I-CBP112 (hydrochloride) |
| Katalog-Nr.GC43889 |
I-CBP112 (Hydrochlorid) ist ein selektiver Inhibitor von CBP/P300, der ihre Bromodomänen (Kds \u003d 142 bzw. 625 nM) direkt bindet. I-CBP112 reduziert signifikant das Leukämie-initiierende Potenzial von MLL-AF9(+) akuten myeloischen Leukämiezellen in einer dosisabhängigen Weise in vitro und in vivo. I-CBP112 erhöht die zytotoxische Aktivität des BET-Bromodomänen-Inhibitors JQ1 sowie von Doxorubicin.
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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