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NF-κB
IκB/IKK inhibitor
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NF-κB inhibitor
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STAT inhibitor
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Apoptosis related activator
TPCA-1
僅限科研使用
TPCA-1
別名: GW683965
TPCA-1 (GW683965)是一種IKK-2抑制劑，無細(xì)胞試驗(yàn)中IC50為17.9 nM，抑制NF-κB通路，比作用于IKK-1選擇性高22倍。TPCA-1 也是 STAT3 的抑制劑并可促進(jìn)凋亡。
TPCA-1 Chemical Structure
CAS: 507475-17-4
產(chǎn)品質(zhì)控
批次：
純度：
99.85%
99.85
TPCA-1相關(guān)產(chǎn)品
| 相關(guān)靶點(diǎn) | IκB IKK | 點(diǎn)擊展開 |
|---|---|---|
| 相關(guān)產(chǎn)品 | IKK-16 Bay 11-7085 BMS-345541 IMD 0354 MRT67307 HCl SC-514 LY2409881 TBK1/IKKε-IN-5 PS-1145 Dehydrocostus Lactone Wedelolactone WS6 BAY-985 WS3 AZD3264 Rosmarinic acid TBK1/IKKε-IN-2 | 點(diǎn)擊展開 |
| 相關(guān)化合物庫 | FDA藥物庫 免疫/炎癥分子化合物庫 小分子免疫腫瘤化合物庫 NF-κB信號通路庫 FDA抗癌藥物庫 | 點(diǎn)擊展開 |
相關(guān)信號通路圖
細(xì)胞實(shí)驗(yàn)數(shù)據(jù)示例
| 細(xì)胞系 | 實(shí)驗(yàn)類型 | 給藥濃度 | 孵育時間 | 活性描述 | 文獻(xiàn)信息(PMID) |
|---|---|---|---|---|---|
| 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 | ||
| 點(diǎn)擊查看更多細(xì)胞系數(shù)據(jù) | |||||
生物活性
| 產(chǎn)品描述 | TPCA-1 (GW683965)是一種IKK-2抑制劑，無細(xì)胞試驗(yàn)中IC50為17.9 nM，抑制NF-κB通路，比作用于IKK-1選擇性高22倍。TPCA-1 也是 STAT3 的抑制劑并可促進(jìn)凋亡。 | ||||||
|---|---|---|---|---|---|---|---|
| 靶點(diǎn) |
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| 體外研究(In Vitro) | ||||
| 體外研究活性 | 在時間分辨熒光能量共振轉(zhuǎn)移試驗(yàn)中，TPCA-1抑制人IKK-2活性，IC50為17.9 nM。TPCA-1被證明是ATP競爭性的。此外，TPCA-1對IKK-1和JNK3分別表現(xiàn)出400 nM和3600 nM的IC50值。TPCA-1濃度依賴性抑制TNF-α，IL-6，和IL-8的產(chǎn)生，IC50值分別為170，290，和320 nM。[1] TPCA-1抑制膠質(zhì)瘤細(xì)胞增殖，以及TNF誘導(dǎo)的RelA (p65)核轉(zhuǎn)運(yùn)和NFκB依賴性IL8基因表達(dá)。重要的是，TPCA-1抑制IFN誘導(dǎo)的基因表達(dá)，完全抑制MX1和GBP1基因表達(dá)，而對ISG15表達(dá)僅具有很小的作用。[2] |
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| 激酶實(shí)驗(yàn) | IKK-2 試驗(yàn) | |||
| 重組人IKK-2 (殘基1-756)在桿狀病毒中以N端GST標(biāo)記的融合蛋白表達(dá)，其活性使用時間分辨熒光共振能量轉(zhuǎn)移測定法進(jìn)行評估。簡而言之，IKK-2 (終濃度5 nM)在試驗(yàn)緩沖液(50 mM HEPES，10 mM MgCl2，1 mM CHAPS，pH 7.4，1 mM DTT 和0.01% w/v BSA)中稀釋，加入包含不同濃度化合物或二甲基亞砜(DMSO)載體(終濃度3%)的孔中。加入總體積為30 μL 的GST-IκBα 底物(終濃度25 nM)/ATP (終濃度1 μM)起始反應(yīng)。反應(yīng)在室溫下培育30分鐘，然后加入15 μL 50 mM EDTA終止。加入包含W-1024銪螯合物標(biāo)記的抗磷酸絲氨酸- IκBα-32/36單克隆抗體12C2，和別藻藍(lán)素標(biāo)記的抗-GST抗體的檢測試劑(15 μL)緩沖液(100 mM HEPES，pH 7.4，150 mM NaCl，和0.1% w/v BSA)，反應(yīng)在室溫下進(jìn)一步培養(yǎng)60分鐘。GST- IκBαis的磷酸化程度以特定665-nm能量轉(zhuǎn)移信號的比率，參考銪620-nm信號，使用Packard探測酶標(biāo)儀測量。 | ||||
| 細(xì)胞實(shí)驗(yàn) | 細(xì)胞系 | U87，MT330，SJ-G2，和 GBM6 人膠質(zhì)瘤細(xì)胞系 | ||
| 濃度 | 0-50 μM | |||
| 孵育時間 | 3天 | |||
| 方法 | 將來自儲備液(10 mg/mL)的10μL 3-(4,5-二甲基噻唑-2)-2,5-二苯基四氮唑溴鹽(MTT)加入包含膠質(zhì)瘤細(xì)胞的96孔板中，并在37 °C下培育2-4小時。氧化的MTT通過將100 μL 10%十二烷基硫酸鈉(SDS)加入0.01 N HCL中溶解，板在37 °C下濕潤的環(huán)境中培養(yǎng)4小時。板于570 nm下在酶標(biāo)儀上讀數(shù)。 |
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| 體內(nèi)研究(In Vivo) | ||
| 體內(nèi)研究活性 | TPCA-1(3, 10, 或20 mg/kg，i.p., b.i.d.)預(yù)防性給藥，導(dǎo)致小鼠體內(nèi)膠原誘導(dǎo)性關(guān)節(jié)炎(CIA)的嚴(yán)重程度劑量依賴性降低。TPCA-1(10 mg/kg, i.p., b.i.d.)導(dǎo)致的顯著降低的疾病嚴(yán)重程度和疾病發(fā)作的延遲與抗風(fēng)濕藥，與每隔一天預(yù)防性給藥的作用相當(dāng)。TPCA-1- 處理的小鼠爪子組織中，p65的細(xì)胞核定位，以及IL-1β，IL-6，TNF-α，和干擾素-γ的水平顯著降低。此外，TPCA-1給藥導(dǎo)致體內(nèi)膠原誘導(dǎo)的T細(xì)胞增殖顯著減少。TPCA-1以20 mg/kg，而不是3或10 mg/kg，i.p.，b.i.d.治療性給藥顯著降低CIA的嚴(yán)重程度。[1] |
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|---|---|---|
| 動物實(shí)驗(yàn) | Animal Models | 患有膠原誘導(dǎo)性關(guān)節(jié)炎的小鼠 |
| Dosages | 3，10，或 20 mg/kg | |
| Administration | 通過腹腔注射給藥，每日兩次 | |
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化學(xué)信息&溶解度
| 分子量 | 279.29 | 分子式 | C12H10FN3O2S |
| CAS號 | 507475-17-4 | SDF | Download TPCA-1 SDF |
| Smiles | C1=CC(=CC=C1C2=CC(=C(S2)NC(=O)N)C(=O)N)F | ||
| 儲存條件(自收到貨起) | |||
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體外溶解度 |
DMSO : 56 mg/mL ( (200.5 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO) Water : Insoluble Ethanol : Insoluble |
摩爾濃度計算器 |
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體內(nèi)溶解配方 現(xiàn)配現(xiàn)用，請按從左到右的順序依次添加，澄清后再加入下一溶劑 |
動物體內(nèi)配方計算器 | |||||
實(shí)驗(yàn)計算
動物體內(nèi)配方計算器（澄清溶液）
第一步：請輸入基本實(shí)驗(yàn)信息（考慮到實(shí)驗(yàn)過程中的損耗，建議多配一只動物的藥量）
mg/kg
g
μL
只
第二步：請輸入動物體內(nèi)配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請聯(lián)系Selleck為您提供正確的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
計算結(jié)果：
工作液濃度： mg/ml；
DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過該批次藥物DMSO溶解度，請先聯(lián)系Selleck）；
體內(nèi)配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH2O，混勻澄清。
體內(nèi)配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。
注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進(jìn)行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。
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