HO-3867 is a selective STAT3 inhibitor. HO-3867 blocks the JAK/STAT3 pathway in human ovarian cancer cell lines. HO-3867/cisplatin combination treatment significantly inhibites cisplatin-resistant cell proliferation in a concentration-dependent manner. HO-3867 induces G(2)-M cell cycle arrest in A2780 cells. HO-3867 promotes apoptosis by caspase-8 and caspase-3 activation.
APMIS. 2015 Oct;837-46.
Leukemia inhibitory factor promotes tumor growth and metastasis in human osteosarcoma via activating STAT3.
HO-3867 purchased from AbMole
2015 May.
Study on IL-17(A) in Regulating Omentum Metastasis and Drug Resistance of Ovarian Cancer
HO-3867 purchased from AbMole
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Source | APMIS (2015). Figure 4. HO-3867 (Abmole Bioscience, Shanghai, China) |
| Method | The cellular growth, colony formation, and invasion assay | |
| Cell Lines | 143B cells | |
| Concentrations | ||
| Incubation Time | 24 h | |
| Results | In 143B cells, the cellular growth, colony formation, and invasion enhanced by LIF were partially neutralized by HO-3867 (Fig. 4B–D, p = 0.04, 0.016 and 0.05, respectively). |
| Cell Experiment | |
|---|---|
| Cell lines | A2780 (A2780R), PA-1, SKOV3, OV4, and OVCAR3 cells; human ovarian surface epithelial cell |
| Preparation method | Determining cell viability by a colorimetric assay using MTT. In the mitochondria of living cells, yellow MTT undergoes a reductive conversion to formazan, producing a purple color. Cells, grown to ~80% confluence in 75-mm flasks, are trypsinized, counted, seeded in 96-well plates with an average population of 7,000 cells/well, incubated overnight, and then treated with HO-3867 for 24 h. All experiments are done using 8 replicates and repeated at least three times. |
| Concentrations | ~20 μM |
| Incubation time | 24 hours |
| Animal Experiment | |
|---|---|
| Animal models | Mice bearing ovarian cancer A2780 tumor xenografts |
| Formulation | |
| Dosages | ~100 ppm |
| Administration | p.o. |
| Molecular Weight | 464.55 |
| Formula | C28H30F2N2O2 |
| CAS Number | 1172133-28-6 |
| Solubility (25°C) | DMSO |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related STAT Products |
|---|
| STAT3-IN-21, cell-permeable, negative control
STAT3-IN-21, cell-permeable, negative control, a peptide, is a negative control for Stat3 activity detection. |
| STAT3-IN-24, cell-permeable
STAT3-IN-24, cell-permeable (PpYLKTK-mts) is a STAT3 peptide inhibitor. |
| 5-FAM-GpYLPQTV-NH2
5-FAM-GpYLPQTV-NH2 is a fluorescently labeled peptide and has STAT3 inhibitory activity. |
| Ac-GpYLPQTV-NH2
Ac-GpYLPQTV-NH2 is a STAT3 inhibitor with an IC50 value of 0.33 μM. |
| XZH-5
XZH-5 inhibits the phosphorylation of STAT3 and results in the induction of apoptosis and reduction of colony forming ability. |
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