HO-3867 is a selective STAT3 inhibitor. HO-3867 blocks the JAK/STAT3 pathway in human ovarian cancer cell lines. HO-3867/cisplatin combination treatment significantly inhibites cisplatin-resistant cell proliferation in a concentration-dependent manner. HO-3867 induces G(2)-M cell cycle arrest in A2780 cells. HO-3867 promotes apoptosis by caspase-8 and caspase-3 activation.
APMIS. 2015 Oct;837-46.
Leukemia inhibitory factor promotes tumor growth and metastasis in human osteosarcoma via activating STAT3.
HO-3867 purchased from AbMole
|Source||APMIS (2015). Figure 4. HO-3867 (Abmole Bioscience, Shanghai, China)|
|Method||The cellular growth, colony formation, and invasion assay|
|Cell Lines||143B cells|
|Incubation Time||24 h|
|Results||In 143B cells, the cellular growth, colony formation, and invasion enhanced by LIF were partially neutralized by HO-3867 (Fig. 4B–D, p = 0.04, 0.016 and 0.05, respectively).|
|Cell lines||A2780 (A2780R), PA-1, SKOV3, OV4, and OVCAR3 cells; human ovarian surface epithelial cell|
|Preparation method||Determining cell viability 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.|
|Incubation time||24 hours|
|Animal models||Mice bearing ovarian cancer A2780 tumor xenografts|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
HO-3867, a curcumin analog, sensitizes cisplatin-resistant ovarian carcinoma, leading to therapeutic synergy through STAT3 inhibition.
Selvendiran K, et al. Cancer Biol Ther. 2011 Nov 1;12(9):837-45. PMID: 21885917.
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