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GRPR antagonist-1 

Cat. No.: HY-115974
Handling Instructions

GRPR antagonist-1 is a potent gastrin releasing peptide receptor (GRPR) antagonist, having the cytotoxicity against certain cancer cells (IC50 of 4.97, 4.36 and 3.40 μM in PC3, Pan02 and HGC-27 cells, respectively). GRPR antagonist-1 inhibits HGC-27 cell viability by decreasing the Bcl-2 level and increasing the Bax level, causing apoptosis. Anticancer activity.

For research use only. We do not sell to patients.

GRPR antagonist-1 Chemical Structure

GRPR antagonist-1 Chemical Structure

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Description

GRPR antagonist-1 is a potent gastrin releasing peptide receptor (GRPR) antagonist, having the cytotoxicity against certain cancer cells (IC50 of 4.97, 4.36 and 3.40 μM in PC3, Pan02 and HGC-27 cells, respectively). GRPR antagonist-1 inhibits HGC-27 cell viability by decreasing the Bcl-2 level and increasing the Bax level, causing apoptosis. Anticancer activity[1].

IC50 & Target

IC50: 4.97 μM (GRPR) in PC3, 4.36 μM (GRPR) in Pan02, 3.40 μM (GRPR) in HGC-27[1]

In Vitro

GRPR antagonist-1 (compound 5a) (0.032-100 μM; 48 hours) has the cytotoxicity against certain cancer cells, also reduces PC3, Pan02, HGC-27, and HepG2 cell viability combined with HDAC inhibitor (1 μM)[1].
GRPR antagonist-1 (1, 2, 8 μM; 24 hours) increases the rate of late apoptosis/necrosis, inducing apoptosis of HGC-27 cells[1].
GRPR antagonist-1 (0.8, 4 μM; 24 hours) inhibits HGC-27 cell viability by decreasing the Bcl-2 level and increasing the Bax level, causing apoptosis[1].

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

Cell Proliferation Assay

Cell Line: PC3, HepG2, HGC-27, Pan02, and HK2 cells[1]
Concentration: 0.032-100 μM
Incubation Time: 48 hours
Result: Showed the cytotoxicity against these cancer cells, also reduced PC3, Pan02, HGC-27, and HepG2 cell viability combined with HDAC inhibitor (1 μM).

Apoptosis Analysis

Cell Line: HGC-27[1]
Concentration: 1, 2, 8 μM
Incubation Time: 24 hours
Result: Increased the rate of late apoptosis/necrosis, inducing apoptosis of HGC-27 cells.

Western Blot Analysis

Cell Line: HGC-27[1]
Concentration: 0.8, 4 μM
Incubation Time: 24 hours
Result: Inhibited HGC-27 cell viability by decreasing the Bcl-2 level and increasing the Bax level, causing apoptosis.
Molecular Weight

558.59

Formula

C29H33F3N4O4

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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GRPR antagonist-1
Cat. No.:
HY-115974
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