MPD2
MPD2 is a Cereblon (CRBN) ligand and SARS-CoV-2 MPro degrader with an IC50 <1000 nM against SARS-CoV-2 MPro[1]. MPD2 engages CRBN to mediate ubiquitination and proteasomal degradation of SARS-CoV-2 MPro, reducing SARS-CoV-2 MPro protein levels in infected cells. MPD2 inhibits viral replication of various SARS-CoV-2 strains and acts against nirmatrelvir-resistant SARS-CoV-2 viruses. MPD2 can be used for the research of covid-19 and for fighting against drug-resistant viral variants..
(Pink: SARS-CoV‑2 Main Protease ligand (HY-158763); Blue: Cereblon ligand (HY-14658); Black: linker (HY-W275882)).
For research use only. We do not sell to patients.
- Formula: C51H68N6O13
- Molecular Weight:973.12
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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
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK-293T | CC50 |
120 μM
Compound: MPD2
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Cytotoxicity against HEK293T cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
Cytotoxicity against HEK293T cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
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[PMID: 38608245] |
MPD2 (0.1-10 μM; 48 h) significantly reduces the level of MPro-eGFP fusion protein in stably transfected 293T cells in a concentration-dependent manner, and this result is confirmed by flow cytometry analysis[1].
MPD2 (0.03-3 μM; 48 h) exhibits potent activity to induce MPro degradation in MPro-eGFP stably transfected 293T cells, with a DC50 value of 296 nM as determined by Western blot analysis[1].
MPD2 (0.3-3 μM; 48 h) induces MPro degradation via a CRBN-mediated, proteasome-dependent mechanism that requires simultaneous binding to both Mpro and CRBN, as confirmed by competition experiments with MPI8 and pomalidomide and CRISPR-mediated CRBN knockout studies[1].
MPD2 (0.1-3 μM; 48 h) degrades MPro in a proteasome-dependent manner[1].
MPD2 (72 h) exhibits the most potent antiviral activity against the SARS-CoV-2 Delta variant in ACE2+ A549 cells, with an EC50 value of 492 nM, and demonstrates the strongest capacity to reduce MPro protein levels among the tested PROTAC degraders, correlating with its superior antiviral efficacy[1].
MPD2 (0.63-10 μM; 48 h) exhibits broad-spectrum antiviral efficacy against SARS-CoV-2 variants WA.1, BA.1, and XBB.1.5, reducing viral production by 90% in infected A549-hACE2 cells at a concentration of 2.5 μM[1].
MPD2 (48 h) demonstrates 5-fold greater potency against the nirmatrelvir-resistant NSP5 E166A mutant SARS-CoV-2 compared with the wild-type virus, with gradient concentrations tested over 48 hours of treatment[1].
MPD2 (48 h) exhibits significantly lower cytotoxicity in 293T cells, with a CC50 value of 120 μM as determined by MTT assay, which is even higher than the CC50 value (70 μM) of the parent MPI8[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:293T stable cells
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Concentration:0.03 μM; 0.1 μM; 0.3 μM; 1 μM; 3 μM
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Incubation Time:48 h
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Result:Exhibited high potency in inducing MPro degradation in MPro‑eGFP 293T stable cells, with a DC50 value of 296 nM as determined by Western blot analysis using an anti‑MPro antibody.
Induced rapid and long‑lasting degradation of MPro in the same cell line; significant degradation was observed after 6 h of treatment with 3 μM MPD2, and near‑maximal degradation was achieved after 12 h.
Chemical Information
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Molecular Weight 973.12
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Formula C51H68N6O13
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SMILES
O=C(OCC1=CC=CC(OCCCCCCOC2=CC=CC(C(N3C(CC4)C(NC4=O)=O)=O)=C2C3=O)=C1)N[C@@H]([C@H](OC(C)(C)C)C)C(N[C@@H](CC5CCCCC5)C(N[C@@H](C[C@H]6C(NCC6)=O)C=O)=O)=O
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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
[1]. Alugubelli YR, et al. Discovery of First-in-Class PROTAC Degraders of SARS-CoV-2 Main Protease. J Med Chem. 2024 Apr 25;67(8):6495-6507. [Content Brief]
[2]. Mulyadi CH, et al. Triplet-Triplet Annihilation-Based Photon Upconversion with a Macrocyclic Parallel Dimer. Precision chemistry. 2024 Oct 28;2(10):539-544. [Content Brief]
[3]. de Alencar FMS, et al. Terpyridine-based ruthenium complexes containing a 4,5-diazafluoren-9-one ligand with light-driven enhancement of biological activity. Dalton Trans. 2025 Jan 28;54(5):1850-1870. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)