首页Chromatin/EpigeneticEpigenetic Reader Domain666-15
666-15
编号 T5318     别名: CREB inhibitor, CREB inhibitor,
CAS 1433286-70-4     分子式 C33H31Cl2N3O5     分子量 620.52
靶点: CREB;
666-15 is a potent and selective CREB inhibitor (IC50: 81 nM).
规格 库存 单价 数量
2 mg 上海现货 754.00
5 mg 上海现货 1111.00
10 mg 上海现货 2091.00
25 mg 上海现货 4222.00
50 mg 上海现货 7872.00
1 mL * 10 mM (in DMSO) 上海现货 1467.00
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生物活性

产品描述

666-15 is a potent and selective CREB inhibitor (IC50: 81 nM).

靶点活性

CREB,81 nM (in HEK 293T cells)

体外活性

666-15 is a potent and selective inhibitor of CREB-mediated gene transcription (IC50 = 0.081 ± 0.04 μM). 666-15 also potently inhibited cancer cell growth without harming normal cells [1]. Isoproterenol (ISO) induced cardiac hypertrophy. The rate of ROS production, CREB phosphorylation, and miR-132 expression increased after the addition of ISO. Upregulation of miR-132 was blocked by the specific inhibitor of CREB transcription, 666-15 [2].

体内活性

In an in vivo MDA-MB-468 xenograft model, 666-15 completely suppressed the tumor growth without overt toxicity [1]. 666-15 was found to be readily bioavailable to achieve pharmacologically relevant concentrations for CREB inhibition. The mice treated with 666-15 showed no evidence of changes in body weight, complete blood count, blood chemistry profile, cardiac contractility and tissue histologies from liver, kidney, and heart [3].

细胞实验

HEK 293T cells in a 10 cm plate were transfected with pCRE-RLuc (6 μg) with Lipofectamine2000 following the manufacturer’s instructions. Three hours after transfection, the cells were collected and replated into 96-well plates at ?10?000 cells/well. The cells were allowed to attach to the bottom of the plates overnight. The cells were then treated with different concentrations of different compounds for 30 min when forskolin (10 μM) was added to each well. The cells were incubated for further 5 h before cell lysis using 1× 30 μL Renilla luciferase lysis buffer. An amount of 5 μL of the lysate was combined with 30 μL of benzyl-coelenterazine solution in PBS (pH 7.4, 10 μg/mL). The protein concentration in each well was determined. The Renilla luciferase activity was normalized to protein content in each well and expressed as relative luciferase unit/μg protein (RLU/μg protein). The IC50 was derived from nonlinear regression analysis of the RLU/μg protein–concentration curve [1].

动物实验

Each 6- to 8-week old BALB/c nude mouse was inoculated subcutaneously at the right flank with MDA-MB-468 cells (5 × 10^6) in 0.1 mL of HBSS with Matrigel (1:1) for tumor development. When the tumor volume reached approximately 100 mm3, the mice were randomized to be treated with either vehicle or 666-15 at 10 mg/kg. 3i was dissolved in 1% N-methylpyrrolidone (NMP), 5% Tween-80 in H2O. The dosing solution was prepared weekly. The mice were treated once a day for 5 consecutive days a week, and the treatment lasted for 5 weeks. During the treatment, the tumor size and body weight were measured 2–3 times a week. The tumors were measured in two dimensions using a digital caliper, and the volume was expressed in mm3 using the formula V = 0.5ab2, where a and b represent the long and short diameters of the tumor, respectively. The tumor volume was normalized to the initial tumor volume at the time of the first treatment [1].

化学信息

分子量

620.52

分子式

C33H31Cl2N3O5

CAS

1433286-70-4

溶解度

DMSO: 20 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 1.612 ml 8.058 ml 16.116 ml
5 mM 0.322 ml 1.612 ml 3.223 ml
10 mM 0.161 ml 0.806 ml 1.612 ml
50 mM 0.032 ml 0.161 ml 0.322 ml
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