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Structure of HO-3867
CAS No.: 1172133-28-6
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The BI-3802 was designed by Boehringer Ingelheim and could be obtained free of charge through the Boehringer Ingelheim open innovation portal opnMe.com, associated with its negative control.
HO-3867 selectively inhibits the phosphorylation and transcription of STAT3. It is an analog of curcumin.
4.5
*For Research Use Only !
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Search for reports by entering the product batch number.
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CAS No. : | 1172133-28-6 |
Formula : | C28H30F2N2O2 |
M.W : | 464.55 |
SMILES Code : | O=C1/C(CN(CC2=CC(C)(C)N(O)C2(C)C)C/C1=C\C3=CC=C(F)C=C3)=C/C4=CC=C(F)C=C4 |
MDL No. : | MFCD28143913 |
InChI Key : | PWZQFTQMMAIRRM-JFMUQQRKSA-N |
Pubchem ID : | 46871899 |
GHS Pictogram: |
![]() ![]() |
Signal Word: | Danger |
Hazard Statements: | H228-H315-H319 |
Precautionary Statements: | P240-P210-P241-P264-P280-P302+P352-P370+P378-P337+P313-P305+P351+P338-P362+P364-P332+P313 |
Class: | 4.1 |
UN#: | 1325 |
Packing Group: | Ⅱ |
Target |
|
In Vitro:
Cell Line
|
Concentration | Treated Time | Description | References |
Leishmania donovani promastigotes | 1-200 µg/ml | 2 hours | HO-3867 induced oxidative stress-mediated apoptosis in L. donovani promastigotes, characterized by altered cell morphology, phosphatidylserine externalization, mitochondrial depolarization, intracellular lipid accumulation, and cell cycle arrest. | PMC8677699 |
Leishmania major promastigotes | 1-200 µg/ml | 2 hours | HO-3867 induced dose-dependent apoptosis in L. major promastigotes. | PMC8677699 |
CHO cells | 10 μM | 24 hours | HO-3867 exhibited minimal toxicity toward normal cells | PMC4286190 |
Ishikawa (IK) cells | 5 µM | 24 hours | Inhibition of EV secretion and EC cell proliferation | PMC11602708 |
A2780 human epithelial ovarian cancer cells | 10 µM | 24 hours | To evaluate the inhibitory effect of HO-3867 on the STAT3 signaling pathway and its impact on cancer cell apoptosis. Results showed that HO-3867 significantly reduced the phosphorylation levels of STAT3 and induced apoptosis in cancer cells. | PMC2847669 |
HSMC human aortic smooth muscle cells | 10 µM | 24 hours | To evaluate the effect of HO-3867 on the viability of noncancerous cells. Results showed that HO-3867 was significantly less toxic to HSMC cells compared to cancer cells. | PMC2847669 |
OVTOKO cells | 5 μM and 10 μM | 24 hours | Treatment with HO-3867 decreased expression of pSTAT3 Tyr705 as well pSTAT3 Ser727, while total STAT3 remained constant. | PMC5812255 |
JHOC cells | 5 μM and 10 μM | 24 hours | Treatment with HO-3867 decreased expression of pSTAT3 Tyr705 as well pSTAT3 Ser727, while total STAT3 remained constant. | PMC5812255 |
A2780 cells | 10 µM | 24 hours | HO-3867 induced G2/M cell-cycle arrest in A2780 cells by modulating cell-cycle regulatory molecules p53, p21, p27, cdk2 and cyclin, and promoted apoptosis by caspase-8 and caspase-3 activation. | PMC2868073 |
SKOV3 cells | 10 µM | 24 hours | HO-3867 significantly inhibited the proliferation of SKOV3 cells and induced apoptosis. | PMC2868073 |
OVCAR3 cells | 10 µM | 24 hours | HO-3867 significantly inhibited the proliferation of OVCAR3 cells and induced apoptosis. | PMC2868073 |
U2OS cells | 2, 4, 8, 16, 32 μM | 24 hours | HO-3867 significantly reduced the viability of U2OS cells and induced apoptosis | PMC9229449 |
HOS cells | 2, 4, 8, 16, 32 μM | 24 hours | HO-3867 significantly reduced the viability of HOS cells and induced apoptosis | PMC9229449 |
MG-63 cells | 2, 4, 8, 16, 32 μM | 24 hours | HO-3867 significantly reduced the viability of MG-63 cells and induced apoptosis | PMC9229449 |
Ishikawa cells | 5 and 10 μM | 24 hours | HO-3867 significantly decreased the expression of pSTAT3 Ser727 while total STAT3 remained constant; cell viability decreased by 50–80% and induced G2/M arrest in 55% of Ishikawa cells at the G2/M cell cycle checkpoint. | PMC4283766 |
Human oral squamous cell carcinoma SCC-9 cells | 0, 2.5, 5, 10, and 20 µM | 24 hours | To evaluate the effect of HO-3867 on SCC-9 cell growth, results showed that HO-3867 effectively suppressed SCC-9 cell growth. | PMC8995445 |
Human oral squamous cell carcinoma HSC-3 cells | 0, 2.5, 5, 10, and 20 µM | 24 hours | To evaluate the effect of HO-3867 on HSC-3 cell growth, results showed that HO-3867 effectively suppressed HSC-3 cell growth. | PMC8995445 |
A195 cells | 10μM | 24-72 hours | HO-3867 significantly suppressed the survival of A195 cells | PMC5338638 |
Ishikawa cells | 5 and 10 μM | 3 and 6 hours | HO-3867 selectively induced G2/M cell-cycle arrest in Ishikawa cells in a dose and time-dependent manner, with the greatest increase in G2/M cell population at 6 hours. | PMC4283766 |
A2780 cells | 10 μM | 3 hours | HO-3867 inhibited STAT3 nuclear translocation | PMC4286190 |
Human pulmonary artery smooth muscle cells | 0.5 μM and 1 μM | 48 and 72 hours | To study the effect of HO-3867 on peroxynitrite-induced cell proliferation, results showed that HO-3867 is capable of scavenging peroxynitrite and inhibiting peroxynitrite-induced smooth muscle cell proliferation. | PMC3747571 |
HUVEC cells | 5 μM and 10 μM | HO-3867 significantly inhibited formation of capillary-like structures and invasion in HUVEC cells. | PMC5812255 | |
Murine macrophages | 100 µg/ml | HO-3867 was completely safe for normal murine macrophages. | PMC8677699 |
In Vivo:
Species
|
Animal Model
|
Administration | Dosage | Frequency | Description | References |
Nude mice | A2780cDDP xenograft model | Oral | 50 or 100 ppm | 28 days | HO-3867 significantly inhibited tumor growth without toxic side effects | PMC4286190 |
C57BL/6 mice | High-fat diet-induced endometrial hyperplasia model | Oral | 2 mg/kg | 8 weeks | Inhibition of high-fat diet-induced endometrial hyperplasia and EV secretion | PMC11602708 |
Rats | Left-heart failure-induced pulmonary hypertension model | Dietary administration | 100 ppm | Continued for 4 weeks | To study the effect of HO-3867 on left-heart failure-induced pulmonary hypertension, results showed that HO-3867 significantly attenuated the increase in pulmonary artery pressure and inhibited vascular remodeling by restoring PTEN activity. | PMC3747571 |
Mice | Orthotopic ovarian cancer model | Oral | 50 and 100ppm | Once daily for 6 weeks | HO-3867 significantly suppressed ovarian tumor growth, angiogenesis, and metastasis | PMC5338638 |
BALB/c Nude mice | Ovarian cancer xenograft model | Oral | 25, 50, 100 ppm | Once daily for 35 days | HO-3867 significantly inhibited the growth of the ovarian xenografted tumors in a dosage-dependent manner without any apparent toxicity. | PMC2868073 |
BALB/c Nude mice | Endometrial cancer xenograft model | Oral | 50 and 100 ppm | Continuous for 4 weeks | HO-3867 significantly inhibited the growth of xenograft endometrial tumors and induced apoptosis in vivo. | PMC4283766 |
Tags: HO-3867 | HO3867 | HO 3867 | STAT | STAT3 inhibitor | Apoptosis | Signal Transducer and Activator of Transcription 3 | cell growth | cell survival | cell differentiation | immune response | SH2 domain | 1172133-28-6
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