2. Cell Cycle/DNA Damage MAPK/ERK Pathway GPCR/G Protein Immunology/Inflammation Apoptosis Metabolic Enzyme/Protease
  3. PERK Ras COX PD-1/PD-L1 Apoptosis DNA/RNA Synthesis Mitochondrial Metabolism
  4. DPAP

DPAP 是一种 p-ERK1/2 抑制剂，对 p-ERK1/2 的 IC50 为 7.85 μM。DPAP 可抑制 p-ERK1/2 的表达，并破坏 Ras-ERK 信号通路。DPAP 可抑制神经细胞中 COX-2 的表达。DPAP 损伤 DNA 和线粒体，通过线粒体途径诱导细胞凋亡 (Apoptosis)，并上调 PD-L1。DPAP 抑制黑色素瘤转移与血管生成，使脊髓小胶质细胞和星形胶质细胞失活。DPAP 表现出抗黑色素瘤活性，可与抗 PD-1 单克隆抗体联合作用以改变抗肿瘤效果。DPAP 可用于黑色素瘤的研究。

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

DPAP

DPAP 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

DPAP 相关抗体

Top Publications Citing Use of Products

查看 Ras 亚型特异性产品:

查看所有亚型
K-Ras H-Ras N-Ras Ras

查看 COX 亚型特异性产品:

查看所有亚型
COX COX-1 COX-2 COX-3

查看 DNA/RNA Synthesis 亚型特异性产品:

查看所有亚型
RNASE L DNA Polymerases RNA Polymerases Helicases DNA Ligase

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

DPAP is a p-ERK1/2 inhibitor with an IC50 of 7.85 μM against p-ERK1/2. DPAP inhibits the expression of p-MEK1/2 and disrupts the Ras-ERK signaling pathway. DPAP inhibits the expression of COX-2 in nerve cells. DPAP damages DNA and mitochondria, induces Apoptosis via the mitochondrial pathway, and upregulates PD-L1. DPAP inhibits melanoma metastasis and angiogenesis, and inactivates spinal microglia and astrocytes. DPAP exhibits anti-melanoma activity and can be combined with anti-PD-1 monoclonal antibodies to modify anti-tumor effects. DPAP is applicable for the research of melanoma[1].

IC50 & Target[1]

COX-2

 

体外研究
(In Vitro)

DPAP (2 μM; 72 h) 在 A375 黑色素瘤细胞中的细胞摄取量比 CDDP 高 2.53 倍[1]。
DPAP (72 h) 可抑制黑色素瘤 A375 细胞、小鼠黑色素瘤 B16-F10 细胞及正常肾 HK-2 细胞的增殖，孵育 72 h 后其 IC50 分别为 8.05 μM、5.96 μM 和 35.12 μM，显示出对癌细胞的选择性细胞毒性[1]。
DPAP (1-8 μM; 72 h) 可提高 A375 黑色素瘤细胞中 DNA 结合 Pt 的水平；在 8 μM 作用 72 h 时，可上调 γ-H2AX 的表达，表明存在 DNA 损伤[1]。
DPAP (8 μM; 48 h) 可诱导黑色素瘤 A375 细胞发生 S 期细胞周期阻滞[1]。
DPAP (8 μM; 72 h) 可调控凋亡相关蛋白的表达 (上调 Cyt c 和 Bax，下调 Bcl-2) 并诱导黑色素瘤 A375 细胞发生晚期凋亡[1]。
DPAP (8 μM; 72 h) 可调节黑色素瘤 A375 细胞中 Ras-ERK 信号通路[1]。
DPAP (8 μM; 24 h) 在 HT22 小鼠海马神经元细胞中下调 p-ERK1/2 和 COX-2 的表达，但不改变 NF-L 的表达[1]。

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

DPAP 相关抗体:

Cell Cycle Analysis[1]

Cell Line: A375 cells
Concentration: 8 μM
Incubation Time: 48 h
Result: Arrested A375 cells primarily in the S phase, similar to CDDP, indicating inhibition of DNA synthesis.

Western Blot Analysis[1]

Cell Line: A375 cells
Concentration: 8 μM
Incubation Time: 72 h
Result: Significantly downregulated p-MEK1/2 and p-ERK1/2 expression relative to control cells, while having only slight effects on NRAS, MEK1/2, and ERK1/2 expression.

Western Blot Analysis[1]

Cell Line: HT22 cells
Concentration: 8 μM
Incubation Time: 24 h
Result: Suppressed p-ERK1/2 and COX-2 expression in HT22 cells relative to control cells, and did not affect NF-L expression, unlike CDDP which reduced NF-L levels.
体内研究
(In Vivo)

DPAP (1.5 mg Pt kg-1；静脉注射；每 2 天 1 次；共 15 天) 具有强效的体内抗黑色素瘤活性，可将肿瘤体积降至 PBS 对照组的 26.8%，肿瘤重量降至 PBS 对照组的 8.4%，且未观察到全身毒性，同时可有效抑制 Ras-ERK 通路与血管生成[1]。
DPAP (1.5 mg Pt kg−1；静脉注射；每 2 天 1 次；持续 1 周) 可抑制荷黑色素瘤小鼠脊髓背角中小胶质细胞和星形胶质细胞的活化，显示出减轻癌痛相关中枢敏化的潜力[1]。
DPAP (2.5 mg Pt kg-1；静脉注射；每 2 天 1 次；持续 2 周) 联合 anti-PD-1 mAb (12.5 mg kg-1；静脉注射；第 4、9 和 14 天给) 可协同增强抗黑色素瘤效果[1]。
DPAP (10-40 mg kg-1；静脉注射；每 2 天 1 次) 在健康雌性 C57BL/6 小鼠中具有 33.60 mg kg-1 的高半数致死量及良好的生物相容性[1]。

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

Animal Model: C57BL/6 (female, 6−8 weeks old, 18−20 g, subcutaneous inoculation of murine B16−F10 melanoma cells, tumors grown to ~50 mm3)[1]
Dosage: 1.5 mg Pt kg-1
Administration: i.v.; once every 2 days; 15 days
Result: Reduced average tumor weight to 0.10 g, compared to 1.19 g in the PBS control group.
Reduced average tumor volume to 412.11 mm3, compared to 1539.47 mm3 in the PBS control group.
Caused no significant change in mouse body weight relative to the PBS group.
Showed no apparent alterations in heart, liver, spleen, lung, and kidney tissues via histological examination.
Significantly reduced the fluorescence intensity of p-ERK1/2 in tumor tissue.
Significantly weakened the fluorescence intensity of VEGF-A in tumor tissue.
分子量

746.46

Formula

C22H28Cl2N2O10Pt
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

DPAP 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:

DPAPPERKRasCOXPD-1/PD-L1ApoptosisDNA/RNA SynthesisMitochondrial MetabolismProtein kinase R-like endoplasmic reticulum kinasePKR-like endoplasmic reticulum kinaseCyclooxygenasePD-1/Programmed death-ligand 1Ras-ERK signaling pathwayB16-F10 mouse melanoma cellsCOX-2HT22 mouse hippocampal neuron cellsmelanomaA375 human melanoma cellsp-MEK1/2HUVECsp-ERK1/2ERK2Inhibitorinhibitorinhibit

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：
DPAP
目录号：
HY-182899
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