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.
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)
All PROTACs Isoforms
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Biological Activity
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ZBP1 25.69 nM (DC50) |
ZBP1 Covalent PROTAC-1 (C-PROTAC) forms stable covalent bonds with nucleophilic groups on the wild-type ZBP1 Zα domain, resulting in efficient labeling, which is significantly reduced in mutant ZBP1G12C Zα domains with altered nucleophilic residues[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 greater efficacy than traditional PROTAC[1].
ZBP1 Covalent PROTAC-1 (C-PROTAC) (100 nM) mediates ZBP1 degradation in unspecified cells via a proteasome-dependent pathway, as degradation is blocked by the proteasome inhibitor MG132[1].
ZBP1 Covalent PROTAC-1 (C-PROTAC) (12.5-200 nM) inhibits the ZBP1-dependent necroptotic pathway in unspecified cells by reducing phosphorylation of RIPK3 and MLKL, without affecting Caspase-8 expression related to apoptosis[1].
ZBP1 Covalent PROTAC-1 (C-PROTAC) (100 nM) degrades virus-induced ZBP1, restores cell viability to 95.8%, and significantly reduces proinflammatory cytokine expression in H1N1 influenza virus-infected cells[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.
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 (278 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)