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Chemical Structure| 1172133-28-6 Chemical Structure| 1172133-28-6

Structure of HO-3867
CAS No.: 1172133-28-6

Chemical Structure| 1172133-28-6

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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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Product Details of HO-3867

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

Safety of HO-3867

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:

Related Pathways of HO-3867

JAK-STAT

Isoform Comparison

Biological Activity

Target
  • STAT3

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

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.15mL

0.43mL

0.22mL

10.76mL

2.15mL

1.08mL

21.53mL

4.31mL

2.15mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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