Home JAK/STAT STAT inhibitor - Apoptosis related activator HO-3867 For research use only.

HO-3867

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

HO-3867 Chemical Structure

CAS No. 1172133-28-6

Purity & Quality Control

Batch: S750101 DMSO]13 mg/mL]false]Ethanol]6 mg/mL]false]Water]Insoluble]false Purity: 99.89%
99.89

HO-3867 Related Products

Signaling Pathway

STAT Signaling Pathways

STAT Signaling Pathway

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
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]
Cell Research 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.
In Vivo
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]
Animal Research Animal Models Mice bearing ovarian cancer A2780 tumor xenografts
Dosages ~100 ppm
Administration p.o.

Chemical Information & Solubility

Molecular Weight 464.55 Formula

C28H30F2N2O2
CAS No. 1172133-28-6 SDF Download HO-3867 SDF
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
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 13 mg/mL ( (27.98 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 6 mg/mL

Water : Insoluble


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In vivo
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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. )

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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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