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Cat. No.: HY-181920

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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)).

For research use only. We do not sell to patients.

Formula: C₄₉H₅₂N₈O₁₀S₂
Molecular Weight:977.11

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

RPG-01-132 Chemical Structure

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- Cellular Effect
- In Vitro
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
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Biological Activity

Description

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^[1]. (Pink: Dengue Virus ligand (HY-121663); Blue: Cereblon E3 ligase ligand; Black: linker (HY-130481)).

All PROTACs Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
Huh-7.5	DC₅₀	2.4 μM	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.	41667458
Huh-7.5	EC₅₀	0.47 μM	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.	41667458
Huh-7.5	DC₅₀	3 μM	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.	41667458
Huh-7.5	DC₅₀	1.85 μM	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.	41667458
Huh-7.5	EC₅₀	1 μM	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.	41667458
Huh-7.5	EC₅₀	0.58 μM	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.	41667458

In Vitro

RPG-01-132 (0.04-20 μM; 24 h) induces CRL4^CRBN-dependent degradation of the DENV2 C protein in wild-type Huh7.5 cells, with a DC₅₀ of 2.4 μM and a maximum degradation rate of 84%^[1].
RPG-01-132 (0.04-20 μM; 24 h) inhibits the replication of DENV2 NGC in wild-type Huh7.5 cells via CRL4^CRBN-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 CRL4_CRBN-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 CRL4_CRBN-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].
RPG-01-132 (0.156-0.625 μM; 24 h) reverses the DENV2 C protein-mediated inhibition of the IFN-β promoter in HEK293 cells, and this effect is dependent on the targeted degradation of the C protein^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis^[1]

Cell Line:

DENV2 New Guinea C (NGC)-infected wild-type Huh7.5 cells
Concentration:

0.04, 0.08, 0.16, 0.31, 0.62, 1.25, 2.5, 5, 10, 20 μM
Incubation Time:

24 h
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.

Western Blot Analysis^[1]

Cell Line:

Huh7.5 cells infected with DENV2 16681 wild-type or C-S34L mutant virus
Concentration:

0.04, 0.08, 0.16, 0.31, 0.62, 1.25, 2.5, 5, 10, 20 μM
Incubation Time:

24 h
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

Molecular Weight 977.11
Formula C₄₉H₅₂N₈O₁₀S₂
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
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

Handling Instructions (2659 KB)

References

[1]. Chakravarty A, et al. Degraders of the dengue virus capsid protein exhibit differentiated pharmacology relative to capsid inhibitors. Nature communications. 2026 Feb 10;17(1):2594. [Content Brief]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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