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I-CBP112 hydrochloride

Catalog No. T4247 CAS 2147701-33-3

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.

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I-CBP112 hydrochloride Chemical Structure

I-CBP112 hydrochloride, CAS 2147701-33-3

Pack Size	Availability	Price/USD
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

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Purity: 97.98%

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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

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 60 mg/mL (118.8 mM)

References and Literature

1. Zucconi BE, et al. Modulation of p300/CBP Acetylation of Nucleosomes by Bromodomain LigandI-CBP112. Biochemistry. 2016 Jul 12;55(27):3727-34. 2. 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):5106-19.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Histone Modification Compound Library NO PAINS Compound Library Epigenetics Compound Library Bioactive Compound Library Bioactive Compounds Library Max Hematonosis Compound Library PPI Inhibitor Library Transcription Factor-Targeted Compound Library

Related Products

Related compounds with same targets

AU-15330 ZEN-3219 dCBP-1 GNE-375 Bromodomain inhibitor-12 (+)-JQ1 PA TTK21 CPI-0610 carboxylic acid

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Keywords

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

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