2. Apoptosis Cell Cycle/DNA Damage
  3. MDM-2/p53 Topoisomerase Bcl-2 Family Caspase Cyclin G-associated Kinase (GAK)
  4. ZM484

ZM484 是一种强效的 p53-MDM2/TOP1 双重抑制剂，在体内和体外均表现出抗增殖和抗肿瘤活性。ZM484 通过释放 CPT 和一种有效的 p53-MDM2 抑制剂，有效上调 p53 和 MDM2 蛋白并维持 TOP1 抑制活性。ZM484 通过调控关键细胞凋亡 (apoptosis) 和细胞周期相关蛋白 (包括 caspase-3、 Bcl-2 和 Cyclin B1) 的表达来诱导细胞周期阻滞和凋亡。ZM484 可用于结直肠癌的相关研究。

MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

ZM484

ZM484 Chemical Structure

1.  客户无需承担相应的运输费用。

2.  同一机构（单位）同一产品试用装仅限申领一次，同一机构（单位）一年内

     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户。

规格 是否有货
50 mg   询价  
100 mg   询价  
250 mg   询价  

* Please select Quantity before adding items.

Customer Review

ZM484 相关抗体

Top Publications Citing Use of Products

查看 Topoisomerase 亚型特异性产品:

查看所有亚型
Topoisomerase Topo I Topo II

查看 Bcl-2 Family 亚型特异性产品:

查看所有亚型
Bcl-2 Bcl-xL Bcl-W Mcl-1 Bfl-1 Bcl-B Bax Bak Bim BNIP3

查看 Caspase 亚型特异性产品:

查看所有亚型
Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

ZM484 is a potent dual p53-MDM2/TOP1 inhibitor that exhibits antiproliferative and antitumor activity both in vitro and in vivo. ZM484 effectively upregulates p53 and MDM2 proteins and maintains TOP1 inhibitory activity by the release of camptothecin (CPT) and a potent p53-MDM2 inhibitor. ZM484 induces cell cycle arrest and apoptosis by regulating the expression of key apoptosis- and cycle-related proteins, including caspase-3, Bcl-2, and Cyclin B1. ZM484 can be used for colorectal cancer research[1].

体外研究
(In Vitro)

ZM484 (72 小时) 对三种癌细胞系 HCT116、 SJSA-1 和 A549 表现出强效的抗增殖活性，IC50 值分别为 0.03、0.97 和 0.11 μM[1]。
ZM484 (1.56-50 μM，72 小时) 对非癌性 MRC-5 细胞系表现出极小的细胞毒性[1]。 ZM484 (3.125-100 μM，30 分钟) 在 100 μM 浓度下未表现出溶血活性[1]。 ZM484 (50 μM，0-24 小时) 在 24 小时内浓度保持率超过 95 %，即使在 pH 值为 2 或 5 的酸性缓冲溶液中也表现出优异的稳定性[1]。
ZM484 (25-100 nM，8 天) 显著降低 HCT116 细胞的集落形成能力[1]。
ZM484 (0.195-200 μM，15 分钟) 以浓度依赖性方式抑制 TOP1 活性，在低至 0.195 μM的浓度下仍能保持效力[1]。
ZM484 (50-100 nM，4 小时) 以浓度依赖性方式上调 p53 和 MDM2 蛋白水平[1]。
ZM484 (10-40 nM，24 小时) 有效诱导 HCT116 细胞周期阻滞在 S 期和 G2 期[1]。
ZM484 (10-640 nM，48 小时) 在癌细胞中表现出强效的、浓度依赖性的促凋亡作用，同时伴随 caspase-3、Bcl-2 表达水平的剂量依赖性降低[1]。

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

ZM484 相关抗体:

Cell Cytotoxicity Assay[1]

Cell Line: HCT116 cells
Concentration: 25, 50, and 100 nM
Incubation Time: 8 days
Result: Significantly reduced the colony formation ability of HCT116 cells at concentrations of 25, 50, and 100 nM.

Western Blot Analysis[1]

Cell Line: HCT116 cells
Concentration: 50 and 100 nM
Incubation Time: 4 h
Result: Increased p53 and MDM2 protein levels in a concentration-dependent manner.
Exhibited more activity than Idasanutlin (HY-15676) at 50 and 100 nM for p53 protein upregulation.

Cell Cycle Analysis[1]

Cell Line: HCT116 cells
Concentration: 10 and 40 nM
Incubation Time: 24 h
Result: Induced a dose-dependent increase in the S phase (29.8 % and 43.3 % at 10 and 40 nM, respectively) and G2 phase (20.9 % and 28.3 %) cell populations.

Apoptosis Analysis[1]

Cell Line: HCT116 cells
Concentration: 40, 160, and 640 nM
Incubation Time: 48 h
Result: Induced significant apoptosis in a concentration-dependent manner, with apoptotic rates of 11.6 %, 16.8 %, and 25.8 % at concentrations of 40, 160, and 640 nM, respectively.
Induced apoptosis more effectively than Idasanutlin or the vehicle control.
Decreased the expression levels of caspase-3, Bcl-2 in a dose-dependent manner.
体内研究
(In Vivo)

ZM484 (10 mg/kg，腹腔注射，每隔一天一次，持续 12 天) 在 HCT116 异种移植模型中表现出显著肿瘤生长抑制作用[1]。

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

Animal Model: Female BALB/c nude mice (4-6 weeks) subcutaneously injected with HCT116 cells[1]
Dosage: 10 mg/kg
Administration: i.p., every other day for 12 days
Result: Exhibited the highest tumor growth inhibition (TGI of 81.07 %) among the tested groups, surpassing the positive controls Idasanutlin (25 mg/kg, i.g., qd, TGI = 68.59 %) and Irinotecan (HY-16562) (50 mg/kg, i.p., qw, TGI = 64.01 %).
分子量

1374.35

Formula

C67H72Cl2F2N6O15S2
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

ZM484 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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:

ZM484ZM 484ZM-484MDM-2/p53TopoisomeraseBcl-2 FamilyCaspaseCyclin G-associated Kinase (GAK)Auxilin 2p53MDM2TOP1antiproliferativeantitumorcell cycle arrestCPTapoptosiscaspase-3Bcl-2Cyclin B1colorectal cancerHCT116SJSA-1A549HCT116 xenograft modelInhibitorinhibitorinhibit

您最近查看的产品:

Your information is safe with us. * Required Fields.

   产品名称：

  

* 需求量：

* 客户姓名：

 

* Email：

* 电话：

 

* 公司或机构名称：

   留言给我们：

Bulk Inquiry

Inquiry Information

产品名称：
ZM484
目录号：
HY-178036
需求量：

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

   产品名称：

  

* Lot #：

* 客户姓名：

 

* Email：

   电话：

 

* 部门：

* 公司或机构名称：

 

   留言给我们：

Request for HNMR Report

We have received your request and will respond to you as soon as possible.

嗨！很高兴为您提供帮助！

尊敬的 MCE 客户您好，
请您选择所在区域，我们将转接对应客服为您服务！

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z

热 A B C F G H J L N Q S T X Y Z