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Chemical Structure| 1420290-99-8 Chemical Structure| 1420290-99-8

Structure of HJC0152
CAS No.: 1420290-99-8

Chemical Structure| 1420290-99-8

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HJC0152 inhibits STAT3 promoter activity in MDA-MB-231 cells in a dose-dependent manner.

Synonyms: HJC0152 (hydrochloride)

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Product Details of HJC0152

CAS No. :1420290-99-8
Formula : C15H14Cl3N3O4
M.W : 406.65
SMILES Code : O=C(NC1=CC=C([N+]([O-])=O)C=C1Cl)C2=CC(Cl)=CC=C2OCCN.[H]Cl
Synonyms :
HJC0152 (hydrochloride)
MDL No. :MFCD29770804

Safety of HJC0152

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319
Precautionary Statements:P501-P270-P264-P280-P302+P352-P337+P313-P305+P351+P338-P362+P364-P332+P313-P301+P312+P330

Related Pathways of HJC0152

JAK-STAT

Isoform Comparison

Biological Activity

Target
  • STAT3

In Vitro:

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 Mol Cancer Ther. 2017 Apr;16(4):578-590.
266-6 cells 10 µM 48 hours Inhibited STAT3 activity, rescued p-STAT1 nuclear translocation and enhanced ISG expression Int J Mol Sci. 2024 Aug 19;25(16):9007.

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Nude mice MDA-MB-231 xenograft model Intraperitoneal and oral 7.5 mg/kg (ip), 25 mg/kg (po) Not specified 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.

Protocol

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1 mM

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10 mM

2.46mL

0.49mL

0.25mL

12.30mL

2.46mL

1.23mL

24.59mL

4.92mL

2.46mL

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