GRPR antagonist-1

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

GRPR antagonist-1 

GRPR antagonist-1 是一种有效的胃泌素释放肽受体 (GRPR) 拮抗剂，对某些癌细胞具有细胞毒性 (在PC3、Pan02、HGC-27 细胞中的 IC50 分别是 4.97、4.36、3.40 μM)。GRPR antagonist-1 通过降低 Bcl-2 水平、增加 Bax 水平，来抑制 HGC-27 细胞活力，引起细胞凋亡。具有抗癌活性。

GRPR antagonist-1

GRPR antagonist-1 Chemical Structure

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生物活性

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]
体外研究
(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].

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 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.

分子量

558.59

Formula

C29H33F3N4O4
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.
参考文献

  • [1]. Yu, Mj., et al. Structure–activity relationship studies on Pd176252 derivatives leading to discovery of novel GRP receptor antagonist with potent anticancer activity. Med Chem Res 30, 2069–2089 (2021).

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