KB02-JQ1 |
カタログ番号GC60964 |
KB02-JQ1 は、選択性の高い PROTAC ベースの BRD4 分解剤 (分子接着剤) ですが、BRD2 または BRD3 は分解しません。 KB02-JQ1 は、DCAF16 (E3 リガーゼ) を共有結合で修飾することにより BRD4 の分解を促進し、生物系におけるタンパク質分解の耐久性を向上させることができます。 JQ1はリンカーを介してユビキチンE3リガーゼリガンドKB02に結合し、KB02-JQ1を形成します。
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Cas No.: 2384184-44-3
Sample solution is provided at 25 µL, 10mM.
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].
KB02-JQ1 (5-40 μM; 24 hours; HEK293T cells) treatment shows concentration-dependent degradation of endogenous BRD4 in HEK293T cells[1]. Western Blot Analysis[1] Cell Line: HEK293T cells
[1]. Zhang X, et al. Electrophilic PROTACs that degrade nuclear proteins by engaging DCAF16. Nat Chem Biol. 2019 Jul;15(7):737-746.
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