HO-3867

Catalog No.S7501

For research use only.

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. HO-3867 induces apoptosis.

HO-3867 Chemical Structure

CAS No. 1172133-28-6

Selleck's HO-3867 has been cited by 19 publications

Purity & Quality Control

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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. HO-3867 induces apoptosis.
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 (from reference)

Cell Research:

[1]

  • 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.

Animal Research:

[1]

  • Animal Models: Mice bearing ovarian cancer A2780 tumor xenografts
  • Dosages: ~100 ppm
  • Administration: p.o.

Solubility (25°C)

In vitro

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

Chemical Information

Molecular Weight 464.55
Formula

C28H30F2N2O2

CAS No. 1172133-28-6
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1(C=C(C(N1O)(C)C)CN2CC(=CC3=CC=C(C=C3)F)C(=O)C(=CC4=CC=C(C=C4)F)C2)C

In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
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Molarity Calculator

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Tech Support

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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