compound 3i (666-15)
中文名称：化合物3i
Compound 3i (666-15)是一种有效的、选择性地抑制CREB介导的基因转录的抑制剂，IC50为81 nM。它还能抑制癌细胞的生长，而不影响正常细胞。
compound 3i (666-15) Chemical Structure
CAS: 1433286-70-4
客户使用Selleck的发表文献12篇
产品质控
compound 3i (666-15)相关产品
相关信号通路图
Epigenetic Reader Domain抑制剂选择性比较
细胞实验数据示例
| 细胞系 | 实验类型 | 给药浓度 | 孵育时间 | 活性描述 | 文献信息 |
|---|---|---|---|---|---|
| HEK293T | Function assay | 50 nM | 1 hr | Inhibition of CREB-mediated gene transcription in human HEK293T cells assessed as inhibition of forskolin-stimulated Nurr1/NR4A2 transcription at 50 nM after 1 hr by qRT-PCT analysis | 26023867 |
| HEK293T | Function assay | > 1 uM | 30 mins | Inhibition of VP16/CREB (unknown origin) interaction in human HEK293T cells assessed as inhibition of forskolin-stimulated gene transcription at > 1 uM after 30 mins by CRE-RLuc complementation assay | 26023867 |
| HEK293T | Function assay | > 1 uM | 30 mins | Inhibition of P53 (unknown origin) transfected in human HEK293T cells assessed as inhibition of forskolin-stimulated gene transcription at > 1 uM after 30 mins by CRE-RLuc complementation assay | 26023867 |
| MDA-MB-468 | Antitumor assay | 10 mg/kg | 5 weeks | Antitumor activity against human MDA-MB-468 cells xenografted in BALB/c mouse assessed as reduction in tumor volume at 10 mg/kg, ip once a day, 5 days per week for 5 weeks relative to control | 26023867 |
| HEK293T | Function assay | 100 nM | 1 hr | Inhibition of CREB in HEK293T cells assessed as inhibition of Fsk-induced NR4A2 gene expression at 100 nM pre-incubated for 1 hr before Fsk stimulation for 45 mins by qRT-PCR analysis | 31765143 |
| MDA-MB-468 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human MDA-MB-468 cells assessed as inhibition of cell growth after 72 hrs by MTT assay, GI50=0.046μM | 26023867 | |
| MDA-MB-231 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth after 72 hrs by MTT assay, GI50=0.073μM | 26023867 | |
| HEK293T | Function assay | 30 mins | Inhibition of CREB (unknown origin) expressed in HEK293T cells assessed as inhibition of forskolin-induced CREB transcription activity incubated for 30 mins by luciferase reporter gene assay, IC50=0.081μM | 31765143 | |
| MCF7 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth after 72 hrs by MTT assay, GI50=0.31μM | 26023867 | |
| A549 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human A549 cells assessed as inhibition of cell growth after 72 hrs by MTT assay, GI50=0.47μM | 26023867 | |
| HEK293T | Function assay | 30 mins | Inhibition of NFkappaB (unknown origin)-mediated gene transcription in human HEK293T cells transfected with an NFkappaB firefly luciferase reporter gene assessed as inhibition of TNFalpha-stimulated gene transcription pretreated for 30 mins measured after, IC50=5.29μM | 26023867 | |
| HEK293T | Function assay | Inhibition of CREB-mediated gene transcription in human HEK293T cells transfected with pCRE-RLuc by renilla luciferase reporter assay, IC50=0.081μM | 26023867 | ||
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | Compound 3i (666-15)是一种有效的、选择性地抑制CREB介导的基因转录的抑制剂，IC50为81 nM。它还能抑制癌细胞的生长，而不影响正常细胞。 | ||
|---|---|---|---|
| 靶点 |
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| 体外研究(In Vitro) | ||||
| 体外研究活性 | 666-15可有效地抑制癌细胞生长。在MDA-MB-231和MDA-MB-468细胞中，666-15的GI50值分别为73 nM和46 nM。在A549和MCF-7细胞中，666-15同样也具有较强的活性，GI50分别为0.47 μM和0.31 μM。在不依赖于直接的CREB或CBP结合反应的活细胞中，666-15可抑制CREB的转录活性[1]。 |
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|---|---|---|---|---|
| 细胞实验 | 细胞系 | HEK 293T细胞 | ||
| 浓度 | 0.05, 0.1, 0.5 μM | |||
| 孵育时间 | -- | |||
| 方法 | 用不同浓度的666-15对HEK 293T细胞进行处理，然后用forskolin处理。通过qRT-PCR分析Nurr1/NR4A2的相对mRNA水平。 |
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| 体内研究(In Vivo) | ||
| 体内研究活性 |
在体内MDA-MB-468异种移植瘤模型中，666-15可完全地抑制肿瘤生长，而没有明显毒性。对小鼠腹腔注射10 mg/kg的666-15，耐受性良好[1]。 |
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|---|---|---|
| 动物实验 | Animal Models | 6-8周龄BALB/c裸小鼠，在其右翼皮下接种了MDA-MB-468细胞形成肿瘤 |
| Dosages | 10 mg/kg | |
| Administration | IP | |
化学信息&溶解度
| 分子量 | 620.52 | 分子式 | C33H31Cl2N3O5 |
| CAS号 | 1433286-70-4 | SDF | -- |
| Smiles | C1=CC=C2C=C(C(=CC2=C1)C(=O)NCCOC3=CC4=CC=CC=C4C=C3C(=O)NC5=C(C=C(C=C5)Cl)O)OCCCN.Cl | ||
| 储存条件(自收到货起) | 3年 -20°C 粉状 | ||
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体外溶解度 |
DMSO : 100 mg/mL ( (161.15 mM)； DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Ethanol : 3 mg/mL Water : Insoluble |
摩尔浓度计算器 |
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体内溶解度 现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂 |
动物体内配方计算器 | ||||
实验计算
动物体内配方计算器（澄清溶液）
第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）
第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）
计算结果：
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；
体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH2O，混匀澄清。
体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。
注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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