protac bet degrader 2 Search Results


protac bet degrader 2  (MedChemExpress)
90
MedChemExpress protac bet degrader 2
Chemical structures of tested compounds. The compounds tested included pan-BRD PROTAC dBET1, PROTAC BET Degrader-1, and PROTAC BET <t>Degrader-2;</t> the pan-BRD ligands (+)-JQ1 and HJB97; the cereblon ligands thalidomide and lenalidomide; the BRD/BD2 selective ligand RVX-208; and the VHL ligand VH032.
Protac Bet Degrader 2, supplied by MedChemExpress, used in various techniques. Bioz Stars score: 90/100, based on 1 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
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Chemical structures of tested compounds. The compounds tested included pan-BRD PROTAC dBET1, PROTAC BET Degrader-1, and PROTAC BET Degrader-2; the pan-BRD ligands (+)-JQ1 and HJB97; the cereblon ligands thalidomide and lenalidomide; the BRD/BD2 selective ligand RVX-208; and the VHL ligand VH032.

Journal: ACS Pharmacology & Translational Science

Article Title: General Stepwise Approach to Optimize a TR-FRET Assay for Characterizing the BRD/PROTAC/CRBN Ternary Complex

doi: 10.1021/acsptsci.1c00032

Figure Lengend Snippet: Chemical structures of tested compounds. The compounds tested included pan-BRD PROTAC dBET1, PROTAC BET Degrader-1, and PROTAC BET Degrader-2; the pan-BRD ligands (+)-JQ1 and HJB97; the cereblon ligands thalidomide and lenalidomide; the BRD/BD2 selective ligand RVX-208; and the VHL ligand VH032.

Article Snippet: We purchased dBET1, PROTAC BET Degrader-1, PROTAC BET Degrader-2, HJB97, thalidomide, and lenalidomide from MedChemExpress USA (Monmouth Junction, NJ).

Techniques:

TR-FRET dose–response curves of PROTAC ternary complex formation. The compounds tested include dBET1, PROTAC BET Degrader-1, PROATC BET Degrader-2, (+)-JQ1, HJB97, thalidomide, and lenalidomide. The assays were performed under condition 5 with a 180 min incubation with Tb-anti-GST (2 nM), GST-BRD2(BD1) (2 nM), His-CRBN(DDB1) (8 nM), and AF488-anti-His (4 nM). (a) Relative TR-FRET signals in RTU (10 000 × 520 nm/490 nm). (b) Normalized TR-FRET signals as fold change to DMSO.

Journal: ACS Pharmacology & Translational Science

Article Title: General Stepwise Approach to Optimize a TR-FRET Assay for Characterizing the BRD/PROTAC/CRBN Ternary Complex

doi: 10.1021/acsptsci.1c00032

Figure Lengend Snippet: TR-FRET dose–response curves of PROTAC ternary complex formation. The compounds tested include dBET1, PROTAC BET Degrader-1, PROATC BET Degrader-2, (+)-JQ1, HJB97, thalidomide, and lenalidomide. The assays were performed under condition 5 with a 180 min incubation with Tb-anti-GST (2 nM), GST-BRD2(BD1) (2 nM), His-CRBN(DDB1) (8 nM), and AF488-anti-His (4 nM). (a) Relative TR-FRET signals in RTU (10 000 × 520 nm/490 nm). (b) Normalized TR-FRET signals as fold change to DMSO.

Article Snippet: We purchased dBET1, PROTAC BET Degrader-1, PROTAC BET Degrader-2, HJB97, thalidomide, and lenalidomide from MedChemExpress USA (Monmouth Junction, NJ).

Techniques: Incubation

Comparison of PROTAC BET Degrader-1, PROTAC BET Degrader-2, and dBET1 for their Previously Reported IC 50 Values and TR-FRET Maximal PROTAC Efficacy Concentrations

Journal: ACS Pharmacology & Translational Science

Article Title: General Stepwise Approach to Optimize a TR-FRET Assay for Characterizing the BRD/PROTAC/CRBN Ternary Complex

doi: 10.1021/acsptsci.1c00032

Figure Lengend Snippet: Comparison of PROTAC BET Degrader-1, PROTAC BET Degrader-2, and dBET1 for their Previously Reported IC 50 Values and TR-FRET Maximal PROTAC Efficacy Concentrations

Article Snippet: We purchased dBET1, PROTAC BET Degrader-1, PROTAC BET Degrader-2, HJB97, thalidomide, and lenalidomide from MedChemExpress USA (Monmouth Junction, NJ).

Techniques: Comparison, Inhibition, Concentration Assay