HO-3867

Catalog No.S7501

HO-3867 Chemical Structure

Molecular Weight(MW): 464.55

HO-3867, an analog of curcumin, is a selective STAT3 inhibitor that inhibits its phosphorylation, transcription, and DNA binding without affecting the expression of other active STATs.

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2 Customer Reviews

  • Cell apoptosis as measured by TUNEL. Representative sections as determined at 12 hours after reperfusion (3100 magnification). Apoptotic nuclei were stained red, and the software of Image J was used to analyse quantity of TUNEL-positive cells in the livers. Scale bars5100 lm. *P<0.05, **P<0.01, ***P<0.001 compared with IR group.

    Liver Transpl, 2016, 22(12):1697-1709. HO-3867 purchased from Selleck.

    The inhibitory effect of IL-6/IL-6R on TRPM7 currents is blocked by the STAT3 inhibitor HO-3867, but not by the inhibitor MAPK signaling pathway. (A) Relative currents normalized to TRPM7 currents recorded during perfusion with divalent-free extracellular solution. The specific STAT3 inhibitor HO-3867 did not inhibit TRPM7 inward currents at -100 mV, but blocked the effect of IL-6/sIL-6R (n = 3, * p < 0.05 vs. control, # p < 0.05 vs. IL-6/sIL-6R). (B) The specific MAPK−MEK inhibitor PD98059, did not inhibit TRPM7 inward currents at -100 mV, and did not block the effect of IL-6/sIL-6R (n = 3, * p < 0.05 vs. control). All currents were normalized to controls at -100 mV.

    PLOS ONE, 2016, 11(3): e0152120.. HO-3867 purchased from Selleck.

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Biological Activity

Description HO-3867, an analog of curcumin, is a selective STAT3 inhibitor that inhibits its phosphorylation, transcription, and DNA binding without affecting the expression of other active STATs.
Targets
STAT3 [1]
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. [1]

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. [1] HO-3867 sensitizes cisplatin-resistant ovarian carcinoma through STAT3 inhibition. [2] 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. [3]

Protocol

Cell Research:

[1]

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  • Cell lines: A2780 (A2780R), PA-1, SKOV3, OV4, and OVCAR3 cells; human ovarian surface epithelial cell
  • Concentrations: ~20 μM
  • Incubation Time: 24 hours
  • Method:

    Cell viability is determined 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.


    (Only for Reference)
Animal Research:

[1]

+ Expand
  • Animal Models: Mice bearing ovarian cancer A2780 tumor xenografts
  • Formulation: --
  • Dosages: ~100 ppm
  • Administration: p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 13 mg/mL warmed (27.98 mM)
Ethanol 6 mg/mL warmed (12.91 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 464.55
Formula

C28H30F2N2O2

CAS No. 1172133-28-6
Storage powder
in solvent
Synonyms N/A

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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STAT Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID