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  4. GRPR antagonist-1

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.

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GRPR antagonist-1 Chemical Structure

GRPR antagonist-1 Chemical Structure

CAS No. : 3052544-28-9

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GRPR antagonist-1 Related Antibodies

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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].

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

GRPR antagonist-1 Related Antibodies

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
CAS No.
SMILES

CC(C)(OC(N1CCN(CC1)C([C@H](CC2=CNC3=C2C=CC=C3)NC(CC4=CC=C(C=C4)C(F)(F)F)=O)=O)=O)C
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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GRPR antagonist-1 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

GRPR antagonist-13052544-28-9GRPR antagonist1GRPR antagonist 1OthersGRPRPd176252AnticancerHistone deacetylaseHGC-27HDAC inhibitorInhibitorinhibitorinhibit

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