1. Apoptosis Cell Cycle/DNA Damage
  2. MDM-2/p53 DNA/RNA Synthesis Apoptosis
  3. p53 Activator 2

p53 Activator 2 (compound 10ah) 嵌入 DNA 并导致显着的 DNA 双链断裂。p53 Activator 2 增加 p53、p-p53、CDK4、p21 的表达,导致细胞周期停滞在 G2/M 期。p53 Activator 2 诱导细胞凋亡并显着下调抗凋亡蛋白 Bcl-2、Bcl-xL 和 cyclin B1。p53 Activator 2 对 MGC-803 细胞具有抗增殖活性,IC50 为 1.73 µM。p53 Activator 2 对 MGC-803 异种移植肿瘤模型显示出有效的抗癌作用。

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p53 Activator 2 Chemical Structure

p53 Activator 2 Chemical Structure

CAS No. : 2338764-89-7

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

p53 Activator 2 (compound 10ah) intercalats into DNA and results in significant DNA double-strand break.p53 Activator 2 increases the expression of p53, p-p53, CDK4, p21 to cause cell cycle arrest at G2/M phase.p53 Activator 2 induce apoptosis and significantly down-regulates the anti-apoptosis proteins Bcl-2, Bcl-xL and the levels of cyclin B1.p53 Activator 2 has anti-proliferation activity against MGC-803 cells, with an IC50 of 1.73 µM. p53 Activator 2 displays potent anticancer efficiency against MGC-803 xenograft tumors models[1].

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
A549 IC50
5.48 μM
Compound: 10ah
Cytotoxicity against human A549 cells expressing wild type p53 assessed as reduction in cell viability preincubated for 48 hrs and measured after 4 hrs by MTT assay
Cytotoxicity against human A549 cells expressing wild type p53 assessed as reduction in cell viability preincubated for 48 hrs and measured after 4 hrs by MTT assay
[PMID: 31761381]
DU-145 IC50
4.15 μM
Compound: 10ah
Cytotoxicity against human DU145 cells expressing mutant type p53 assessed as reduction in cell viability preincubated for 48 hrs and measured after 4 hrs by MTT assay
Cytotoxicity against human DU145 cells expressing mutant type p53 assessed as reduction in cell viability preincubated for 48 hrs and measured after 4 hrs by MTT assay
[PMID: 31761381]
L02 IC50
7.46 μM
Compound: 10ah
Cytotoxicity against human HL-7702 cells expressing wild type p53 assessed as reduction in cell viability preincubated for 48 hrs and measured after 4 hrs by MTT assay
Cytotoxicity against human HL-7702 cells expressing wild type p53 assessed as reduction in cell viability preincubated for 48 hrs and measured after 4 hrs by MTT assay
[PMID: 31761381]
MGC-803 IC50
1.73 μM
Compound: 10ah
Cytotoxicity against human MGC-803 cells expressing mutant type p53 assessed as reduction in cell viability preincubated for 48 hrs and measured after 4 hrs by MTT assay
Cytotoxicity against human MGC-803 cells expressing mutant type p53 assessed as reduction in cell viability preincubated for 48 hrs and measured after 4 hrs by MTT assay
[PMID: 31761381]
PC-3 IC50
4.53 μM
Compound: 10ah
Cytotoxicity against human PC-3 cells assessed as reduction in cell viability preincubated for 48 hrs and measured after 4 hrs by MTT assay
Cytotoxicity against human PC-3 cells assessed as reduction in cell viability preincubated for 48 hrs and measured after 4 hrs by MTT assay
[PMID: 31761381]
T-24 IC50
1.79 μM
Compound: 10ah
Cytotoxicity against human T-24 cells expressing wild type p53 assessed as reduction in cell viability preincubated for 48 hrs and measured after 4 hrs by MTT assay
Cytotoxicity against human T-24 cells expressing wild type p53 assessed as reduction in cell viability preincubated for 48 hrs and measured after 4 hrs by MTT assay
[PMID: 31761381]
分子量

363.41

Formula

C20H21N5O2

CAS 号
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.

纯度 & 产品资料
参考文献
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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.

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产品名称:
p53 Activator 2
目录号:
HY-146095
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