2. Cell Cycle/DNA Damage Epigenetics Apoptosis Cytoskeleton
  3. Topoisomerase HDAC Apoptosis Kinesin RAD51
  4. SeSA-HCPT

SeSA-HCPT 是一种具有口服活性的双靶点抑制剂，兼具 Topo I 和 HDAC 抑制活性。SeSA-HCPT 可在前列腺癌细胞中诱导强烈的 DNA 损伤、细胞凋亡 (apoptosis) 及 S 期阻滞。SeSA-HCPT 可抑制癌细胞的增殖与迁移。SeSA-HCPT 可通过抑制 KIF4A-RAD51 信号通路损伤同源重组。SeSA-HCPT 可显著抑制 CRPC 肿瘤生长，且全身毒性极低。

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

SeSA-HCPT

SeSA-HCPT 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

SeSA-HCPT 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 DNA gyrase

查看 HDAC 亚型特异性产品:

查看所有亚型
HDAC HDAC1 HDAC2 HDAC3 HDAC4 HDAC5 HDAC6 HDAC7 HDAC8 HDAC9 HDAC10 HDAC11 HD1 HD2

查看 Kinesin 亚型特异性产品:

查看所有亚型
Kinesin-5/Eg5/KSP Kinesin-6 Kinesin-7/CENP-E Kinesin-12 Kinesin-14 Kinesin-13

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

SeSA-HCPT is an orally active dual-target inhibitor integrating Topo I and HDAC inhibition. SeSA-HCPT induces potent DNA damage, apoptosis, S-phase arrest in prostate cancer cells. SeSA-HCPT inhibits cancer cells proliferation and migration. SeSA-HCPT impairs homologous recombination by
suppressing KIF4A-RAD51 signaling. SeSA-HCPT markedly inhibits CRPC tumor growth with
minimal systemic toxicity[1].

IC50 & Target[1]

Topoisomerase I

 

KIF4A

 

体外研究
(In Vitro)

SeSA-HCPT (48 h) 对 AR 阳性 (LNCaP) 和 AR 阴性 (PC3、DU145) 人前列腺癌细胞表现出更优的选择性细胞毒性，其 IC50 值分别为 0.182、0.198 和 0.175 μM 而对正常人角质形成细胞 HaCaT 的毒性极低 (IC50 =5.17 μM)[1]。
SeSA-HCPT (200 nM; 24-48 h) 可显著诱导人前列腺癌细胞 PC3、DU145 和 LNCaP 发生更高水平的细胞凋亡[1]。
SeSA-HCPT (0.175-5.17 μM; 24 h) 可诱导人前列腺癌细胞 PC3、DU145 和 LNCaP 发生 S 期细胞周期阻滞，对人正常角质形成细胞 HaCaT 无作用，并可上调 PC3 和 DU145 细胞中 Cyclin E 的表达[1]。
SeSA-HCPT (3-10 μM) 在 3 和 5 μM 浓度下抑制 Topo1 介导的 DNA 松弛，且对 Topo1-DNA 复合物的结合亲和力，可增强其阻断 Topo1 催化功能的能力[1]。
SeSA-HCPT (1.25-5 nM) 可抑制 PC3 和 DU145 人前列腺癌细胞中的 HDAC 活性[1]。
SeSA-HCPT (1.25-5 nM) 可在人前列腺癌细胞 PC3 和 DU145 中诱导剂量依赖性的 DNA 损伤：γ-H2AX 水平升高[1]。
SeSA-HCPT (5 nM; 24-48 h) 可显著抑制 PC3 和 DU145 人前列腺癌细胞的增殖及迁移[1]。
SeSA-HCPT (0-50 nM; 24 h) 通过下调 KIF4A 并减少 Rad51 向 DNA 损伤位点的募集，损伤 PC3 和 DU145 人前列腺癌细胞中同源重组介导的 DNA 修复，同时诱导 DNA 损伤反应；且在 0 至 50 nM 范围内可诱导 KIF4A 水平呈剂量依赖性降低[1]。

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

SeSA-HCPT 相关抗体:

Apoptosis Analysis[1]

Cell Line: PC3, DU145, LNCaP cells
Concentration: 200 nM (Annexin V/PI staining); 200 nM (Western blot)
Incubation Time: 48 h (Annexin V/PI staining); 24 h (Western blot)
Result: Induced significantly higher levels of apoptosis.
Increased levels of cleaved caspase-3 and p21 in all three cell lines.

Cell Cycle Analysis[1]

Cell Line: PC3, DU145, LNCaP, HaCaT cells
Concentration: 0.175, 0.182, 0.198, 5.17 μM
Incubation Time: 24 h
Result: Induced significant S-phase arrest in PC3, DU145, and LNCaP cells.
Upregulated Cyclin E expression in PC3 and DU145 cells, with no significant changes in Cyclin A2 or Cyclin B levels.
Did not alter cell cycle distribution in HaCaT cells.

Western Blot Analysis[1]

Cell Line: PC3, DU145 cells
Concentration: 1, 5, 10, 30, 50 nM
Incubation Time: 24 h
Result: Increased γ-H2AX and phosphorylated ATM
(pS1981-ATM) levels at 5 nM.
Reduced KIF4A levels from 1 to 50 nM.
体内研究
(In Vivo)

SeSA-HCPT (20 mg/kg；灌胃；单剂量) 可强效抑制去势抵抗性前列腺癌异种移植物的生长，降低肿瘤细胞增殖能力，诱导 DNA 损伤，且仅表现出极低的全身毒性[1]。

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

Animal Model: BALB/c nude (male, 5-week-old, subcutaneous xenograft of PC3 cells)[1]
Dosage: 20 mg/kg
Administration: I.g.; sigle dose
Result: Reduced tumor weight and growth significantly.
Reduced Ki67-positive cells pronouncedly.
Increased γ-H2AX-positive cells significantly .
Showed no significant body weight difference compared with controls.
Caused no significant alterations in hepatic (ALT, AST, ALP) or renal (BUN, creatinine) parameters.
分子量

1519.37

Formula

C76H76N6O18Se2
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

SeSA-HCPT 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:

SeSA-HCPTTopoisomeraseHDACApoptosisKinesinRAD51Histone deacetylasestopoisomerase IHaCaT cellsKIF4Anormal human keratinocytescastration-resistant prostate cancerprostate cancer cellsPC3DU145LNCaPInhibitorinhibitorinhibit

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：
SeSA-HCPT
目录号：
HY-181694
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