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JET-209
- Development stage
- Unknown
- Lead developer
- University of Michigan
- Modality
- PROTACs (E3 ligase recruitment) → Targeted Protein Degraders (TPDs) → Small Molecules, Bivalent/Multivalent Binders → Multivalent & Scaffold-Based Small Molecules → Small Molecules
01
Overview
JET-209: sourced facts only. name: "This compound, JET-209, achieved a half-maximal degradation (DC50) value of 0.05 nM for CBP and 0.2 nM for p300 with maximum degradation (Dmax) >95% for both proteins in the RS4;11 leukemia cell line after 4 h of treatment." [PMID:37276143]; target: "This compound, JET-209, achieved a half-maximal degradation (DC50) value of 0.05 nM for CBP and 0.2 nM for p300 with maximum degradation (Dmax) >95% for both proteins in the RS4;11 leukemia cell line after 4 h of treatment." [PMID:37276143]; developer: "Program in Chemical Biology, University of Michigan, Ann Arbor, Michigan 48104, United States." [PMID:37276143]; modality: "We describe herein our design, synthesis, and extensive evaluation of exceptionally potent PROTAC degraders of CBP/p300, exemplified by JET-209 (24)." [PMID:37276143]; stage: "JET-209 effectively inhibited tumor growth in xenograft tumor models at tolerated dose schedules." [PMID:37276143]
02
Targets
EP300 (Histone acetyltransferase p300 (EP300) catalytic domain)
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