2. Vitamin D Related/Nuclear Receptor MAPK/ERK Pathway Apoptosis Metabolic Enzyme/Protease Neuronal Signaling Membrane Transporter/Ion Channel Immunology/Inflammation NF-κB
  3. Androgen Receptor p38 MAPK Caspase Cytochrome P450 Calcium Channel Reactive Oxygen Species (ROS) Apoptosis Mitochondrial Metabolism GLUT
  4. PeS-9

PeS-9 是一种雄激素受体 (AR) 降解剂，可诱导雄激素受体降解。PeS-9 通过促进细胞毒性 ROS 产生，诱导线粒体和内质网应激，导致线粒体细胞色素 C 和 AIF 释放。PeS-9 可激活 caspase-9 和 caspase-3，引起 DNA 片段化和细胞凋亡 (apoptosis)。PeS-9 具有抗前列腺癌活性，并在体内表现出抗肿瘤和抗转移活性，且副作用较小。PeS-9 可用于 GLUT-1 过表达肿瘤的研究。

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PeS-9

PeS-9 Chemical Structure

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PeS-9 相关抗体

Top Publications Citing Use of Products

查看 p38 MAPK 亚型特异性产品:

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p38 MAPK p38α p38β MAPK13 p38δ p38γ

查看 Caspase 亚型特异性产品:

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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 Cytochrome P450 亚型特异性产品:

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CYP1 CYP2 CYP3 CYP4 CYP11 CYP17 Aromatase/CYP19A1 CYP26 CYP51 CYP1A2 CYP2D6 CYP2C9 CYP2C19 CYP3A4 CYP17A1

查看 Calcium Channel 亚型特异性产品:

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N-type calcium channel L-type calcium channel P/Q-type calcium channel T-type calcium channel Calcium Channel

查看 GLUT 亚型特异性产品:

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GLUT1 GLUT2 GLUT3 GLUT4

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PeS-9 is an Androgen Receptor (AR) degrader that induces androgen receptor degradation PeS-9 induces mitochondrial and ER stress by promoting cytotoxic ROS production, leading to the release of mitochondrial cytochrome C and AIF. PeS-9 subsequently activates caspases-9 and -3, causing DNA fragmentation and apoptotic cell death. PeS-9 has anticancer activity against prostate cancer and exerts in vivo antitumor and antimetastatic activity with minor side effects. PeS-9 can be used for the study of targeting monotherapy against GLUT-1-overexpressing tumors[1].
体外研究
(In Vitro)

PeS-9 (48 h) 在癌细胞中显示出细胞毒性，IC50 分别为 0.49 μM (DU145) 和 0.58 μM (LNCaP)，而在非癌细胞中细胞毒性较低，IC50 分别为 3.41 μM (PNT2)、3.53 μM (MRC-9)、11.7 μM (HUVEC) 和 7.51 μM (HEK)[1]。

PeS-9 (0-2.5 μM, 4-48 h) 下调 22Rv1 细胞中的 AR 信号通路，产生 ROS，并导致 DNA 损伤[1]。

PeS-9 (48 h) 与抗雄激素药物 Enzalutamide (HY-70002) 和 PARP 抑制剂 Olaparib (HY-10162) 在前列腺癌细胞中具有协同作用，CI ＜ 0.75[1]。

PeS-9 (0-1 μM, 1 h) 通过提高 22Rv1 细胞中应激激酶 p-p38、p-JNK 和 p-ERK 的水平来激活 MAPK 信号通路，此效应可被 MAPK 抑制剂拮抗[1]。

PeS-9 (0-2.5 μM, 1-48 h) 通过靶向线粒体和诱导 ROS 产生诱导 22Rv1 细胞凋亡[1]。

PeS-9 (0-2.5 μM, 1-48 h) 使细胞质 Ca2+ 水平升高、内质网 (ER) 扩张、线粒体膜通透性改变以及 DNA 损伤 (通过升高的 sub-G1 细胞群进行量化)[1]。

PeS-9 (0.5-4 μM, 24 h) 抑制 22Rv1 细胞的葡萄糖摄取，这一效应可被 GLUT-1 抑制剂 Phloretin (HY-N0142) 抑制[1]。

PeS-9 (0.1-10 μM, every 5 days over 20 days) 剂量依赖性降低肿瘤类器官的存活分数[1]。

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

PeS-9 相关抗体:

Western Blot Analysis[1]

Cell Line: 22Rv1 cells
Concentration: 1, 2 μM
Incubation Time: 48 h
Result: Downregulated AR-FL, AR-V7, PSA, IGF-1 proteins dose-dependently.

Real Time qPCR[1]

Cell Line: 22Rv1 cells
Concentration: 0, 0.5, 1, 2 μM
Incubation Time: 48 h
Result: Inhibited the transcription of TMPRSS2, FKBP5 and PSA genes dose-dependently.

Immunofluorescence[1]

Cell Line: 22Rv1 cells
Concentration: 1.25, 2.5 μM
Incubation Time: 4, 24 h,48h
Result: Induced DNA double-strand breaks (DSBs), as demonstrated by γH2AX/53BP1 foci formation Triggered primary DNA damage within 4 hours of treatment, reached peak damage levels at 24 hours, and showed signs of DNA repair activation by 48 hours.

Western Blot Analysis[1]

Cell Line: 22Rv1 cells
Concentration: 0.5-4 μM
Incubation Time: 48 h
Result: Increased Bax/Bcl-2 ratio (0.5, 1, 2, 4, 8 μM).
Downregulated of antiapoptotic surviving-survivin (1, 2 μM).
Released cytotoxic mitochondrial proteins such as apoptosis-inducing factor (AIF) and cytochrome C to cellular cytoplasm (2, 4 μM).
Increased the level of caspase-9, caspase-3 and PRAP (2, 4 μM).
体内研究
(In Vivo)

PeS-9 (27.9 mg/kg, i.p., 每天给药持续 15 天) 在 22RV1 皮下移植瘤 NSG 小鼠中具有体内抗肿瘤和抗转移活性，且副作用较小[1]。

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

Animal Model: NOD/SCID gamma (NSG) 8-12 weeks mice bearing subcutaneously xenotransplanted human prostate cancer 22Rv1 cells[1].
Dosage: 27.9 mg/kg
Administration: Daily i.p. administration for 15 days
Result: Reduced 40.0% tumor volume compared with the control group (1069.5 mm3 vs. 646.6 mm3).
Reduced 4.4-fold lung micrometastases.
Showed no significant difference on the weights of the body, heart, lungs, liver, and kidney.
Enlarged spleen that indicate an immunostimulatory effect of the treatment.
Showed no significant difference on the white and red blood cells, platelets, hemoglobin content, and hematocrit.
Revealed no signs of tissue damage, inflammation or granuloma.
分子量

580.56

Formula

C26H28O13S
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

PeS-9 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 *
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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:

PeS-9PeS9PeS 9Androgen Receptorp38 MAPKCaspaseCytochrome P450Calcium ChannelReactive Oxygen Species (ROS)ApoptosisMitochondrial MetabolismGLUTCYPsCa2+ channelsCa channelsGlucose transporterMAPK22Rv1 cellscancerInhibitorinhibitorinhibit

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