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I-CBP112 hydrochloride

Names

[ CAS No. ]:
2147701-33-3

[ Name ]:
I-CBP112 hydrochloride

[Synonym ]:
I-CBP112 (hydrochloride)
1-[7-(3,4-Dimethoxyphenyl)-9-{[(3S)-1-methyl-3-piperidinyl]methoxy}-2,3-dihydro-1,4-benzoxazepin-4(5H)-yl]-1-propanone hydrochloride (1:1)
1-Propanone, 1-[7-(3,4-dimethoxyphenyl)-2,3-dihydro-9-[[(3S)-1-methyl-3-piperidinyl]methoxy]-1,4-benzoxazepin-4(5H)-yl]-, hydrochloride (1:1)

Biological Activity

[Description]:

I-CBP112 hydrochloride is a selective inhibitor of CBP/P300 that directly binds their bromodomains (Kds = 142 and 625 nM, respectively). I-CBP112 significantly reduces the leukemia-initiating potential of MLL-AF9(+) acute myeloid leukemia cells in a dose-dependent manner in vitro and in vivo. I-CBP112 increases the cytotoxic activity of BET bromodomain inhibitor JQ1 as well as doxorubicin[1].

[Related Catalog]:

Research Areas >> Cancer
Signaling Pathways >> Epigenetics >> Epigenetic Reader Domain

[References]

[1]. Picaud S, et al. Generation of a Selective Small Molecule Inhibitor of the CBP/p300 Bromodomain for Leukemia Therapy. Cancer Res. 2015 Dec 1;75(23):5106-5119.

Chemical & Physical Properties

[ Molecular Formula ]:
C27H37ClN2O5

[ Molecular Weight ]:
505.046

[ Exact Mass ]:
504.239105


Related Compounds

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