2. Apoptosis Immunology/Inflammation Cytoskeleton Cell Cycle/DNA Damage Neuronal Signaling
  3. Apoptosis COX Caspase Microtubule/Tubulin Monoamine Oxidase
  4. Geiparvarin

Geiparvarin is an anticancer agent and an inhibitor of MAO-B (pIC50 = 6.84 μM). Geiparvarin exerts anti-tumor effects by downregulating COX2 expression and inhibiting angiogenesis. Geiparvarin blocks the cell cycle at the G1 phase and induces apoptosis of cancer cells. Geiparvarin has anti-microtubule activity and destroys the cytoskeleton to exert anti-proliferative effects. Geiparvarin has research significance for lung cancer, leukemia, and breast cancer.

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Geiparvarin

Geiparvarin Chemical Structure

CAS No. : 36413-91-9

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Geiparvarin Related Antibodies

Top Publications Citing Use of Products

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COX COX-1 COX-2 COX-3

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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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MAO-A MAO-B

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Description

Geiparvarin is an anticancer agent and an inhibitor of MAO-B (pIC50 = 6.84 μM). Geiparvarin exerts anti-tumor effects by downregulating COX2 expression and inhibiting angiogenesis. Geiparvarin blocks the cell cycle at the G1 phase and induces apoptosis of cancer cells. Geiparvarin has anti-microtubule activity and destroys the cytoskeleton to exert anti-proliferative effects. Geiparvarin has research significance for lung cancer, leukemia, and breast cancer[1][2][3][4][5].

IC50 & Target

COX-2

 

Caspase 3

 

MAO-B

6.84 μM (pIC50)

In Vitro

Geiparvarin (Compound 8) (72h) inhibits the proliferation of human tumor cell lines (IC50: 5.7 μM for SHSY5Y, 6.3 μM for HL-60, 9.2 μM for K562, 9.8 μM for HT-1080, 11.5 μM for A-549)[1].

Geiparvarin (8 μM, 24-72 h) arrests HL-60 cell cycle at the G1 phase and induces caspase-independent apoptosis[1].

Geiparvarin (72 h) shows complete inhibitory effects on drug-resistant cell lines and is not affected by transporters that mediate the efflux of antitumor drugs[1].

Geiparvarin (1 μM, 24 h) inhibits cell invasion ability in HOS and 143B cells[2].

Geiparvarin (0.5-2 μM, 24-48 h) activates apoptotic pathways in HOS and 143B cells, inhibits COX2 and downstream angiogenic pathways, and induces caspase-dependent apoptosis[2].

Geiparvarin exerts its antitumor effects in osteosarcoma cells by downregulating COX2, and overexpression of COX2 reverses its inhibition of proliferation and invasion[2].

Geiparvarin (10 μM, 24 h) disrupts the cytoskeleton, especially intermediate filaments, in Balb/c 3T3 fibroblasts[3].

Geiparvarin (0.01-10 μM) shows a significant increase in the inhibition rate of MAO-B extracted from rat liver mitochondria with increasing concentration, pIC50 = 6.84 (IC50 = 1.45 μM)[4].

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

Geiparvarin Related Antibodies

Cell Viability Assay[1]

Cell Line: K562 cells, HL-60 cells, HT-1080 cells, A-549 cells, SHSY5Y cells , CEM cells, CEM/Vbl100 cells, LoVo cells, LoVo/Doxo cells;
Concentration:
Incubation Time: 72 h
Result: Had an IC50 range of 5.7 μM-11.5 μM in human tumor cell lines.

Cell Cytotoxicity Assay[5]

Cell Line: L02 cells, A-549 cells, HeLa cells, QGY-7701 cells, SW480 cells , SGC7901 cells, MDA-MB-231 cells
Concentration:
Incubation Time: 48 h
Result: Had significant inhibitory activity against a variety of cancer cells (such as SGC7901: IC₅₀=7.59 μM; HeLa: IC₅₀=9.09 μM) and had low toxicity to normal liver cells L02 (IC₅₀>300 μM).
Ranged in IC₅₀ values of cells after treatment: 7.59-20.34 μM.

Apoptosis Analysis[1][2]

Cell Line: HOS Cells, 143B Cells, HL-60 cells
Concentration: 0.5 μM, 1 μM, 2 μM for HOS Cells and 143B Cells 8 μM for HL-60 cells
Incubation Time: 24 h, 48 h for HOS Cells and 143B Cells; 72 h for HL-60 cells
Result: Significantly increased Caspase-3 enzyme activity.
Reduced the proportion of G1 phase cells from 43.7 % to S phase cells from 34.8 % after 72 hours.
Induced DNA fragmentation in HL-60 cells.
Caused chromatin condensation and apoptotic body formation in HL-60 cells, as observed by electron microscopy.

Cell Invasion Assay[2]

Cell Line: HOS Cells, 143B Cells
Concentration: 1 μM
Incubation Time: 24 h
Result: Significantly reduced the number of cells penetrating the membrane.

Western Blot Analysis[2]

Cell Line: HOS Cells, 143B Cells
Concentration: 0.5 μM, 1 μM, 2 μM
Incubation Time: 24 h, 48 h
Result: Down-regulated COX2, VEGF, CD31 (angiogenesis-related proteins) and up-regulated cleaved PARP/caspase-3 (apoptosis proteins).

Immunofluorescence[3]

Cell Line: Balb/c 3T3 fibroblasts
Concentration: 10 μM
Incubation Time: 24 h
Result: Slightly shortened microfilaments and reduced their density, inhibited microtubule polymerization, and caused the intermediate filament vimentin to reorganize into short fibers and accumulate around the nucleus.
In Vivo

Geiparvarin (Compound 8) (0.5 mg/kg, i.p., every three days for several weeks/daily) inhibits tumor growth and lung metastasis in a 143B/9901 cell xenograft tumor model in nude mice without significant toxicity[2].

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

Animal Model: 143B/9901 cells xenograft tumor model in female nude mice (6 weeks)[2]
Dosage: 0.5 mg/kg
Administration: Intraperitoneal injection (i.p.), every 3 days for several weeks; Intraperitoneal injection (i.p.),every day (for safety assessment)
Result: Significantly reduced the tumor volume and weight of the subcutaneous transplanted tumor model, and increased the apoptotic cells in the tumor tissue.
Inhibited the growth of primary tumors and lung metastasis, and reduced the number and size of lung metastatic nodules.
Increased the weight of mice, and there was no pathological damage to major organs.
Molecular Weight

326.34

Formula

C19H18O5
CAS No.
SMILES

C/C(C(OC(C)1C)=CC1=O)=C\COC2=CC=C(C=CC(O3)=O)C3=C2
Structure Classification
Initial Source
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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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Geiparvarin 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:

Geiparvarin36413-91-9ApoptosisCOXCaspaseMicrotubule/TubulinMonoamine OxidaseCyclooxygenaseMAOOsteosarcomaLung Metastasis143B cells9901 cellsK562 cellsHL-60 cellsHT-1080 cellsA-549 cellsSHSY5Y cellsLoVo/Doxo cellsCEM/Vbl100 cellsBalb/c 3T3 fibroblasts CancerInhibitorinhibitorinhibit

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