2. Cell Cycle/DNA Damage Cytoskeleton Apoptosis
  3. Microtubule/Tubulin Apoptosis Caspase
  4. E7974

E7974 is a selective inhibitor of α-tubulin (α-tubulin) with an IC50 of 3.9 μM. E7974 disrupts mitotic spindle formation, induces G2-M phase cell cycle arrest, initiates apoptosis, activates caspase-3, and induces poly (ADP-ribose) polymerase cleavage. E7974 reduces the area of choroidal neovascularization in mouse models, and exerts anti-angiogenic effects when loaded in modified micelles. E7974 can be used in research related to cancer and choroidal neovascularization.

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E7974

E7974 Chemical Structure

CAS No. : 610787-07-0

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E7974 Related Antibodies

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Description

E7974 is a selective inhibitor of α-tubulin (α-tubulin) with an IC50 of 3.9 μM. E7974 disrupts mitotic spindle formation, induces G2-M phase cell cycle arrest, initiates apoptosis, activates caspase-3, and induces poly (ADP-ribose) polymerase cleavage. E7974 reduces the area of choroidal neovascularization in mouse models, and exerts anti-angiogenic effects when loaded in modified micelles. E7974 can be used in research related to cancer and choroidal neovascularization[1][2].

IC50 & Target[1]

α-Tubulin

3.9 μM (IC50)

In Vitro

E7974 (300 nM; 0-24 h) induces sustained G2-M phase mitotic arrest in human histiocytic lymphoma U-937 cells, thereby triggering apoptosis characterized by the formation of subdiploid cells starting at 8 h post-treatment[1].
E7974 (300 nM; 1-13 h) induces maximal mitotic arrest in human histiocytic lymphoma U-937 cells[1].
E7974 (300 nM; 0-24 h) induces apoptosis in human histiocytic lymphoma U-937 cells, which is confirmed by the cleavage of procaspase-3 and PARP starting at 6 h post-treatment[1].
E7974 (19.5-65 nM; 18 h) disrupts mitotic spindle formation and induces mitotic arrest in DU 145 human prostate cancer cells, and also reduces microtubule density in non-dividing cells at higher concentrations[1].
E7974 (300 nM) induces G2-M phase mitotic arrest and subsequent apoptosis in human prostate cancer cell line DU 145[1].

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

E7974 Related Antibodies

Cell Cycle Analysis[1]

Cell Line: U-937 human histiocytic lymphoma cells
Concentration: 300 nM
Incubation Time: 0-24 h
Result: Induced a G2-M block beginning as early as 4 h of treatment, with the G1 phase completely depleted by 10 h.
Showed an increasing hypodiploid cell population, indicative of apoptosis, evident at 8 h, and nearly all cells were hypodiploid after 24 h.
Demonstrated approximately 80% of U-937 cells in the G2-M peak after 14 h of treatment were positive for phospho-histone H3, confirming mitotic arrest, and close to half of hypodiploid cells were also phospho-histone H3 positive.

Cell Cycle Analysis[1]

Cell Line: U-937 human histiocytic lymphoma cells
Concentration: 300 nM
Incubation Time: 0, 10, 30, 45, 60 min, followed by 12 h incubation in drug-free medium
Result: Showed percentages of cells in G2-M after 12 h in drug-free medium were 15% (0 min exposure), 35% (10 min), 47% (30 min), 62% (45 min), and 71% (60 min).
Demonstrated a 60-minute exposure to E7974 was sufficient to induce near-complete mitotic arrest 12 h later.

Western Blot Analysis[1]

Cell Line: U-937 human histiocytic lymphoma cells
Concentration: 300 nM
Incubation Time: 0-24 h
Result: Induced proteolytic cleavage of procaspase-3 (generating active caspase-3) and PARP (generating an 84 kDa cleaved fragment) after 6 h of exposure, correlating with the appearance of hypodiploid cells detected by flow cytometry.

Immunofluorescence[1]

Cell Line: DU 145 human prostate cancer cells
Concentration: 19.5 nM, 65 nM
Incubation Time: 18 h
Result: Induced marked increases in numbers of mitotic cells (positive for phospho-histone H3), with disorganized, tangled arrays of short microtubule fragments forming abnormal mitotic spindles; chromosomes failed to align at the cell center, indicating arrest in late prophase or prometaphase.
Showed at the higher concentration (65 nmol/L), nonmitotic cells had marked decreases in microtubule density.
In Vivo

E7974 (0.2-20 µM; intravitreal; single dose immediately after laser coagulation) via intravitreal administration of 20 µM alone significantly reduces CNV area in a murine laser-induced CNV model[2].

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

Animal Model: C57BL/6J mice (male, adult, laser-induced choroidal neovascularization)[2]
Dosage: 0.2 µM; 2 µM; 20 µM
Administration: intravitreal; single dose immediately after laser coagulation
Result: Did not significantly reduce CNV area compared to vehicle-treated eyes (0.2 µM standalone).
Did not significantly reduce CNV area compared to vehicle-treated eyes (2 µM standalone).
Caused a significant reduction in CNV area compared to vehicle-treated eyes (20 µM standalone).
Molecular Weight

437.63

Formula

C24H43N3O4
CAS No.
SMILES

C(N[C@H](C(N([C@H](/C=C(/C(O)=O)\C)[C@@H](C)C)C)=O)C(C)(C)C)(=O)[C@@H]1N(C(C)C)CCCC1
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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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E7974 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:

E7974610787-07-0E 7974E-7974Microtubule/TubulinApoptosisCaspaseU-937 human histiocytic lymphoma cellsmitotic spindlepoly ADP ribose polymeraseα-tubulinβ-tubulincaspase-3G2-M cell cycle arresttubulin polymerizationapoptosisbovine tubulinInhibitorinhibitorinhibit

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