HJC0152 markedly suppresses cell growth and triggers apoptosis, which is evident through changes in cell shape at concentrations of 1, 5, and 10 μM. Studies indicate that a 10 μM concentration of HJC0152 reduces STAT3 promoter activity by about 32% in MDA-MB-231 cells, and a higher concentration of 20 μM leads to a further reduction in STAT3 promoter activity by 62% compared to the control group. Additionally, the overall levels of STAT3 diminish following HJC0152 treatment. The compound also promotes the activation of cleaved caspase-3 and the downregulation of cyclin D1 in MDA-MB-231 cells[1].
HJC0152 细胞实验
Cell Line
Concentration
Treated Time
Description
References
Human pulmonary artery endothelial cells (hPAECs)
1 μM
48 hours
To investigate the inhibitory effect of HJC0152 on STAT3 activity and its impact on BMPR2 expression in hPAECs. Results demonstrated that HJC0152 significantly inhibited STAT3 phosphorylation and enhanced SERCA2a-induced BMPR2 expression.
Int J Mol Sci. 2021 Aug 24;22(17):9105.
Human pulmonary artery smooth muscle cells (hPASMCs)
1 μM
48 hours
To evaluate the inhibitory effect of HJC0152 on STAT3 activity and its impact on BMPR2 expression. Results showed that HJC0152 significantly inhibited STAT3 phosphorylation and enhanced SERCA2a-induced BMPR2 expression.
Int J Mol Sci. 2021 Aug 24;22(17):9105.
Panc-1
1.08 μM
Evaluate the inhibitory effect of HJC0152 on the proliferation of Panc-1 cells
ACS Med Chem Lett. 2013 Feb 14;4(2):180-185.
AsPC1
1.9 μM
Evaluate the inhibitory effect of HJC0152 on the proliferation of AsPC1 cells
ACS Med Chem Lett. 2013 Feb 14;4(2):180-185.
MDA-MB-231
1.64 μM
Evaluate the inhibitory effect of HJC0152 on the proliferation of MDA-MB-231 cells
ACS Med Chem Lett. 2013 Feb 14;4(2):180-185.
MCF-7
0.91 μM
Evaluate the inhibitory effect of HJC0152 on the proliferation of MCF-7 cells
ACS Med Chem Lett. 2013 Feb 14;4(2):180-185.
H1299
1.25, 2.5, 5, 10, 20 μmol/L
24, 48, 72 hours
HJC0152 significantly inhibited NSCLC cell proliferation in a concentration- and time-dependent manner. The IC50 values were 5.11 μmol/L (A549), 5.01 μmol/L (H460), and 13.21 μmol/L (H1299).
Cell Prolif. 2020 Mar;53(3):e12777.
H460
1.25, 2.5, 5, 10, 20 μmol/L
24, 48, 72 hours
HJC0152 significantly inhibited NSCLC cell proliferation in a concentration- and time-dependent manner. The IC50 values were 5.11 μmol/L (A549), 5.01 μmol/L (H460), and 13.21 μmol/L (H1299).
Cell Prolif. 2020 Mar;53(3):e12777.
A549
1.25, 2.5, 5, 10, 20 μmol/L
24, 48, 72 hours
HJC0152 significantly inhibited NSCLC cell proliferation in a concentration- and time-dependent manner. The IC50 values were 5.11 μmol/L (A549), 5.01 μmol/L (H460), and 13.21 μmol/L (H1299).
Cell Prolif. 2020 Mar;53(3):e12777.
LN229
0.01, 0.1, 1, 2, 5, 10, 20, 50, or 100 μmol/L
24 hours
HJC0152 inhibited the proliferation of LN229 cells with an IC50 value of 1.749 μM.
Am J Cancer Res. 2019 Apr 1;9(4):699-713.
U251
0.01, 0.1, 1, 2, 5, 10, 20, 50, or 100 μmol/L
24 hours
HJC0152 inhibited the proliferation of U251 cells with an IC50 value of 1.821 μM.
Am J Cancer Res. 2019 Apr 1;9(4):699-713.
U87
0.01, 0.1, 1, 2, 5, 10, 20, 50, or 100 μmol/L
24 hours
HJC0152 inhibited the proliferation of U87 cells with an IC50 value of 5.396 μM.
Am J Cancer Res. 2019 Apr 1;9(4):699-713.
CAL27 cells
1 μM
24 hours
Inhibited cell proliferation, migration, and invasion, induced apoptosis
Mol Cancer Ther. 2017 Apr;16(4):578-590.
SCC25 cells
2 μM
24 hours
Inhibited cell proliferation, migration, and invasion, induced apoptosis
Evaluate the inhibitory effect of HJC0152 on the growth of MDA-MB-231 xenograft tumors in vivo
ACS Med Chem Lett. 2013 Feb 14;4(2):180-185.
BALB/c nude mice
A549 NSCLC xenograft model
Oral
7.5 mg/kg
Once daily for 30 days
HJC0152 significantly inhibited the growth of A549 xenograft tumours, extending the tumour volume doubling time from 2.03 days in the control group to 4.62 days, and significantly reducing tumour weight.
Cell Prolif. 2020 Mar;53(3):e12777.
BALB/c-nu mice
U87 xenograft tumor model
Intratumoral injection
7.5 mg/kg
Daily for 4 weeks
HJC0152 significantly suppressed the growth of U87 xenograft tumors, with both tumor volume and weight significantly reduced, and did not cause significant loss of body weight in mice.
Am J Cancer Res. 2019 Apr 1;9(4):699-713.
BALB/c-nu mice
SCC25-derived orthotopic tumor model
Intraperitoneal injection
7.5 mg/kg
Daily for 28 days
Significantly inhibited tumor growth and invasion
Mol Cancer Ther. 2017 Apr;16(4):578-590.
Rats
Severe PAH model induced by unilateral left pneumonectomy combined with monocrotaline (PNT/MCT)
Intraperitoneal injection
7.5 mg/kg
Single injection, lasting 4 weeks
To evaluate the therapeutic effect of HJC0152 in a severe PAH model. Results showed that HJC0152 significantly reduced mean pulmonary artery pressure (mPAP) and pulmonary vascular resistance (PVR), and improved right ventricular function.
Int J Mol Sci. 2021 Aug 24;22(17):9105.
C57BL/6 mice
CVB3-induced acute pancreatitis and myocarditis model
Intraperitoneal injection
12.5 mg/kg
Once at 1 day before and 1 day after infection
Mitigated viral-induced pancreatitis and myocarditis pathology by increasing IFN-β and ISG expression, reducing viral load in multiple organs
Int J Mol Sci. 2024 Aug 19;25(16):9007.
HJC0152 动物研究
Animal study
In mice, intraperitoneal administration of HJC0152 at a dosage of 7.5 mg/kg results in enhanced tumor growth inhibition. The xenograft tumor growth in mice is considerably curtailed when treated with HJC0152 at 25 mg/kg. Importantly, at a dosage of 75 mg/kg, HJC0152 exhibits no significant toxic effects[1].
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