2. PROTAC Metabolic Enzyme/Protease Immunology/Inflammation NF-κB Cell Cycle/DNA Damage
  3. PROTACs Reactive Oxygen Species (ROS) CDK
  4. ZnPc-PEG2-VH032

ZnPc-PEG2-VH032 是一种依赖于 VHL 途径的光降解靶向嵌合体 (PDTAC) 和细胞毒性剂。ZnPc-PEG2-VH032 (HY-120217) 结合 VHL 配体结构域，随后在光照条件下特异性降解 VHL，且该过程不依赖于非特异性 ROS 介导的蛋白质损伤。ZnPc-PEG2-VH032 以 Zinc phthalocyanine (HY-19204) 作为光敏剂，在 680 nm LED 光照下可通过 I 型与 II 型光动力途径产生 ROS，一方面通过 ROS 靶向降解已结合的 VHL 蛋白，另一方面直接发挥光动力细胞毒性。同时 VHL 的降解可下调 CDK2/4 的磷酸化水平，诱导肿瘤细胞周期阻滞，进一步增强肿瘤细胞对 ROS 氧化损伤的敏感性，实现协同抗肿瘤效应。ZnPc-PEG2-VH032 在非肌层浸润性膀胱癌 (NMIBC) 原位小鼠模型中发挥了显著体内效力。
(粉色: Reactive Oxygen Species (ROS) 配体 (HY-19204)；蓝色: VHL 配体 (HY-120217)；黑色: )。

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ZnPc-PEG2-VH032

ZnPc-PEG2-VH032 Chemical Structure

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ZnPc-PEG2-VH032 相关抗体

Top Publications Citing Use of Products

查看 PROTACs 亚型特异性产品:

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

查看 CDK 亚型特异性产品:

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CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85 CDK10 CDK15 CDK17 CDK18 CDK20 PITSLRE

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

ZnPc-PEG2-VH032 is a VHL-pathway-dependent photodegradation targeting chimera (PDTAC) and cytotoxic agent. ZnPc-PEG2-VH032 (HY-120217) binds to the VHL ligand domain, and then specifically degrades VHL under light irradiation, a process independent of non-specific ROS-mediated protein damage. ZnPc-PEG2-VH032 uses Zinc phthalocyanine (HY-19204) as a photosensitizer, and generates ROS via type I and type II photodynamic pathways under 680 nm LED irradiation. On one hand, it targets and degrades the bound VHL protein through ROS; on the other hand, it exerts direct photodynamic cytotoxicity. Meanwhile, the degradation of VHL downregulates the phosphorylation level of CDK2/4, induces cell cycle arrest in tumor cells, further enhances the sensitivity of tumor cells to oxidative damage caused by ROS, and achieves a synergistic anti-tumor effect. ZnPc-PEG2-VH032 exerts significant in vivo efficacy in an orthotopic mouse model of non-muscle invasive bladder cancer (NMIBC)[1]. (Pink: Reactive Oxygen Species (ROS) ligand (HY-19204); Blue: VHL ligand (HY-120217); Black: ).

IC50 & Target[1]

VHL

 

CDK2

 

体外研究
(In Vitro)

ZnPc-PEG2-VH032 以高亲和力结合 VHL 蛋白，与特定残基形成氢键，并与周围其他残基相互作用以稳定复合物[1]。

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

ZnPc-PEG2-VH032 相关抗体:
体内研究
(In Vivo)

ZnPc-PEG2-VH032 (0.625 mg/kg；膀胱灌注；第 1、3、5、8、10 天；随后给予 680 nm LED 光照) 在 C57BL/6 小鼠中对原位非肌层浸润性膀胱癌 (NMIBC) 表现出光激活的体内抗肿瘤功效，其活性与 Mitomycin C (MMC) (HY-13316) 相当[1]。

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

Animal Model: C57BL/6 mice (female, 16-20 g weight, orthotopic non-muscle-invasive bladder cancer model via mCherry-MB-49 bladder carcinoma cell implantation with silver nitrate etching)[1]
Dosage: 0.625 mg/kg
Administration: bladder instillation; days 1, 3, 5, 8, 10; followed by 10 minutes of 680 nm LED light exposure (12 J/cm2) 2 hours post-administration
Result: Showed no antitumor activity under non-illuminated conditions (bladder mCherry fluorescence intensity similar to PBS control).
Reduced bladder mCherry fluorescence intensity to nearly absent levels under light-treated conditions, matching efficacy of positive control mitomycin C.
Achieved near-complete elimination of tumor structures in the bladder while preserving normal bladder tissue architecture.
Maintained stable mouse body weights throughout the treatment cycle.
分子量

1285.74

Formula

C68H61N13O8SZn
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

ZnPc-PEG2-VH032 相关分类

  • 摩尔计算器

  • 稀释计算器

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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:

ZnPc-PEG2-VH032PROTACsReactive Oxygen Species (ROS)CDKCyclin dependent kinaseperitumoral tissueorthotopic NMIBCphotodynamic therapyC57BL/6 micenormal cellscancer cellsnon-muscle-invasive bladder cancerVHLROSVHL proteinInhibitorinhibitorinhibit

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