首页Chromatin/EpigeneticEpigenetic Reader DomainI-CBP112 hydrochloride
I-CBP112 hydrochloride
编号 T4247    
CAS 2147701-33-3     分子式 C27H36N2O5HCl     分子量 505.00
靶点: CBP/p300, Leukemia cell; CBP/p300, Prostate cancer cell; CBP/p300;
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.
纯度:98.0%
规格 库存 单价 数量
1 mg 上海现货 808.00
2 mg 上海现货 1454.00
5 mg 上海现货 2416.00
10 mg 上海现货 4568.00
25 mg 上海现货 8472.00
1 mL * 10 mM (in DMSO) 上海现货 4568.00
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生物活性

产品描述

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.

靶点活性

CBP/p300, Leukemia cell,5.5±1.1μM

CBP/p300, Prostate cancer cell,9.1±1.2μM

CBP/p300,

体外活性

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].

体内活性

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].

化学信息

分子量

505.00

分子式

C27H36N2O5HCl

CAS

2147701-33-3

溶解度

DMSO: ≥32 mg/mL

( < 1 mg/ml refers to the product slightly soluble or insoluble )

储存条件

store at -80°C

备注

For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

配制溶液

1 mg 5 mg 10 mg
1 mM 1.98 ml 9.901 ml 19.802 ml
5 mM 0.396 ml 1.98 ml 3.96 ml
10 mM 0.198 ml 0.99 ml 1.98 ml
50 mM 0.04 ml 0.198 ml 0.396 ml
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