ZBP1 PROTAC-1
ZBP1 PROTAC-1 is a Z-DNA-binding protein 1 (ZBP1) PROTAC degrader with a DC50 of 25.69 nM. ZBP1 PROTAC-1 consists of a DNA aptamer that specifically binds to ZBP1 and an E3 enzyme-recruiting moiety. ZBP1 PROTAC-1 combines the specificity and covalent binding ability of DNA aptamers with the PROTAC-mediated degradation function. By degrading ZBP1, ZBP1 PROTAC-1 inhibits the phosphorylation of RIPK3/MLKL to necrotic apoptosis and reduces the levels of proinflammatory cytokines (IL-18, IL-1β, IL-6, TNF-α, IFN-β). ZBP1 PROTAC-1 can be used in the research of viral pneumonia and influenza A H1N1 virus infection.
For research use only. We do not sell to patients.
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All PROTACs Isoforms
More
Biological Activity
|
IL-1β |
IL-6 |
IL-18 |
ZBP1 PROTAC-1 (C-PROTAC) forms stable covalent bonds with nucleophilic amino acid groups on the Zα domain of purified ZBP1, enabling specific labeling of the wild-type protein that is reduced in Zα domain mutants lacking these nucleophilic groups[1].
ZBP1 PROTAC-1 specifically labels purified ZBP1 via its aptamer-guided targeting, showing minimal off-target labeling of purified BSA[1].
ZBP1 PROTAC-1 (12.5-200 nM; 0-48 h) potently and selectively degrades ZBP1 in cells via the proteasome system, with a DC50 of 25.69 nM and a ZBP1 half-life of 17.03 h, showing superior efficacy over non-covalent traditional PROTAC[1].
ZBP1 PROTAC-1 (12.5-200 nM) specifically inhibits ZBP1-mediated necroptotic signaling in CBL0137-treated cells by reducing RIPK3 and MLKL phosphorylation, without impacting apoptosis-related Caspase-8 expression[1].
ZBP1 PROTAC-1 (100 nM) effectively degrades virus-upregulated ZBP1 in H1N1-infected cells, requiring both its aptamer and NASA-VHL ligand modules for activity[1].
ZBP1 PROTAC-1 (100 nM) restores viability of H1N1-infected cells to 95.8%, demonstrating superior therapeutic efficacy over traditional PROTAC[1].
ZBP1 PROTAC-1 (100 nM) effectively restores cellular proliferation and activity in H1N1-infected cells, with superior efficacy over traditional PROTAC[1].
ZBP1 PROTAC-1 (100 nM) suppresses the H1N1-induced inflammatory response in cells by reducing mRNA levels of proinflammatory cytokines IL-18, IL-1β, IL-6, TNF-α, and IFN-β[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:Cells pre-treated with CBL0137 to upregulate ZBP1
-
Concentration:12.5, 25, 50, 100 and 200 nM
-
Incubation Time:0, 3, 6, 12, 24 and 48 h
-
Result:Achieved at least a 3-fold greater reduction in ZBP1 protein levels than a non-covalent traditional PROTAC.
Caused significant ZBP1 reduction after 12 h incubation, with a ZBP1 half-life (t1/2) of 17.03 h.
Revealed a DC50 (half-maximal degradation concentration) of 25.69 nM, substantially lower than the 81.52 nM DC50 of the traditional PROTAC.
Chemical Information
-
SMILES
O=C(CCCCC(N[3'-AAGTGCCATCGTGCGTATCCCTCGCGTCTGCTTGCTC GTCCCAACCCACCACCGCCCGATACGCACCTCACGACHTT-5'])=O)N1C2=C(C3=C(C4=C(C1)C=CC=C4)N(CCOCCOCCOCC(N[C@@H](C(C)(C)C)C(N5C[C@@H](C[C@H]5C(NCC6=CC=C(C7=C(C)N=CS7)C=C6)=O)O)=O)=O)N=N3)C=CC=C2
-
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
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)