HJC0350 is a potent and specific EPAC2 antagonist with an IC50 of 0.3 µM.
IC50 & Target
IC50: 0.3 µM (EPAC2)[1]
体外研究 (In Vitro)
HJC0350 has an apparent IC50 value of 0.3 µM for competing with 8-NBD-cAMP binding of EPAC2, and is about 133-fold more potent than cAMP. HJC0350 is found not to inhibit EPAC1-mediated Rap1-GDP exchange activity at 25 µM in the presence of equal concentration of cAMP, indicating that it is EPAC2-specific antagonists. Pretreatment of HEK293/EPAC2-FL cells with 10 µM HJC0350 fully blocks the 007-AM induced decrease of FRET[1].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
277.38
Formula
C15H19NO2S
CAS 号
885434-70-8
运输条件
Room temperature in continental US; may vary elsewhere.
[1]. Chen H, et al. Identification and characterization of small molecules as potent and specific EPAC2 antagonists. J Med Chem. 2013 Feb 14;56(3):952-62.
HJC0416 hydrochloride is a potent and orally active STAT3 inhibitor with an enhanced anticancer profile than Stattic (HY-13818). HJC0416 hydrochloride is a promising anti-cancer agent for breast cancer study[1].
IC50 & Target[1]
STAT3
体外研究 (In Vitro)
HJC0416 hydrochloride inhibits the proliferation of both ER-positive, and ER-negative (triple negative) breast cancer cells with IC50 values of 1.76 µM and 1.97 µM, respectively. However, it displays a marked antiproliferative effect against pancreatic cancer cell line AsPC1 and Panc-1 with IC50 values of 40 nM and 1.88 µM, respectively[1].HJC0416 hydrochloride (1-10 µM; 48 hours) inhibits cell growth and induced apoptosis accompanying cellular morphological changes in MDA-MB-231 breast cancer cells[1].HJC0416 hydrochloride (5 µM; 24 hours) decreases the STAT3 promoter activity by approximately 51%, while stattic (HY-13818) only decreases the STAT3 promoter activity by 39% in MDA-MB-231 cells after transient transfecting with pSTAT3-Luc vector[1].HJC0416 hydrochloride (1-10 µM; 12 hours) has a comparable potency in downregulating STAT3 protein production and phosphorylation at Tyr-705 site when compares with Stattic (HY-13818). Additionally, it also induces cleaved caspase-3 and downregulated cyclin D1 levels in MDA-MB-231 cells[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Cycle Analysis[1]
Cell Line:
MDA-MB-231 breast cancer cells
Concentration:
1-10 µM
Incubation Time:
48 hours
Result:
Induced cell apoptosis in cancer cells.
Apoptosis Analysis[1]
Cell Line:
MDA-MB-231 breast cancer cells
Concentration:
1 µM; 5 µM; 10 µM
Incubation Time:
12 hours
Result:
Decreased p-STAT3 phosphorylation expression and cyclin D1 level.
体内研究 (In Vivo)
HJC0416 hydrochloride (intraperitoneal injection; 10 mg/kg; 7 days) shows a 67% decrease of tumor volume as compared to the control mice. Similarly, HJC0416 hydrochloride (oral administration; 100 mg/kg; 14 days) also significantly reduces tumor volume at a dose of 100 mg/kg by 46%. The i.p. route appeared to have a better reduction of tumor volume. It is also noteworthy that HJC0416 does not show significant signs of toxicity at a dose of 100 mg/kg[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model:
Mice with MDA-MB-231 cells[1]
Dosage:
10 mg/kg (i.p.); 100 mg/kg (oral)
Administration:
Intraperitoneal injection, 7 days; oral administration, 14 days
Result:
Exhibited antitumor effects in the MDA-MB-231 triple-negative breast cancer murine xenograft model.
分子量
429.32
Formula
C18H18Cl2N2O4S
CAS 号
2415263-08-8
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
溶解性数据
In Vivo:
1.
All drugs were dissolved in 50% DMSO with 50% polyethylene glycol for in vivo administration[1].
参考文献
[1]. Haijun Chen, et al.Discovery of Potent Anticancer Agent HJC0416, an Orally Bioavailable Small Molecule Inhibitor of Signal Transducer and Activator of Transcription 3 (STAT3). Eur J Med Chem. 2014 Jul 23;82:195-203.
HJC0416 hydrochloride is a potent and orally active STAT3 inhibitor with an enhanced anticancer profile than Stattic (HY-13818). HJC0416 hydrochloride is a promising anti-cancer agent for breast cancer study[1].
IC50 & Target[1]
STAT3
体外研究 (In Vitro)
HJC0416 hydrochloride inhibits the proliferation of both ER-positive, and ER-negative (triple negative) breast cancer cells with IC50 values of 1.76 µM and 1.97 µM, respectively. However, it displays a marked antiproliferative effect against pancreatic cancer cell line AsPC1 and Panc-1 with IC50 values of 40 nM and 1.88 µM, respectively[1].HJC0416 hydrochloride (1-10 µM; 48 hours) inhibits cell growth and induced apoptosis accompanying cellular morphological changes in MDA-MB-231 breast cancer cells[1].HJC0416 hydrochloride (5 µM; 24 hours) decreases the STAT3 promoter activity by approximately 51%, while stattic (HY-13818) only decreases the STAT3 promoter activity by 39% in MDA-MB-231 cells after transient transfecting with pSTAT3-Luc vector[1].HJC0416 hydrochloride (1-10 µM; 12 hours) has a comparable potency in downregulating STAT3 protein production and phosphorylation at Tyr-705 site when compares with Stattic (HY-13818). Additionally, it also induces cleaved caspase-3 and downregulated cyclin D1 levels in MDA-MB-231 cells[1].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Cycle Analysis[1]
Cell Line:
MDA-MB-231 breast cancer cells
Concentration:
1-10 µM
Incubation Time:
48 hours
Result:
Induced cell apoptosis in cancer cells.
Apoptosis Analysis[1]
Cell Line:
MDA-MB-231 breast cancer cells
Concentration:
1 µM; 5 µM; 10 µM
Incubation Time:
12 hours
Result:
Decreased p-STAT3 phosphorylation expression and cyclin D1 level.
体内研究 (In Vivo)
HJC0416 hydrochloride (intraperitoneal injection; 10 mg/kg; 7 days) shows a 67% decrease of tumor volume as compared to the control mice. Similarly, HJC0416 hydrochloride (oral administration; 100 mg/kg; 14 days) also significantly reduces tumor volume at a dose of 100 mg/kg by 46%. The i.p. route appeared to have a better reduction of tumor volume. It is also noteworthy that HJC0416 does not show significant signs of toxicity at a dose of 100 mg/kg[1].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model:
Mice with MDA-MB-231 cells[1]
Dosage:
10 mg/kg (i.p.); 100 mg/kg (oral)
Administration:
Intraperitoneal injection, 7 days; oral administration, 14 days
Result:
Exhibited antitumor effects in the MDA-MB-231 triple-negative breast cancer murine xenograft model.
分子量
429.32
Formula
C18H18Cl2N2O4S
CAS 号
2415263-08-8
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
溶解性数据
In Vivo:
1.
All drugs were dissolved in 50% DMSO with 50% polyethylene glycol for in vivo administration[1].
参考文献
[1]. Haijun Chen, et al.Discovery of Potent Anticancer Agent HJC0416, an Orally Bioavailable Small Molecule Inhibitor of Signal Transducer and Activator of Transcription 3 (STAT3). Eur J Med Chem. 2014 Jul 23;82:195-203.
HJC0416 hydrochloride is a potent and orally active STAT3 inhibitor with an enhanced anticancer profile than Stattic (HY-13818). HJC0416 hydrochloride is a promising anti-cancer agent for breast cancer study[1].
IC50 & Target[1]
STAT3
体外研究 (In Vitro)
HJC0416 hydrochloride inhibits the proliferation of both ER-positive, and ER-negative (triple negative) breast cancer cells with IC50 values of 1.76 µM and 1.97 µM, respectively. However, it displays a marked antiproliferative effect against pancreatic cancer cell line AsPC1 and Panc-1 with IC50 values of 40 nM and 1.88 µM, respectively[1].HJC0416 hydrochloride (1-10 µM; 48 hours) inhibits cell growth and induced apoptosis accompanying cellular morphological changes in MDA-MB-231 breast cancer cells[1].HJC0416 hydrochloride (5 µM; 24 hours) decreases the STAT3 promoter activity by approximately 51%, while stattic (HY-13818) only decreases the STAT3 promoter activity by 39% in MDA-MB-231 cells after transient transfecting with pSTAT3-Luc vector[1].HJC0416 hydrochloride (1-10 µM; 12 hours) has a comparable potency in downregulating STAT3 protein production and phosphorylation at Tyr-705 site when compares with Stattic (HY-13818). Additionally, it also induces cleaved caspase-3 and downregulated cyclin D1 levels in MDA-MB-231 cells[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Cycle Analysis[1]
Cell Line:
MDA-MB-231 breast cancer cells
Concentration:
1-10 µM
Incubation Time:
48 hours
Result:
Induced cell apoptosis in cancer cells.
Apoptosis Analysis[1]
Cell Line:
MDA-MB-231 breast cancer cells
Concentration:
1 µM; 5 µM; 10 µM
Incubation Time:
12 hours
Result:
Decreased p-STAT3 phosphorylation expression and cyclin D1 level.
体内研究 (In Vivo)
HJC0416 hydrochloride (intraperitoneal injection; 10 mg/kg; 7 days) shows a 67% decrease of tumor volume as compared to the control mice. Similarly, HJC0416 hydrochloride (oral administration; 100 mg/kg; 14 days) also significantly reduces tumor volume at a dose of 100 mg/kg by 46%. The i.p. route appeared to have a better reduction of tumor volume. It is also noteworthy that HJC0416 does not show significant signs of toxicity at a dose of 100 mg/kg[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model:
Mice with MDA-MB-231 cells[1]
Dosage:
10 mg/kg (i.p.); 100 mg/kg (oral)
Administration:
Intraperitoneal injection, 7 days; oral administration, 14 days
Result:
Exhibited antitumor effects in the MDA-MB-231 triple-negative breast cancer murine xenograft model.
分子量
429.32
Formula
C18H18Cl2N2O4S
CAS 号
2415263-08-8
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
溶解性数据
In Vivo:
1.
All drugs were dissolved in 50% DMSO with 50% polyethylene glycol for in vivo administration[1].
参考文献
[1]. Haijun Chen, et al.Discovery of Potent Anticancer Agent HJC0416, an Orally Bioavailable Small Molecule Inhibitor of Signal Transducer and Activator of Transcription 3 (STAT3). Eur J Med Chem. 2014 Jul 23;82:195-203.
HJC0197 is a potent Epac1 (exchange protein directly activated by cAMP 1) and Epac2 (IC50=5.9 μM for Epac2) antagonist. HJC0197 selectively blocks cAMP-induced Epac activation. HJC0197 inhibits Epac1-mediated Rap1-GDP exchange activity at 25 μM in the presence of equal concentration of cAMP[1].
体外研究 (In Vitro)
HJC0197 (25 μM) also inhibits Epac1-mediated Rap1-GDP exchange activity at 25 μM in the presence of equal concentration of cAMP[1]
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
339.45
Formula
C19H21N3OS
CAS 号
1383539-73-8
运输条件
Room temperature in continental US; may vary elsewhere.
[1]. Chen H, et al. 5-Cyano-6-oxo-1,6-dihydro-pyrimidines as potent antagonists targeting exchange proteins directly activated by cAMP. Bioorg Med Chem Lett. 2012 Jun 15;22(12):4038-43.
HJC0152 hydrochloride is a signal transducers and activators of transcription 3 (STAT3) inhibitor.
IC50 & Target
STAT3
体外研究 (In Vitro)
HJC0152 hydrochloride (compound 11) significantly inhibits cell proliferation and induces apoptosis accompanying cellular morphological changes at concentrations of 1, 5, and 10 μM. Results show that treatment with 10 μM HJC0152 hydrochloride decreases the STAT3 promoter activity in MDA-MB-231 cells by approximately 32%, and increasing the dose of HJC0152 hydrochloride to 20 μM further decreases STAT3 promoter activity by 62% as compare with control. Total STAT3 is reduced after treatment with HJC0152 hydrochloride. HJC0152 hydrochloride induces cleaved caspase-3 and down regulates cyclin D1 in MDA-MB-231 cells[1].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究 (In Vivo)
Mice treated with 7.5 mg/kg of HJC0152 hydrochloride (compound 11) via ip show a better effect in inhibiting tumor growth. The growth of xenograft tumors in mice is significantly reduced by HJC0152 hydrochloride at a dose of 25 mg/kg. It is also noteworthy that HJC0152 hydrochloride does not show significant signs of toxicity at a dose of 75 mg/kg[1].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
406.65
Formula
C15H14Cl3N3O4
CAS 号
1420290-99-8
运输条件
Room temperature in continental US; may vary elsewhere.
[1]. Chen H, et al. Discovery of O-Alkylamino Tethered Niclosamide Derivatives as Potent and Orally Bioavailable Anticancer Agents. ACS Med Chem Lett. 2013 Feb 14;4(2):180-185.
Cell Assay [1]
Breast cancer MDA-MB-231 cells are incubated in 6-well plates (2.5×105/well). Cells are then treated with DMSO, or HJC0152 hydrochloride (compound 11) at different concentrations for 48 h, and then both adherent and floating cells are collected, washed once with PBS. Resuspended cells are incubated with 100 μL PBS containing 1% BSA and 100 μL Annexin V and dead cell detection reagent at room temperature for 20 min. Apoptosis is measured immediately using the Muse Cell Analyzer with the MuseTM Apoptosis Kit[1].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration [1]
Fifty-four female nude mice are are used for orthotopic tumor studies at 4 to 6 weeks of age. The mice are maintained in a barrier unit with 12 h light-dark switch. Freshly harvested MDA-MB-231 cells (2.5×106 cells per mouse, resuspended in 100 μL PBS) are injected into the 3rd mammary fat pad of the mice, and then randomly assigned into 8 groups (5 to10 mice per group). For the intraperitoneal treatment experiment, the mice are treated daily with 2.5 mg/kg HJC0152 hydrochloride (compound 11) (Group A) or vehicle (Group D) when the tumor volume reaches 200 mm3. A Body weights and tumors volume are measured daily and tumor volume is calculated according to the formula V=0.5×L×W2, where L=length (mm) and W=width (mm)[1].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献
[1]. Chen H, et al. Discovery of O-Alkylamino Tethered Niclosamide Derivatives as Potent and Orally Bioavailable Anticancer Agents. ACS Med Chem Lett. 2013 Feb 14;4(2):180-185.
