I-CBP112

I-CBP112，是一种特异性的乙酰赖氨酸竞争性蛋白质-蛋白质相互作用抑制剂，靶向 CBP/p300 溴结构域，增强 p300 的乙酰化作用。更多视频请关注视频号【艾维缔】。哔哩哔哩【IVDSHOW】。抖音【军哥聊表观】。

关键词

I-CBP112

所属分类

抑制剂

目录号

T3969

获取报价

猜你喜欢

产品描述
产品组分
文件资源
营销中心
注意事项
FAQ
文献追踪

I-CBP112 是一种特异性的乙酰赖氨酸竞争性蛋白质-蛋白质相互作用抑制剂，靶向 CBP/p300 溴结构域，增强 p300 的乙酰化作用。

生物活性

产品描述	I-CBP112 is a specific and potent acetyl-lysine competitive protein-protein interaction inhibitor targeting the CBP/p300 bromodomains.
靶点活性	CBP-p300 (Leukemia cells):5.5±1.1 μM (IC50), CBP-p300 (Prostate cancer cells):9.1±1.2 μM (IC50)
体外活性	将人类和小鼠白血病细胞系暴露于I-CBP112后，显著抑制了菌落形成并且促进了细胞分化，而无明显的细胞毒性。I-CBP112对BioMAP原代细胞板的暴露引起了独特的细胞因子和标志蛋白表达反应。I-CBP112显著增强了p300在组蛋白H3K18和H3K23位点的乙酰化作用。I-CBP112使H3K18ac增加约3倍，I-CBP112诱导的CBP在这些相同位点以及H4K5位点的乙酰化也有所增强。I-CBP112激活p300和CBP介导的H3K18乙酰化的EC50值约为2μM。
体内活性	I-CBP112 在体外和体内显著以剂量依赖方式降低了MLL-AF9+ AML细胞的白血病发起潜力。
激酶实验	TGase 2 from guinea pig liver is preincubated for 10 min with various concentrations of GK13 or GK921 in 0.1 mL of reaction buffer, with or without 10 mM CaCl2, followed by the addition of 0.4 mL of substrate solution containing 2
细胞实验	I-CBP112 is dissolved in DMSO and diluted with appropriate medium before use. Cells (6000 KG1a and 13000 LNCaP cells/well) are plated in 96-well flat-bottom plates approximately 24 h prior to drug treatment. After 24 h, 10–20% fetal bovine serum-containing medium is replaced with 2.5% serum medium, and cells are treated with I-CBP112 in 0.18% DMSO; 0.18% DMSO is shown to have negligible cell growth effects under the conditions used in our experiments. After being exposed to I-CBP112 for 66 h, cells are subjected to a final concentration of 0.476% [3H]thymidine per well and allowed to proliferate for an additional 6 h (exposure to I-CBP112 for a total of 72 h). Cells are harvested, and the counts of 3H in each well are taken relative to those treated with vehicle alone to quantify the effect of the ligand on proliferation[1].

化学信息

分子量	468.59
分子式	C₂₇H₃₆N₂O₅
CAS No.	1640282-31-0
Smiles	CCC(=O)N1CCOc2c(C1)cc(cc2OC[C@H]1CCCN(C)C1)-c1ccc(OC)c(OC)c1
密度	1.129 g/cm3 (Predicted)

产品组分

内容	型号	规格	储存温度
I-CBP112	T3969-01	1mg	-20°C
I-CBP112	T3969-02	2mg	-20°C
I-CBP112	T3969-03	5mg	-20°C
I-CBP112	T3969-04	10mg	-20°C
I-CBP112	T3969-05	25mg	-20°C
I-CBP112	T3969-06	50mg	-20°C
I-CBP112	T3969-07	100mg	-20°C
I-CBP112	T3969-08	500mg	-20°C
操作手册	1	1	常温

文件资源

营销中心
注意事项

保存建议厂家推荐蓝冰运输。当您收到产品后，按照说明书建议保存于-20°C。
FAQ
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.

Discovery of a peptide proteolysis-targeting chimera (PROTAC) drug of p300 for prostate cancer therapy.

Dize Zhang, Bohan Ma, ..., Lei Li

EBioMedicine | 2024 Jul 12 | 38954976

Glutamine Deprivation Suppresses Lung Cancer Metastasis via Inducing the Activation of ZAKα and Translation Inhibition

Yinrui Lei, Huiyun Lin, ..., Fang Guo

Europe PMC | 2024 Jan 18