ZBP1 Covalent PROTAC-1
ZBP1 Covalent PROTAC-1 is a covalent PROTAC degrader targeting ZBP1, with a DC50 of 25.69 nM. ZBP1 Covalent PROTAC-1 integrates a ZBP1-binding DNA aptamer, a linker containing covalent NASA, and an E3 ligase-recruiting moiety to guide ubiquitin-proteasome system-mediated degradation of ZBP1. ZBP1 Covalent PROTAC-1 exhibits inhibitory activity against necroptosis signaling pathways and inflammatory responses. ZBP1 Covalent PROTAC-1 can be used for research on viral pneumonia.
(Pink: Target protein ligand; Blue: VHL ligand (HY-125845); Black: linker).
For research use only. We do not sell to patients.
- Molecular Weight:24590.00
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Storage:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
[1]|
ZBP1 25.69 nM (DC50) |
In Vitro
ZBP1 Covalent PROTAC-1 (100 nM) significantly restores the proliferative capacity of H1N1 virus-infected cells, indicating that C-PROTAC not only prevents cell death but also promotes the recovery of cellular function[1].
ZBP1 Covalent PROTAC-1 (0-400 nM) exhibits good biocompatibility with no cytotoxicity in unspecified cells[1].
ZBP1 Covalent PROTAC-1 (12.5-200 nM; 0-48 h) potently degrades CBL0137-induced ZBP1 in unspecified cells, with a DC50 of 25.69 nM and a degradation half-life of 17.03 h, exhibiting at least 3-fold higher potency than conventional PROTACs[1].
ZBP1 Covalent PROTAC-1 (C-PROTAC) (100 nM) mediates the degradation of ZBP1 in unspecified cells through a proteasome-dependent pathway, as the proteasome inhibitor MG132 (HY-13259) blocks this degradation process[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Unspecified cell line
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Concentration:100 nM (comparison with traditional PROTAC); 12.5-200 nM (dose-response); 100 nM (time-course)
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Incubation Time:0-48 h (time-course)
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Result:Achieved at least a 3-fold greater reduction in ZBP1 levels than traditional PROTAC.
Induced significant ZBP1 degradation after 12 h, with a degradation half-life of 17.03 h.
Exhibited a DC50 of 25.69 nM, substantially lower than the DC50 of 81.52 nM for traditional PROTAC.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Balb/c healthy mice (6-8 weeks)[1]
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Dosage:1.5 mg/kg
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Administration:once daily; for 5 consecutive days
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Result:Significantly improved the survival rate of H1N1-infected mice: the survival rate in the virus-infected group was only 20%, whereas it increased to 80% in the NLP@C-PROTAC treatment group.
Effectively alleviated weight loss caused by viral infection.
Significantly reduced the lung wet-to-dry weight ratio in H1N1-infected mice.
Significantly reduced the lung index (lung weight/body weight) of H1N1-infected mice.
Significantly improved the pathological appearance of the lungs in H1N1-infected mice.
Significantly reduced the mRNA expression levels of various pro-inflammatory factors—including IL-18, IL-6, IL-1β, TNF-α, and IFN-β—in the lung tissue of H1N1-infected mice.
Significantly reduced inflammatory cell infiltration in the lung tissue of H1N1-infected mice.
Significantly reduced apoptosis in the lung tissue of H1N1-infected mice.
Significantly restored the alveolar space area in H1N1-infected mice.
Chemical Information
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Appearance Solid
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Molecular Weight 24590.00
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Color White to pink
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SMILES
O=C(CCCCC(N(CC#N)S(=O)(C1=CC=C(C=C1)CCS[3'-AAGTGCCATCGTGCGTATCCCTCGCGTCTGCTTGCTC GTCCCAACCCACCACCGCCCGATACGCACCTCACGACTT-5'])=O)=O)N2C3=C(C4=C(C5=C(C2)C=CC=C5)N(CCOCCOCCOCC(N[C@@H](C(C)(C)C)C(N6C[C@@H](C[C@H]6C(NCC7=CC=C(C8=C(C)N=CS8)C=C7)=O)O)=O)=O)N=N4)C=CC=C3
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Purity & Documentation
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Data Sheet (295 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
ZBP1 Covalent PROTAC-1 Related Classifications
HY-177119 Related Classifications
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