HP211206
Based on 1 Customer Validation
HP211206 is a bifunctional CRBN-recruiting SARS-CoV-2 Mpro PROTAC degrader with a CRBN IC50 of 3.2 μM and a SARS-CoV-2 Mpro DC50 of 621 nM. HP211206 recruits E3 ubiquitin ligase CRBN to drive ubiquitination and proteasomal degradation of wild-type SARS-CoV-2 Mpro and E166 mutant while inhibiting Mpro enzymatic activity, exhibits no cytotoxicity against normal mammalian cells at tested concentrations, and can be used for the study of COVID-19 and SARS-CoV-2 infection
(Pink: ligand (HY-170599); Blue: Cereblon ligand (HY-41547); Black: linker (HY-B0236)).
Para uso exclusivo en investigación. No vendemos a pacientes.
- No. CAS: 3119106-17-8
- Fòrmula: C42H55F2N9O10
- Peso molecular:883.94
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Almacenamiento:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Actividad biológica
Descripciòn
IC50 & Target
IC50: 181.9 nM (SARS-CoV-2 Mpro);
DC50: 621 nM (SARS-CoV-2 Mpro)[1].
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK-293T | DC50 |
621 nM
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Half-maximum degradation of overexpressed wild-type SARS-CoV-2 Mpro in human HEK 293T cells, determined by grayscale analysis of protein levels after 48 h of treatment with HP211206.
Half-maximum degradation of overexpressed wild-type SARS-CoV-2 Mpro in human HEK 293T cells, determined by grayscale analysis of protein levels after 48 h of treatment with HP211206.
|
38064654 |
In Vitro
HP211206 (3-10000 nM; 2-48 h) induces time- and dose-dependent degradation of wild-type SARS-CoV-2 Mpro in HEK 293T cells, with a DC50 of 621 nM, and exhibits no cytotoxicity at concentrations up to 100000 nM[1].
HP211206 (10-3000 nM; 2-48 h) induces dose-dependent degradation of drug-resistant SARS-CoV-2 Mpro mutants SARS-CoV-2 MproE166V and SARS-CoV-2 MproE166A in HEK 293T cells[1].
HP211206 (3-10000 nM; 2-48 h) dose-dependently and time-dependently degrades SARS-CoV-2 Mpro in transfected HEK 293T cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HEK 293T cells
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Concentration:0.1-100 μM
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Incubation Time:48 h
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Result:Showed no significant cytotoxicity at all tested concentrations.
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Cell Line:HEK 293T cells transfected with pcDNA3.1(+)-SARS-CoV-2 Mpro plasmid
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Concentration:1000 nM
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Incubation Time:2, 6, 12, 24, 36, 48 h
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Result:Induced degradation of transfected SARS-CoV-2 Mpro in time-dependent manners.
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Cell Line:HEK 293T cells transfected with pcDNA3.1(+)-SARS-CoV-2 Mpro plasmid
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Concentration:3, 10, 30, 100, 300, 1000, 3000,10000 nM
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Incubation Time:48 h
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Result:Induced degradation of transfected SARS-CoV-2 Mpro in dose-dependent manners.
Chemical Information
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No. CAS 3119106-17-8
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Appearance Solid
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Peso molecular 883.94
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Fòrmula C42H55F2N9O10
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Color Light yellow to green yellow
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SMILES
O=C(CCC1N2C(C(C(NCCCCCC(N(C)[C@@H](C)C(N[C@@H](C(C)(C)C)C(N3[C@H](C(N[C@H](C#N)C[C@H]4C(NCC4)=O)=O)C[C@@H](OC(F)F)C3)=O)=O)=O)=CC=C5)=C5C2=O)=O)NC1=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Pureza y Documentación
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Ficha de datos (271 KB)
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SDS (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instrucciones de manejo (2659 KB)
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
HP211206 Related Classifications
HY-170598 Related Classifications
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