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DW-71177
- Development stage
- Preclinical
- Lead developer
- Korea Research Institute of Chemical Technology
- Modality
- Small Molecules
- Administration
- None (research Use Only; No Clinical Route Established)
01
Overview
DW-71177 is a novel [1,2,4]triazolo[4,3-a]quinoxaline‑based **potent and BD1‑selective BET (bromodomain and extraterminal domain) inhibitor**. It binds selectively to the BD1 bromodomain of BET family proteins, specifically targeting the Kac-binding pocket of BD1 with high affinity (ITC KD of 6.7 nM for BRD4-BD1, 20-fold selectivity over BD2)[4][7]. This selectivity allows DW-71177 to efficiently inhibit oncogenes associated with **acute myeloid leukemia**, but with a milder impact on housekeeping genes than pan-BET inhibitors[3][7]. Its mechanism is inhibition of cancer-related transcriptional changes, focusing on genes enriched with BRD4 and histone acetylation marks[7]. DW-71177 has shown strong anti-leukemic activity in preclinical studies and is used for research purposes investigating epigenetic therapies for leukemia[1][2][6][7][10]. It is currently for research use only and not for human or veterinary use[1][10].
- Other names
- DW-71177DW71177DW 71177
02
Targets
BRD4 (Bromodomain-containing protein 4)
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