I-<wbr/>CBP112 (hydro<wbr>chloride)

I-CBP112 (hydrochloride)

CAT N°: 14468
Price:

From 66.00 56.10

I-CBP112 is an inhibitor of p300 and CREB-binding protein (CBP) histone acetyltransferases.{67112} It binds to the p300 and CBP bromodomains (Kds = 167 and 151 nM, respectively) and is selective for p300 and CBP over BRD4, as well as a panel of 104 nuclear receptors and ion channels and a panel of 32 enzymes at 10 µM. I-CBP112 displaces acetylated histones from CBP in a cell-free assay (IC50 = 170 nM). It reduces colony formation and increases differentiation of primary murine leukemic blasts and delays disease initiation following leukemic blast transplantation into sub-lethally irradiated mice when used at concentrations of 5 and 10 µM.

Territorial Availability: Available through Bertin Technologies only in France

  • Synonyms
    • 1-[7-(3,4-dimethoxyphenyl)-2,3-dihydro-9-[[(3S)-1-methyl-3-piperidinyl]methoxy]-1,4-benzoxazepin-4(5H)-yl]-1-propanone, monohydrochloride
  • Correlated keywords
    • inhibitors inhibits inhibitions epigenetics chromatins research genes regulations CBPs CREBBP EP-300 EPs 300 EP300 ICBP112 CBP-112 bromodomains BETs extra-terminal extra terminal selective HCl hydrochlorides transcriptional transcriptions coactivators co-activators modulates modulating DNA deoxyribonucleic acids replications repairs cells growths transformations developments mediates mediations binds bindings acetylated acetylations lysines residues histones proteins Structural Genomic Consortium SGC 1640282-31-0 BRD-4
  • Product Overview:
    I-CBP112 is an inhibitor of p300 and CREB-binding protein (CBP) histone acetyltransferases.{67112} It binds to the p300 and CBP bromodomains (Kds = 167 and 151 nM, respectively) and is selective for p300 and CBP over BRD4, as well as a panel of 104 nuclear receptors and ion channels and a panel of 32 enzymes at 10 µM. I-CBP112 displaces acetylated histones from CBP in a cell-free assay (IC50 = 170 nM). It reduces colony formation and increases differentiation of primary murine leukemic blasts and delays disease initiation following leukemic blast transplantation into sub-lethally irradiated mice when used at concentrations of 5 and 10 µM.

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