HO-3867 - ≥98% , CAS No.1172133-28-6
In stock
SKU
H413764
STAT3 Selective Inhibitors | Activators
Information
HO-3867, an analog of curcumin, is a selectiveSTAT3inhibitor that inhibits its phosphorylation, transcription, and DNA binding without affecting the expression of other active STATs. HO-3867 inducesapoptosis.
Targets
STAT3
In vitro
HO-3867 produces significant cytotoxicity in A2780 and other tested ovarian cancer cell lines, with less toxic to noncancerous ovarian surface epithelial cells. HO-3867 induces G(2)-M cell cycle arrest in A2780 cells and promotes apoptosis by caspase-8 and caspase-3 activation. HO-3867 blocks the JAK/STAT3 pathway in human ovarian cancer cell lines.
In vivo
HO-3867 (100 ppm p.o.) inhibits the growth of ovarian cancer xenograft tumor in mice without any apparent signs of toxicity, and also results in inhibition of pSTAT3 as well as downregulation of the STAT3-targeting proteins. HO-3867 sensitizes cisplatin-resistant ovarian carcinoma through STAT3 inhibition. HO-3867 (100 ppm p.o.) also attenuates left-heart-failure-induced pulmonary hypertension by decreasing oxidative stress and increasing PTEN expression in the lung of rats.
Cell Research(from reference)
Cell lines：A2780 (A2780R), PA-1, SKOV3, OV4, and OVCAR3 cells; human ovarian surface epithelial cell
Concentrations：~20 μM
Incubation Time：24 hours
More Information
| CAS | 1172133-28-6 |
|---|---|
| Synonyms | 1-[(2,5-dihydro-1-hydroxy-2,2,5,5-tetramethyl-1H-pyrrol-3-yl)methyl]-3,5-bis[(4-fluorophenyl)methylene]-(3E,5E)-4-piperidinone |
| Specifications & Purity | ≥98% |
| Storage | Store at -20°C |
| Shipped In | Ice chest + Ice pads |
| Product Description | Information HO-3867, an analog of curcumin, is a selectiveSTAT3inhibitor that inhibits its phosphorylation, transcription, and DNA binding without affecting the expression of other active STATs. HO-3867 inducesapoptosis. Targets STAT3 In vitro HO-3867 produces significant cytotoxicity in A2780 and other tested ovarian cancer cell lines, with less toxic to noncancerous ovarian surface epithelial cells. HO-3867 induces G(2)-M cell cycle arrest in A2780 cells and promotes apoptosis by caspase-8 and caspase-3 activation. HO-3867 blocks the JAK/STAT3 pathway in human ovarian cancer cell lines. In vivo HO-3867 (100 ppm p.o.) inhibits the growth of ovarian cancer xenograft tumor in mice without any apparent signs of toxicity, and also results in inhibition of pSTAT3 as well as downregulation of the STAT3-targeting proteins. HO-3867 sensitizes cisplatin-resistant ovarian carcinoma through STAT3 inhibition. HO-3867 (100 ppm p.o.) also attenuates left-heart-failure-induced pulmonary hypertension by decreasing oxidative stress and increasing PTEN expression in the lung of rats. Cell Research(from reference) Cell lines：A2780 (A2780R), PA-1, SKOV3, OV4, and OVCAR3 cells; human ovarian surface epithelial cell Concentrations：~20 μM Incubation Time：24 hours |
| Pubchem Sid | 504770827 |
| Pubchem Sid Url | https://pubchem.ncbi.nlm.nih.gov/substance/504770827 |
| Solubility | Solubility (25°C) In vitro DMSO: 13 mg/mL warmed with 50ºC Water: bath (27.98 mM); Ethanol: 6 mg/mL warmed with 50ºC Water: bath (12.91 mM); Water: Insoluble; |
| PubChem CID | 46871899 |
| Molecular Formula | C28H30F2N2O2 |
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