Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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.
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
1 mg | In stock | $ 83.00 | |
2 mg | In stock | $ 148.00 | |
5 mg | In stock | $ 249.00 | |
10 mg | In stock | $ 471.00 | |
25 mg | In stock | $ 773.00 | |
50 mg | In stock | $ 1,080.00 | |
100 mg | In stock | $ 1,460.00 | |
1 mL * 10 mM (in DMSO) | In stock | $ 471.00 |
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]. |
Molecular Weight | 505.05 |
Formula | C27H37ClN2O5 |
CAS No. | 2147701-33-3 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 60 mg/mL (118.8 mM)
You can also refer to dose conversion for different animals. More
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I-CBP112 hydrochloride 2147701-33-3 Chromatin/Epigenetic Epigenetic Reader Domain inhibit Inhibitor I CBP112 hydrochloride I-CBP 112 Hydrochloride I-CBP-112 hydrochloride I-CBP112 I-CBP112 Hydrochloride I-CBP-112 Hydrochloride ICBP112 hydrochloride inhibitor