2. Metabolic Enzyme/Protease Apoptosis Epigenetics Cell Cycle/DNA Damage
  3. Phosphatase Apoptosis Caspase PARP
  4. PFKFB4-IN-1

PFKFB4-IN-1 是一种高效且选择性的 ATP 竞争性 PFKFB4 抑制剂 (IC50 = 4.50 μM)，可降低细胞内 PFKFB4 蛋白水平。PFKFB4-IN-1 对 PFKFB1/4 和 PFKFB3/4 亚型的选择性超过 12 倍。PFKFB4-IN-1 可抑制癌细胞增殖、诱导细胞凋亡 (apoptosis) 并抑制细胞迁移。PFKFB4-IN-1 可抑制 MDA-MB-231 异种移植小鼠模型中肿瘤生长。PFKFB4-IN-1 可用于乳腺癌、肺癌和肝癌的相关研究。

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

我们将采用定制合成服务的方式为您快速提供所需产品和技术服务

PFKFB4-IN-1

PFKFB4-IN-1 Chemical Structure

CAS No. : 2664831-55-2

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

PFKFB4-IN-1 相关抗体

Top Publications Citing Use of Products

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

查看 PARP 亚型特异性产品:

查看所有亚型
PARP PARP1 PARP2 PARP3 PARP4 TNKS1/PARP5A TNKS2/PARP5B PARP7 PARP10 PARP14 PARP15 PARP12 PARP16

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PFKFB4-IN-1 is a potent and selective ATP-competitive PFKFB4 inhibitor (IC50 = 4.50 μM) that reduces intracellular PFKFB4 protein levels. PFKFB4-IN-1 exhibits >12-fold selectivity over PFKFB1/4 and PFKFB3/4. PFKFB4-IN-1 inhibits cancer cell proliferation, induces apoptosis, and inhibits cell migration. PFKFB4-IN-1 inhibits tumor growth in the MDA-MB-231 xenograft mouse model. PFKFB4-IN-1 can be used for breast, lung and liver cancer research[1].

IC50 & Target[1]

PFKFB4

4.50 μM (IC50)

体外研究
(In Vitro)

PFKFB4-IN-1 (compound 2v) (2-100 μM，72 小时) 表现出广谱抗癌活性，对 MCF-7、HepG2 和 A549 细胞的 IC50 值分别为 4.02 μM、11.07 μM 和 11.2 μM，同时对正常人肝细胞 (HL7702，IC50 > 50 μM) 的细胞毒性显著降低[1]。
PFKFB4-IN-1 (0-48 小时) 以时间和浓度依赖的方式抑制 MCF-7 乳腺癌细胞的增殖[1]。
PFKFB4-IN-1 (6-18 μM，24 小时) 抑制 MCF-7 乳腺癌细胞的迁移和克隆形成，并通过 caspase-3 激活和 PARP 裂解途径诱导其凋亡[1]。
PFKFB4-IN-1 (0-25 μM，24 小时) 可抑制 MCF-7 细胞中 PFKFB4 蛋白的表达水平，并抑制糖酵解代谢，显著降低细胞内 ATP 和 NADP+/NADPH 水平[1]。
PFKFB4-IN-1 可稳定结合于 PFKFB4 的 ATP 结合口袋内，并与 Asn168、Gly51 和 Tyr428 残基形成关键的氢键[1]。
PFKFB4-IN-1 不会显著增加 MCF-7 细胞中的活性氧 (ROS) 水平和 DNA 损伤[1]。

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

PFKFB4-IN-1 相关抗体:

Western Blot Analysis[1]

Cell Line: MCF7 cells
Concentration: 6, 12, and 18 μM
Incubation Time: 0, 1, 2, 4, 8 and 24 h
Result: Progressively increased levels of cleaved PARP and cleaved caspase-3.
Did not accelerate PFKFB4 protein degradation in MCF-7 cells.

Cell Migration Assay [1]

Cell Line: MCF7 cells
Concentration: 6, 12, and 18 μM
Incubation Time: 0 and 24 h
Result: Significantly inhibited the migration of MCF-7 cells into the wounded area, with a significant reduction in the number of migrating cells compared to the control group.

Cell Proliferation Assay[1]

Cell Line: MCF7 cells
Concentration: 6, 12, and 18 μM
Incubation Time: 7 days
Result: Markedly inhibited colony formation in MCF-7 cells even at low concentrations.
Completely prevented colony growth at 18 μM.

Apoptosis Analysis[1]

Cell Line: MCF7 cells
Concentration: 6, 12, and 18 μM
Incubation Time: 24 h
Result: Induced apoptosis in a concentration-dependent manner, with the apoptotic rate of MCF-7 cells increasing from 5.61% to 6.55% and 9.68%, respectively.
体内研究
(In Vivo)

PFKFB4-IN-1 (30 mg/kg，腹腔注射，每日一次，连续 14 天) 可抑制 MDA-MB-231 异种移植小鼠模型中的肿瘤生长[1]。
PFKFB4-IN-1 (5 μM，于受精后 24 小时内开始给药并持续暴露 72 小时) 在斑马鱼发育毒性模型中表现出良好的急性安全性[1]。

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

Animal Model: Female BALB/c-nu nude mice subcutaneously injected with MDA-MB-231 cells[1]
Dosage: 30 mg/kg
Administration: i.p., q.d. for 14 days
Result: Exerted a notable inhibitory effect on tumor growth with the tumor growth inhibition (TGI) of 71.9%.
Induced pronounced nuclear shrinkage in tumor tissues, suggesting that its antitumor effect may be attributed to the induction of apoptosis.
Showed no significant body weight fluctuations and no damages in organ tissues.
Animal Model: Zebrafish embryos[1]
Dosage: 5 μM
Administration: a single dose at 24 h post-fertilization for 72 h
Result: Resulted in only negligible embryonic mortality and minimal morphological deformities during the early stages of development.
分子量

318.20

Formula

C11H6N6O6
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

PFKFB4-IN-1 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:

PFKFB4-IN-12664831-55-2PhosphataseApoptosisCaspasePARPpoly ADP ribose polymeraseATP-competitivePFKFB4MDA-MB-231A549MCF-7HepG2breast cancerlung cancerliver cancerzebrafishInhibitorinhibitorinhibit

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：
PFKFB4-IN-1
目录号：
HY-178367
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