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CAS No. 1172133-28-6
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.
Selleck's HO-3867 has been cited by 13 publications
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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.
Inhibition of Stat3 activity on autophagy and hepatic IRI. (A) Pathological analyses showing that inhibition of Stat3 activity increased histopathologic injury in livers subjected to IRI treatment (×200). Scale bars=20μm. And quantified IR-induced liver injury by measuring Suzuki's score. (B) Levels of serum AST and ALT were increased when Stat3 activity was inhibited. (C) Quantitative analysis using TUNEL showing that inhibition of Stat3 activity increased hepatic apoptosis. (D) Immunohistochemistry showing that Cleaved caspase-3 expression increased when Stat3 was inhibited (magnification × 200). Scale bars=20μm. (E) Western blot analysis showing that ATG5 expression was decreased while Bax increased when the expression of p-stat3 (Tyr705) was decreased. (F) Quantitative analysis using transmission electron microscopy (TEM) showing that the number of autophagosomes per cross-sectioned cell were significantly decreased when Stat3 was inhibited. Each data point represents mean±standard deviation of three independent experiments. ***P < 0.001 vs 2h group.
J Cell Biochem, 2018, 119(4):3440-3450. HO-3867 purchased from Selleck.
Interleukin (IL)-22-mediated protection against sodium nitroprussiate (SNP)-induced apoptosis in fibroblast-like synoviocytes established from rheumatoid arthritis (RA) patients (RA-FLS) is mediated by upregulation of the anti-apoptotic proteins Bcl2 and Bcl-xL. Cells were pretreated with HO-3867 (10 lmol/L) or STA21 (25 lmol/L) 2 h before the addition of IL-22 (100 ng/mL). Cells were then cultured for 30 min prior to the addition of SNP (1.33 mmol/L) and incubation for an additional 24 h. a. Western blot analysis of Bcl-2 protein expression in RA-FLS. A representative Western blot is shown in the left panel. Expression of Bcl-2 was quantified by densitometric analysis (right panel). Data represent the mean SD of three independent experiments. b. Western blot analysis of Bcl-xL in RA-FLS. A representative Western blot is shown in the left panel. Expression of Bcl-xL was quantified by densitometric analysis (right panel). Data represent the mean SD of three independent experiments. Each value is expressed as the ratio of the measured protein level to that of b-actin. *P < 0.05, #P > 0.05 versus control, &P < 0.05 versus SNP, %P < 0.05 versus SNP+ IL-22.
Int J Rheum Dis, 2017, 20(2):214-224. HO-3867 purchased from Selleck.
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Choose Selective STAT Inhibitors
|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.|
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. 
|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.  HO-3867 sensitizes cisplatin-resistant ovarian carcinoma through STAT3 inhibition.  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. |
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