| Identification | Back Directory | [Name]
6H-Thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine-6-acetamide, N-[2-[2-[2-[[2-[[1-(2-chloroacetyl)-1,2,3,4-tetrahydro-6-quinolinyl]oxy]acetyl]amino]ethoxy]ethoxy]ethyl]-4-(4-chlorophenyl)-2,3,9-trimethyl-, (6S)- | [CAS]
2384184-44-3 | [Synonyms]
KB02-JQ1
6H-Thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine-6-acetamide, N-[2-[2-[2-[[2-[[1-(2-chloroacetyl)-1,2,3,4-tetrahydro-6-quinolinyl]oxy]acetyl]amino]ethoxy]ethoxy]ethyl]-4-(4-ch
6H-Thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine-6-acetamide, N-[2-[2-[2-[[2-[[1-(2-chloroacetyl)-1,2,3,4-tetrahydro-6-quinolinyl]oxy]acetyl]amino]ethoxy]ethoxy]ethyl]-4-(4-chlorophenyl)-2,3,9-trimethyl-, (6S)- | [Molecular Formula]
C38H43Cl2N7O6S | [MDL Number]
MFCD32857147 | [MOL File]
2384184-44-3.mol | [Molecular Weight]
796.76 |
| Hazard Information | Back Directory | [Uses]
KB02-JQ1 is a highly selective and PROTAC-based BRD4 degrader (molecular glue), but does not degrade BRD2 or BRD3. KB02-JQ1 promotes BRD4 degradation by covalently modifying DCAF16 (E3 ligase) and can improve the durability of protein degradation in biological systems. JQ1 binds ubiquitin E3 ligase ligand KB02 via a linker to form KB02-JQ1[1]. | [IC 50]
BRD4 | [References]
[1] Zhang X, et al. Electrophilic PROTACs that degrade nuclear proteins by engaging DCAF16. Nat Chem Biol. 2019 Jul;15(7):737-746. DOI:10.1038/s41589-019-0279-5 |
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