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

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).
(Pink: Reactive Oxygen Species (ROS) ligand (HY-19204); Blue: VHL ligand (HY-120217); Black: linker).

For research use only. We do not sell to patients.

ZnPc-PEG2-VH032

ZnPc-PEG2-VH032 Chemical Structure

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ZnPc-PEG2-VH032 Related Antibodies

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

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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

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Description

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: linker).

IC50 & Target[1]

VHL

 

CDK2

 

In Vitro

ZnPc-PEG2-VH032 binds with high affinity to VHL protein, forming hydrogen bonds with specific residues and interacting with additional surrounding residues to stabilize the complex[1].

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

ZnPc-PEG2-VH032 Related Antibodies
In Vivo

ZnPc-PEG2-VH032 (0.625 mg/kg; bladder instillation; days 1, 3, 5, 8, 10; followed by 680 nm LED light exposure) exhibits light-activated in vivo antitumor efficacy against orthotopic NMIBC in C57BL/6 mice, with activity comparable to the Mitomycin C (MMC) (HY-13316)[1].

MedChemExpress (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.
Molecular Weight

1285.74

Formula

C68H61N13O8SZn
SMILES

O=C(NCCOCCOCCC(N[C@@H](C(C)(C)C)C(N1C[C@H](O)C[C@H]1C(NCC2=CC=C(C3=C(C)N=CS3)C=C2)=O)=O)=O)C(C=C4)=CC=C4OC5=CC=C6C7=NC8=C9C(C=CC=C9)=C%10[N-]8[Zn+2]%11([N]7=C(C6=C5)N=C%12C%13=CC=CC=C%14%13)[N-]%12C%14=NC(C%15=CC=CC=C%16%15)=[N]%11C%16=N%10
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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ZnPc-PEG2-VH032 Related Classifications

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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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