I-CBP112 (hydrochloride)

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].

Product Specifications

CAS Number

[2147701-33-3]

UNSPSC

12352005

Target

Epigenetic Reader Domain

Type

Reference compound

Related Pathways

Epigenetics

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/i-cbp112-hydrochloride.html

Solubility

10 mM in DMSO

Smiles

CCC(N1CCOC2=C(OC[C@@H]3CN(C)CCC3)C=C(C4=CC=C(OC)C(OC)=C4)C=C2C1)=O.[H]Cl

Molecular Formula

C27H37ClN2O5

Molecular Weight

505.05

References & Citations

[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.