent 314 is a multi-target anticancer agent with tubulin polymerization inhibitory activity (IC50 = 6.35 μM) and human carbonic anhydrase IX (Ki = 27.1 nM) and XII (Ki 20.9 = nM) inhibitory activity. Anticancer agent 314 binds to the colchicine-binding pocket of tubulin and inhibits tumor-associated carbonic anhydrase isoforms via zinc coordination within enzyme active sites. Anticancer agent 314 induces G2/M phase cell cycle arrest, apoptosis via p53-dependent signaling, and broad-spectrum antiproliferative activity across multiple cancer cells. Anticancer agent 314 can be used for the research of cancer, such as leukemia, melanoma, ovarian cancer[1].

IC50 & Target[1]

hCA XII

20.9 nM (Ki)

hCA IX

27.1 nM (Ki)

In Vitro

Anticancer agent 314 (Compound 13n) potently inhibits the recombinant human tumor-associated carbonic anhydrase isoforms hCA IX (Ki = 27.1 nM) and hCA XII (Ki = 20.9 nM)[1].
Anticancer agent 314 (1.5-100 μM) potently inhibits cell-free tubulin polymerization with an IC50 of 6.35 μM[1].
Anticancer agent 314 (0.01-100 μM) exhibits broad-spectrum antiproliferative activity across the NCI-60 human tumor cell line panel, with GI50 values ranging from 2.48 to 31.00 μM[1].
Anticancer agent 314 has low cytotoxicity against WI-38 normal human lung fibroblasts, with an IC50 of 68.62 μM[1].
Anticancer agent 314 (6.35 μM; 24 h) potently arrests MCF-7 human breast cancer cells in the G2/M phase of the cell cycle, increasing the G2/M population to 31.97%[1].
Anticancer agent 314 (6.35 μM; 24 h) induces robust apoptosis in MCF-7 human breast cancer cells, increasing the total apoptotic population to 24.68%[1].
Anticancer agent 314 (6.35 μM; 24 h) activates the p53-dependent apoptotic pathway in MCF-7 human breast cancer cells, increasing p53, Bax, and activated caspase-7 levels while reducing Bcl-2 levels[1].

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

Cell Cycle Analysis[1]

Cell Line: MCF-7 human breast cancer cells
Concentration: 6.35 μM
Incubation Time: 24 h
Result: Increased the G2/M phase population from 13.81% (control) to 31.97% (treated).
Suppressed the G0/G1 phase population from 63.58% to 52.76%.
Reduced the S phase population from 22.61% to 15.27%.

Apoptosis Analysis[1]

Cell Line: MCF-7 human breast cancer cells
Concentration: 6.35 μM
Incubation Time: 24 h
Result: Increased the total apoptotic cell population from 0.67% (control) to 24.68% (treated), with 9.51% early apoptotic cells and 15.17% late apoptotic cells.

ELISA Assay[1]

Cell Line: MCF-7 human breast cancer cells
Concentration: 6.35 μM
Incubation Time: 24 h
Result: Increased p53 protein levels 3.43-fold relative to control cells.
Increased Bax levels 12.34-fold relative to control cells.
Reduced Bcl-2 levels 4.37-fold relative to control cells.
Increased caspase-7 activation 7.35-fold relative to control cells.
Molecular Weight

460.47

Formula

C22H16N6O4S

SMILES

CC1=NN2C(C3=CC4=C(OC3=O)C=CC=C4)=CC=NC2=C1/N=N/C5=CC=C(C=C5)S(N)(=O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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    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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Anticancer agent 314
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HY-182245
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