HO-3867

Catalog No.S7501 Batch:S750101

Technical Data

Formula

C₂₈H₃₀F₂N₂O₂

Molecular Weight

464.55

CAS No.

1172133-28-6

Solubility (25°C)*

In vitro

DMSO

13 mg/mL (27.98 mM)

Ethanol

6 mg/mL (12.91 mM)

Water

Insoluble

In vivo (Add solvents to the product individually and in order)

Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O	0.65mg/ml	Taking the 1 mL working solution as an example, add 50 μL of 13 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil	0.33mg/ml	Taking the 1 mL working solution as an example, add 50 μL of 6.6 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

* <1 mg/ml means slightly soluble or 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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 Assay:^{^[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 Study:^{^[1]}	Animal Models Mice bearing ovarian cancer A2780 tumor xenografts Dosages ~100 ppm Administration p.o.

Cell Assay:^{^[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 Study:^{^[1]}

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

References

Customer Product Validation

: Data from [Data independently produced by , , Liver Transpl, 2016, 22(12):1697-1709]

: Data from [Data independently produced by , , PLOS ONE, 2016, 11(3): e0152120.]

: Data from [Data independently produced by , , J Cell Biochem, 2018, 119(4):3440-3450]

: Data from [Data independently produced by , , Int J Rheum Dis, 2017, 20(2):214-224]

Selleck's HO-3867 has been cited by 24 publications

Role of IL-6/STAT3 Axis in Resistance to Cisplatin in Gastric Cancers [ Biomedicines, 2023, 11(3)694]	PubMed: 36979673
Curcumin Analog, HO-3867, Induces Both Apoptosis and Ferroptosis via Multiple Mechanisms in NSCLC Cells with Wild-Type p53 [ Evid Based Complement Alternat Med, 2023, 2023:8378581]	PubMed: 36814470
The regulation of T helper cell polarization by the diterpenoid fraction of Rhododendron molle based on the JAK/STAT signaling pathway [ Front Pharmacol, 2022, 13:1039441]	PubMed: 36386123
The regulation of T helper cell polarization by the diterpenoid fraction of Rhododendron molle based on the JAK/STAT signaling pathway [ Front Pharmacol, 2022, 13:1039441]	PubMed: 36386123
Establishment and characterization of immortalized sweat gland myoepithelial cells [ Sci Rep, 2022, 12(1):7]	PubMed: 34997030
Tumor Environment Promotes Lnc57Rik-Mediated Suppressive Function of Myeloid-Derived Suppressor Cells [ J Immunol, 2022, 209(7):1401-1413]	PubMed: 36038289
IL-27 signalling promotes adipocyte thermogenesis and energy expenditure [ Nature, 2021, 600(7888):314-318]	PubMed: 34819664
Gene deficiency or pharmacological inhibition of PDCD4-mediated FGR signaling protects against acute kidney injury [ Acta Pharm Sin B, 2021, 11(2):394-405]	PubMed: 33643819
Surfactant protein A modulates the activities of the JAK/STAT pathway in suppressing Th1 and Th17 polarization in murine OVA-induced allergic asthma [ Lab Invest, 2021, 10.1038/s41374-021-00618-1]	PubMed: 34108631
Targeting oncogenic mutations in colorectal cancer using cryptotanshinone [ PLoS One, 2021, 16(2):e0247190]	PubMed: 33596259

RETURN POLICY
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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.