RPG-01-132
RPG-01-132 is a PROTAC degrader targeting the DENV capsid protein, with a DC50 of 2.4 μM. RPG-01-132 blocks viral assembly, eliminates viral particles, and interferes with the non-structural functions of the capsid protein. RPG-01-132 exhibits significant antiviral activity against all four DENV serotypes and the ST148 (HY-121663)-resistant DENV2 mutant strain. RPG-01-132 can be applied in studies related to dengue virus infection.
(Pink: Dengue Virus ligand (HY-121663); Blue: Cereblon E3 ligase ligand; Black: linker (HY-130481)).
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- Formule: C49H52N8O10S2
- Masse moléculaire:977.11
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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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Activité biologique
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Chemical Information
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- Pureté et documentation
- Références
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Activité biologique
Description
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Huh-7.5 | DC50 |
2.4 μM
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Reduction of intracellular DENV2 C protein abundance in wild-type Huh7.5 cells infected with DENV2 NGC, measured via Western blot after 24 h of treatment.
Reduction of intracellular DENV2 C protein abundance in wild-type Huh7.5 cells infected with DENV2 NGC, measured via Western blot after 24 h of treatment.
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41667458 |
| Huh-7.5 | EC50 |
0.47 μM
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Reduction of infectious DENV2 NGC progeny virus titer in wild-type Huh7.5 cells, measured via plaque assay after 24 h of treatment.
Reduction of infectious DENV2 NGC progeny virus titer in wild-type Huh7.5 cells, measured via plaque assay after 24 h of treatment.
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41667458 |
| Huh-7.5 | DC50 |
3 μM
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Reduction of intracellular wild-type DENV2 16681 C protein abundance in wild-type Huh7.5 cells, measured via Western blot after 24 h of treatment.
Reduction of intracellular wild-type DENV2 16681 C protein abundance in wild-type Huh7.5 cells, measured via Western blot after 24 h of treatment.
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41667458 |
| Huh-7.5 | DC50 |
1.85 μM
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Reduction of intracellular DENV2 16681 C-S34L mutant C protein abundance in wild-type Huh7.5 cells, measured via Western blot after 24 h of treatment.
Reduction of intracellular DENV2 16681 C-S34L mutant C protein abundance in wild-type Huh7.5 cells, measured via Western blot after 24 h of treatment.
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41667458 |
| Huh-7.5 | EC50 |
1 μM
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Reduction of infectious wild-type DENV2 16681 progeny virus titer in wild-type Huh7.5 cells, measured via plaque assay after 24 h of treatment.
Reduction of infectious wild-type DENV2 16681 progeny virus titer in wild-type Huh7.5 cells, measured via plaque assay after 24 h of treatment.
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41667458 |
| Huh-7.5 | EC50 |
0.58 μM
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Reduction of infectious DENV2 16681 C-S34L mutant progeny virus titer in wild-type Huh7.5 cells, measured via plaque assay after 24 h of treatment.
Reduction of infectious DENV2 16681 C-S34L mutant progeny virus titer in wild-type Huh7.5 cells, measured via plaque assay after 24 h of treatment.
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41667458 |
In Vitro
RPG-01-132 (0.04-20 μM; 24 h) inhibits the replication of DENV2 NGC in wild-type Huh7.5 cells via CRL4CRBN-dependent C protein degradation, with an EC50 of 0.47 μM[1].
RPG-01-132 (4 h) can form a functional ternary complex with DENV2 C and CRBN in HEK293 cells, thereby mediating the proteasome-dependent degradation of C[1].
RPG-01-132 (30 μM; 24 h) blocks the assembly of DENV2 virions in Huh7.5 cells, exhibiting a unique phenotype compared to the parental inhibitor ST148[1].
RPG-01-132 (10 μM; 24 h) exhibits CRL4CRBN-dependent broad-spectrum antiviral activity in Huh7.5 cells, and is active against all four DENV serotypes[1].
RPG-01-132 (0.04-20 μM; 24 h) retains CRL4CRBN-dependent C protein degradation activity in Huh7.5 cells, and exhibits antiviral activity against the ST148-resistant DENV2 16681 C-S34L mutant, with potency comparable to that of wild-type DENV2[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:DENV2 New Guinea C (NGC)-infected wild-type Huh7.5 cells
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Concentration:0.04, 0.08, 0.16, 0.31, 0.62, 1.25, 2.5, 5, 10, 20 μM
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Incubation Time:24 h
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Result:Caused concentration-dependent depletion of intracellular DENV2 C protein, with a DC50 of 2.4 μM and a maximum degradation of 84%.
Lost degradation activity in CRBN-knockout Huh7.5 cells.
Had degradation activity blocked by the neddylation inhibitor MLN4924.
Showed no degradation activity with the CRBN-binding-deficient negative control RPG-01-132-BUMP.
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Cell Line:Huh7.5 cells infected with DENV2 16681 wild-type or C-S34L mutant virus
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Concentration:0.04, 0.08, 0.16, 0.31, 0.62, 1.25, 2.5, 5, 10, 20 μM
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Incubation Time:24 h
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Result:Exhibited comparable degradation activity against wild-type and C-S34L mutant C protein, with DC50 values of 3 μM (wild-type) and 1.85 μM (C-S34L).
Showed comparable antiviral activity against both viruses, with EC50 values of 1 μM (wild-type) and 0.58 μM (C-S34L).
Showed retained activity compared to ST148, which had no detectable antiviral activity against the C-S34L mutant.
Chemical Information
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Masse moléculaire 977.11
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Formule C49H52N8O10S2
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SMILES
O=C(C1=C(N)C2=CC(CCCCC3)=C3N=C2S1)NC4=NN=C(C5=CC=C(C#CCOCCOCCOCCOCCC(NCCCC6=CC=CC(C(N7C(CC8)C(NC8=O)=O)=O)=C6C7=O)=O)C=C5)S4
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
RPG-01-132 Related Classifications
HY-181920 Related Classifications
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