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HJ-4 is a Piperine (HY-N0144) derivative. HJ-4 potently inhibits the proliferation of CRC cells by dose-dependently reducing colony formation and DNA synthesis. HJ-4 markedly suppresses the adhesion, migration, invasion and induces apoptosis of CRC cells. HJ-4 demonstrates anti-tumor efficacy in chicken embryo chorioallantoic membrane (CAM) model implanted with HCT116/SW480 tumor spheroids. HJ-4 can be used for the study of colorectal cancer (CRC).

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HJ-4

HJ-4 Chemical Structure

CAS No. : 1313741-00-2

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Description

HJ-4 is a Piperine (HY-N0144) derivative. HJ-4 potently inhibits the proliferation of CRC cells by dose-dependently reducing colony formation and DNA synthesis. HJ-4 markedly suppresses the adhesion, migration, invasion and induces apoptosis of CRC cells. HJ-4 demonstrates anti-tumor efficacy in chicken embryo chorioallantoic membrane (CAM) model implanted with HCT116/SW480 tumor spheroids. HJ-4 can be used for the study of colorectal cancer (CRC)[1].

In Vitro

HJ-4 (3.125-100 μM, 24 h) inhibits viability of CRC cells (HCT116: IC50 = 15.82 μM; SW480: IC50 = 20.46 μM)[1].
HJ-4 (8-32 μM, 48 h) reduces colony number and size of HCT116/SW480 cells[1].
HJ-4 (8-32 μM, 24 h) decreases EdU-positive HCT116/SW480 cells in EdU incorporation assay, dose-dependently inhibiting DNA synthesis[1].
HJ-4 (8-32 μM, 0-48 h) inhibits adhesion, migration, and invasion of HCT116/SW480 cells[1].
HJ-4 (8-32 μM, 24 h) upregulates p53, PUMA, BAX, cleaved caspase-3, cleaved PARP, and downregulates BCL-2, β-catenin, Cyclin D1 in HCT116/SW480 cells[1].
HJ-4 (8-32 μM, 24 h) increases p53/BAX expression in HCT116/SW480 cells, and promotes YO-PRO-1 (early apoptosis) and PI (late apoptosis) positive cells in HCT116 cells via YO-PRO-1/PI staining[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

Cell Line: HCT116/SW480 cells
Concentration: 8, 16, 32 μM
Incubation Time: 24 h
Result: Upregulated p53, PUMA, BAX, cleaved caspase-3, cleaved PARP.
Downregulated BCL-2, β-catenin, Cyclin D1.
In Vivo

HJ-4 (8-32 μM, local application to tumor site, once daily for 7 days) inhibits angiogenesis in chicken embryo chorioallantoic membrane (CAM) model implanted with HCT116/SW480 tumor spheroids[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: HCT116/SW480 colon cancer cell-derived spheroids were implanted into the vascular-rich regions of the chorioallantoic membrane (CAM) of 7-day-old fertilized chicken embryos[1]
Dosage: 8, 16, 32 μM
Administration: local application to tumor site, once daily for 7 days
Result: Reduced tumor weight.
Showed potent anti-angiogenic effects in the CAM model.
Decreased the number of tertiary blood vessels.
Did not cause obvious embryonic toxicity in the CAM model.
Molecular Weight

392.45

Formula

C23H24N2O4

CAS No.
SMILES

COC1=CC=CC=C1N2CCN(CC2)C(/C=C/C=C/C3=CC4=C(OCO4)C=C3)=O

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HJ-4
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HY-178921
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