| Name | I-CBP112 hydrochloride |
| Description | I-CBP112 is a selective inhibitor of the bromodomain-containing transcription factors. I-CBP112 (1 mM) has little activity against other bromodomains. I-CBP112 targets the CBP/p300 bromodomains. I-CBP112 significantly reduced the leukemia-initiating potential of MLL-AF9(+) acute myeloid leukemia cells in a dose-dependent manner in vitro and in vivo. Interestingly, I-CBP112 increased the cytotoxic activity of BET bromodomain inhibitor JQ1 as well as doxorubicin. |
| In vitro | I-CBP112 markedly increases acetylation by p300 at the histone H3K18 and H3K23 sites. I-CBP112 stimulated H3K18ac by ~3-fold, and induced enhances acetylation of these same sites by CBP as well as at H4K5. The EC50s of activation of I-CBP112 on CBP- and p300-mediated H3K18 acetylation are ~2 μM[1]. In mouse and human leukemia cell lines, I-CBP112 causes substantially impaired colony formation and induces cellular differentiation without significant cytotoxicity. In BioMAP primary cell panel, I-CBP112 results in a unique response on cytokine and marker protein expression[2]. |
| In vivo | I-CBP112 markedly and dose-dependently reduces the leukemia-initiating potential of mLL-AF9+ AmL cells in vitro and in vivo. The synergistic effects of I-CBP112 and current standard therapy (doxorubicin), as well as emerging treatment strategies (BET inhibition), provide new possibilities for combinatorial treatment of leukemia and potentially other cancers[2]. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 60 mg/mL (118.8 mM)
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| Keywords | inhibit | Inhibitor | I CBP112 hydrochloride | I-CBP 112 Hydrochloride | I-CBP-112 hydrochloride | I-CBP112 | I-CBP112 Hydrochloride | I-CBP-112 Hydrochloride | ICBP112 hydrochloride | Epigenetic Reader Domain |
| Inhibitors Related | ABBV-744 | CeMMEC1 | 3-methyl-1,2,3,4-tetrahydroquinazolin-2-one | (+)-JQ-1 | J-147 | Anacardic Acid | Curcumin | dBET6 | Piflufolastat | Naphthol AS-E | Bisdemethoxycurcumin | GSK1379725A |
| Related Compound Libraries | Histone Modification Compound Library | Bioactive Compound Library | Epigenetics Compound Library | Hematonosis Compound Library | Inhibitor Library | NO PAINS Compound Library | PPI Inhibitor Library | Bioactive Compounds Library Max | Transcription Factor-Targeted Compound Library |
United States
