首页工具

购物车

666-15

产品编号 T5318 CAS 1433286-70-4

别名: CREB inhibitor

666-15 (CREB inhibitor) 是一种选择性CREB 抑制剂，IC50为 81 nM，可抑制乳腺癌异种移植模型中的肿瘤生长。

TargetMol的所有产品和服务仅用于科学研究，不能被用于人体，我们也不向个人提供产品和服务。

666-15, CAS 1433286-70-4

规格	价格/CNY	货期
1 mg	￥ 413	现货
5 mg	￥ 945	现货
10 mg	￥ 1,530	现货
25 mg	￥ 3,230	现货
50 mg	￥ 4,770	现货
100 mg	￥ 6,780	现货
1 mL * 10 mM (in DMSO)	￥ 1,130	现货

大包装超大折扣，点击咨询

选择批次

纯度: 99.77%

纯度: 99.47%

纯度: 99.41%

更多批次查询请联系客服

生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

产品描述	666-15 (CREB inhibitor) 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].

别名	CREB inhibitor
分子量	620.52
分子式	C33H31Cl2N3O5
CAS No.	1433286-70-4

存储

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

溶解度

DMSO: 60 mg/mL (96.7 mM)

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.6116 mL	8.0578 mL	16.1155 mL	40.2888 mL
	5 mM	0.3223 mL	1.6116 mL	3.2231 mL	8.0578 mL
	10 mM	0.1612 mL	0.8058 mL	1.6116 mL	4.0289 mL
	20 mM	0.0806 mL	0.4029 mL	0.8058 mL	2.0144 mL
	50 mM	0.0322 mL	0.1612 mL	0.3223 mL	0.8058 mL

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

质量

浓度

容积

分子量

浓度 (起始)

容积 (起始)

浓度 (终)

容积 (终)

溶液体积

质量

配液浓度

参考文献

1. Xie F, et al. Identification of a Potent Inhibitor of CREB-Mediated Gene Transcription with Efficacious in Vivo Anticancer Activity. J Med Chem. 2015 Jun 25;58(12):5075-87. 2. Yang C, et al. Inhibition of Necroptosis Rescues SAH-Induced Synaptic Impairments in Hippocampus via CREB-BDNF Pathway. Front Neurosci. 2019 Jan 7;12:1990. 3. Li BX, et al. Systemic Inhibition of CREB is Well-tolerated in vivo. Sci Rep. 2016 Oct 3;6:34513. 4. Zhi Y, Lu C, Zhu G, et al. Positive regulation of the CREB phosphorylation via JNK-dependent pathway prevents antimony-induced neuronal apoptosis in PC12 cell and mice brain[J]. NeuroToxicology. 2020

文献引用

1. Ding D, Zheng R, Tian Y, et al. Retinoblastoma protein as an intrinsic BRD4 inhibitor modulates small molecule BET inhibitor sensitivity in cancer. Nature Communications. 2022, 13(1): 1-15. 2. Zheng Y, Ding W, Zhang T, et al. Antimony-induced astrocyte activation via mitogen-activated protein kinase activation-dependent CREB phosphorylation. Toxicology Letters. 2021 3. Zou L, Hong D, Li K, et al. Salt-inducible kinase 2 (SIK2) inhibitor ARN-3236 attenuates bleomycin-induced pulmonary fibrosis in mice. BMC Pulmonary Medicine. 2022, 22(1): 1-11 4. Zhi Y, Lu C, Zhu G, et al. Positive regulation of the CREB phosphorylation via JNK-dependent pathway prevents antimony-induced neuronal apoptosis in PC12 cell and mice brain. NeuroToxicology. 2020 Dec;81:101-108

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

666-15 1433286-70-4 Chromatin/Epigenetic Epigenetic Reader Domain breast cancer CREB 66615 666 15 CREB inhibitor inhibit Inhibitor inhibitor

我们的所有产品和服务仅用于科学研究，不能被用于人体，我们也不向个人提供产品和服务。

沪公网安备 31010602006700号

陶术

生物

TargetMol^®中国区唯一合作伙伴

点击进入陶术生物官网

联系我们

电话：

400-820-0310

邮箱：

service@tsbiochem.com

QQ：

2881945090（终端用户）

2885109491（经销商）

经销：

终端：

地址：

上海市静安区江场三路238号8楼

666-15

存储

溶解度

溶液配制表

计算器

输入分子式，点击计算，可计算出产品的分子量。

参考文献

文献引用

相关产品

相关化合物库

剂量换算

体内实验配液计算器

技术支持

Keywords