PROTAC HBeAg degrader-1
PROTAC HBeAg degrader-1 is a HBeAg-targeting PROTAC degrader that recruits VHL. PROTAC HBeAg degrader-1 degrades HBeAg and reduces HBcAg levels in a largely VHL-independent manner, and inhibits secreted HBeAg in a concentration-dependent manner, with particularly stronger inhibitory activity against the HAP-resistant (HBVT109I mutation) strain. PROTAC HBeAg degrader-1 can be used in studies related to hepatitis B virus infection.
(Pink: HBeAg ligand (HY-174857); Blue: VHL ligand (HY-125845); Black: linker).
For research use only. We do not sell to patients.
- Formula: C48H57ClFN9O7S2
- Molecular Weight:990.60
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All PROTACs Isoforms
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Biological Activity
Description
IC50 & Target
[1]|
HBeAg |
HBcAg |
In Vitro
PROTAC HBeAg degrader-1 (compound LH-3) (10 μM; 24 h) reduces the level of total non-secretory HiBiT-tagged HBeAg in HEK293T HiBiT-HBeAg-NS cells to less than 30% of that in the DMSO control group[1].
PROTAC HBeAg degrader-1 (20 μM; 24 h) reduces the level of secreted HiBiT-tagged HBeAg in HEK293T HiBiT-HBeAg-S cells to < 7% of that in the DMSO control group, and decreases the level of intracellular HiBiT-tagged HBeAg to 46% of that in the DMSO control group[1].
PROTAC HBeAg degrader-1 (10 μM; 24 h) reduces secreted and intracellular HiBiT-tagged HBeAg in HEK293T HiBiT-HBeAg-S and HEK293T VHL KO HiBiT-HBeAg-S cells, indicating that this degradation is largely independent of VHL[1].
PROTAC HBeAg degrader-1 (10 μM; 24 h) reduces secreted HiBiT-tagged HBeAg to 8% of the DMSO control level and intracellular HiBiT-tagged HBeAg to 44% of the DMSO control level in HEK293T HiBiT-HBeAg-S cells, and this activity depends on the key motif in the VH032 domain[1].
PROTAC HBeAg degrader-1 (10 μM; 24 h) reduces secreted HiBiT-tagged HBeAg to 9% of the DMSO control level and intracellular HiBiT-tagged HBeAg to 45% of the DMSO control level in HEK293T HiBiT-HBeAg-S cells[1].
PROTAC HBeAg degrader-1 (10 μM; 6 days) reduces the level of HBcAg (p21) in HBV-expressing HepAD38 cells[1].
PROTAC HBeAg degrader-1 (10 μM; 24 h) reduces the level of secreted HBeAg in wild-type HBV-transfected Huh7 cells to approximately 8% of that in untreated cells, and reduces the level of this protein in HBVT109I mutant-transfected Huh7 cells to approximately 11.5% of that in untreated cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HepAD38 HBV-expressing cells
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Concentration:10 μM
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Incubation Time:6 days
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Result:Caused a strong reduction in HBcAg (p21) levels relative to DMSO control.
Chemical Information
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Molecular Weight 990.60
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Formula C48H57ClFN9O7S2
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SMILES
O=C(C1=C(CN2CCN(C(CCCCC(N[C@@H](C(C)(C)C)C(N3[C@H](C(NCC4=CC=C(C5=C(C)N=CS5)C=C4)=O)C[C@@H](O)C3)=O)=O)=O)CC2)NC(C6=NC=CS6)=N[C@H]1C7=CC=C(F)C=C7Cl)OC
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Shipping
Room temperature in continental US; may vary elsewhere.
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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)