I-CBP112 (hydrochloride) |
| Catalog No.GC43889 |
I-CBP112 (chlorhydrate) est un inhibiteur sélectif de CBP/P300 qui lie directement leurs bromodomaines (Kds \u003d 142 et 625 nM, respectivement). I-CBP112 réduit significativement le potentiel d'initiation de la leucémie des cellules de leucémie myéloïde aiguë MLL-AF9 (+) de manière dose-dépendante in vitro et in vivo. I-CBP112 augmente l'activité cytotoxique de l'inhibiteur de bromodomaine BET JQ1 ainsi que de la doxorubicine.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2147701-33-3
Sample solution is provided at 25 µL, 10mM.
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cAMP-responsive element-binding protein binding protein (CREBBP) and E1A-associated protein p300 (EP300) are transcriptional co-activators that modulate DNA replication, DNA repair, cell growth, transformation, and development. Both CBP and EP300 contain bromodomains, which mediate their binding to acetylated lysine residues on histones and other proteins. I-CBP112 is a selective inhibitor of CBP and EP300 that directly binds their bromodomains (Kds = 0.142 and 0.625 μM, respectively). Developed by the Structural Genomics Consortium (SGC), this compound shows only weak cross-reactivity with the bromodomains of bromodomain and extra-terminal proteins and shows no interaction with other bromodomains.
Average Rating: 5 (Based on Reviews and 29 reference(s) in Google Scholar.)
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