3119106-17-8
Chemical Structure
HP211206
- CAS No.: 3119106-17-8
- Formula:C42H55F2N9O10
- Molecular Weight:883.94
InChIKey: MIOBUUSPHNSVRE-KNRSNOANSA-N
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
Biological Activity: 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[1]
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HP211206 | 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 | |||||||||||||||||||||
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