TPCA-1

别名: GW683965

TPCA-1 (GW683965)是一种IKK-2抑制剂,无细胞试验中IC50为17.9 nM,抑制NF-κB通路,比作用于IKK-1选择性高22倍。TPCA-1 也是 STAT3 的抑制剂并可促进凋亡。

TPCA-1 Chemical Structure

TPCA-1 Chemical Structure

CAS: 507475-17-4

规格 价格 库存 购买数量
10mM (1mL in DMSO) 1794.47 现货
10mg 1391.13 现货
50mg 3849.3 现货
1g 24488.1 现货
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TPCA-1相关产品

相关信号通路图

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
C57BL/6 mouse BMDM cells Function assay 0.5 μM 1 h Antiinflammatory activity in C57BL/6 mouse BMDM cells assessed as inhibition of LPS-stimulated TNFalpha production at 0.5 uM pretreated for 1 hr before LPS challenge after 8 to 24 hrs by immunoassay 22533790
C57BL/6 mouse BMDM cells Cytotoxicity assay 24 h Cytotoxicity against C57BL/6 mouse BMDM cells assessed as LDH release after 24 hrs 22533790
MDA-MB-231 Cytotoxicity assay 3 days Cytotoxicity against human MDA-MB-231 cells assessed as cell growth inhibition after 3 days by presto blue dye based plate reader method 27077228
TC32 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells 29435139
DAOY qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells 29435139
SJ-GBM2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells 29435139
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells 29435139
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells 29435139
BT-37 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells 29435139
NB-EBc1 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells 29435139
U-2 OS qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells 29435139
Saos-2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells 29435139
SK-N-SH qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells 29435139
NB1643 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells 29435139
LAN-5 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells 29435139
Rh18 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells 29435139
OHS-50 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells 29435139
RD qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells 29435139
MG 63 (6-TG R) qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells 29435139
Rh30 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells 29435139
Rh41 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells 29435139
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells) 29435139
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells 29435139
TC32 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells 29435139
MG 63 (6-TG R) qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for MG 63 (6-TG R) cells 29435139
U-2 OS qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for U-2 OS cells 29435139
SK-N-SH qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-SH cells 29435139
点击查看更多细胞系数据

生物活性

产品描述 TPCA-1 (GW683965)是一种IKK-2抑制剂,无细胞试验中IC50为17.9 nM,抑制NF-κB通路,比作用于IKK-1选择性高22倍。TPCA-1 也是 STAT3 的抑制剂并可促进凋亡。
靶点
NF-κB [3] STAT3 [3] IKK2 [1]
(Cell-free assay)
17.9 nM
体外研究(In Vitro)
体外研究活性

在时间分辨荧光能量共振转移试验中,TPCA-1抑制人IKK-2活性,IC50为17.9 nM。TPCA-1被证明是ATP竞争性的。此外,TPCA-1对IKK-1和JNK3分别表现出400 nM和3600 nM的IC50值。TPCA-1浓度依赖性抑制TNF-α,IL-6,和IL-8的产生,IC50值分别为170,290,和320 nM。[1] TPCA-1抑制胶质瘤细胞增殖,以及TNF诱导的RelA (p65)核转运和NFκB依赖性IL8基因表达。重要的是,TPCA-1抑制IFN诱导的基因表达,完全抑制MX1和GBP1基因表达,而对ISG15表达仅具有很小的作用。[2]

激酶实验 IKK-2 试验
重组人IKK-2 (残基1-756)在杆状病毒中以N端GST标记的融合蛋白表达,其活性使用时间分辨荧光共振能量转移测定法进行评估。简而言之,IKK-2 (终浓度5 nM)在试验缓冲液(50 mM HEPES,10 mM MgCl2,1 mM CHAPS,pH 7.4,1 mM DTT 和0.01% w/v BSA)中稀释,加入包含不同浓度化合物或二甲基亚砜(DMSO)载体(终浓度3%)的孔中。加入总体积为30 μL 的GST-IκBα 底物(终浓度25 nM)/ATP (终浓度1 μM)起始反应。反应在室温下培育30分钟,然后加入15 μL 50 mM EDTA终止。加入包含W-1024铕螯合物标记的抗磷酸丝氨酸- IκBα-32/36单克隆抗体12C2,和别藻蓝素标记的抗-GST抗体的检测试剂(15 μL)缓冲液(100 mM HEPES,pH 7.4,150 mM NaCl,和0.1% w/v BSA),反应在室温下进一步培养60分钟。GST- IκBαis的磷酸化程度以特定665-nm能量转移信号的比率,参考铕620-nm信号,使用Packard探测酶标仪测量。
细胞实验 细胞系 U87,MT330,SJ-G2,和 GBM6 人胶质瘤细胞系
浓度 0-50 μM
孵育时间 3天
方法

将来自储备液(10 mg/mL)的10μL 3-(4,5-二甲基噻唑-2)-2,5-二苯基四氮唑溴盐(MTT)加入包含胶质瘤细胞的96孔板中,并在37 °C下培育2-4小时。氧化的MTT通过将100 μL 10%十二烷基硫酸钠(SDS)加入0.01 N HCL中溶解,板在37 °C下湿润的环境中培养4小时。板于570 nm下在酶标仪上读数。

体内研究(In Vivo)
体内研究活性

TPCA-1(3, 10, 或20 mg/kg,i.p., b.i.d.)预防性给药,导致小鼠体内胶原诱导性关节炎(CIA)的严重程度剂量依赖性降低。TPCA-1(10 mg/kg, i.p., b.i.d.)导致的显著降低的疾病严重程度和疾病发作的延迟与抗风湿药,与每隔一天预防性给药的作用相当。TPCA-1- 处理的小鼠爪子组织中,p65的细胞核定位,以及IL-1β,IL-6,TNF-α,和干扰素-γ的水平显著降低。此外,TPCA-1给药导致体内胶原诱导的T细胞增殖显著减少。TPCA-1以20 mg/kg,而不是3或10 mg/kg,i.p.,b.i.d.治疗性给药显著降低CIA的严重程度。[1]

动物实验 Animal Models 患有胶原诱导性关节炎的小鼠
Dosages 3,10,或 20 mg/kg
Administration 通过腹腔注射给药,每日两次

化学信息&溶解度

分子量 279.29 分子式

C12H10FN3O2

CAS号 507475-17-4 SDF Download TPCA-1 SDF
Smiles C1=CC(=CC=C1C2=CC(=C(S2)NC(=O)N)C(=O)N)F
储存条件(自收到货起)

体外溶解度
批次:

DMSO : 56 mg/mL ( (200.5 mM) ;DMSO吸湿会降低化合物溶解度,请使用新开封DMSO)

Water : Insoluble

Ethanol : Insoluble

摩尔浓度计算器

体内溶解度
批次:

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

摩尔浓度计算器

质量 浓度 体积 分子量

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)

mg/kg g μL

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)

% DMSO % % Tween 80 % ddH2O
%DMSO %

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,: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: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: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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