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GANT61
僅限科研使用
GANT61
別名: NSC 136476
GANT61 (NSC 136476)是一種GLI1及GLI2誘導的轉(zhuǎn)錄抑制劑，抑制hedgehog，在表達GLI1的HEK293T細胞中IC50為5 μM，選擇性作用于其他通路，如TNF和糖皮質(zhì)激素受體基因的轉(zhuǎn)錄。GANT61在LX-2細胞中可誘導凋亡并激活保護性自噬。
GANT61 Chemical Structure
CAS: 500579-04-4
產(chǎn)品質(zhì)控
批次：
純度：
99.91%
99.91
GANT61相關產(chǎn)品
相關信號通路圖
細胞實驗數(shù)據(jù)示例
| 細胞系 | 實驗類型 | 給藥濃度 | 孵育時間 | 活性描述 | 文獻信息 |
|---|---|---|---|---|---|
| 22Rv | Antitumor assay | 50 mg/kg | 18 days | Antitumor activity in GLI1 positive human 22Rv cells xenografted mouse model at 50 mg/kg, sc after 18 days | 17494766 |
| NIH3T3 | Function assay | 10 uM | Inhibition of Hedgehog/Gli1 mediated transformation in mouse NIH3T3 cells at 10 uM | 17494766 | |
| PANC1 | Function assay | 5 uM | Reduction in GLI1 expression in human PANC1 cells at 5 uM | 17494766 | |
| PANC1 | Function assay | 5 uM | Reduction in PTCH expression in human PANC1 cells at 5 uM | 17494766 | |
| 22Rv | Function assay | 5 uM | Reduction in GlI1 expression in human 22Rv cells at 5 uM | 17494766 | |
| 22Rv | Function assay | 5 uM | Reduction in PTCH expression in human 22Rv cells at 5 uM | 17494766 | |
| HEK293 | Function assay | 30 uM | Inhibition of GLI (unknown origin) expressed in HEK293 cells assessed as reduction in GLI-mediated transcription at 30 uM | 25581017 | |
| TM3 | Function assay | 48 hrs | Inhibition of Hh signaling pathway in mouse TM3 cells assessed as downregulation of Gli1 gene expression after 48 hrs by luciferase reporter gene assay, EC50 = 9.27 μM. | 26976215 | |
| HeLa | Function assay | 4.5 hrs | Inhibition of Ebolavirus glycoprotein/matrix protein VP40 entry in human HeLa cells after 4.5 hrs beta-lactamase reporter assay, IC50 = 6.83 μM. | 29624387 | |
| Rh30 | Function assay | 24 hrs | Inhibition of human Gli1-mediated transcriptional activity in human Rh30 cells after 24 hrs by luciferase reporter gene assay, IC50 = 40 μM. | 20605720 | |
| SK-N-DZ | Cytotoxicity assay | 72 hrs | Cytotoxicity against human SK-N-DZ cells after 72 hrs by fluorometric microculture cytotoxicity assay, GI50 = 5.82 μM. | ChEMBL | |
| SK-N-SH | Cytotoxicity assay | 72 hrs | Cytotoxicity against human SK-N-SH cells after 72 hrs by fluorometric microculture cytotoxicity assay, GI50 = 5.82 μM. | ChEMBL | |
| SK-N-FI | Cytotoxicity assay | 72 hrs | Cytotoxicity against human SK-N-FI cells after 72 hrs by fluorometric microculture cytotoxicity assay, GI50 = 5.82 μM. | ChEMBL | |
| SK-N-AS | Cytotoxicity assay | 72 hrs | Cytotoxicity against human SK-N-AS cells after 72 hrs by fluorometric microculture cytotoxicity assay, GI50 = 5.82 μM. | ChEMBL | |
| IMR32 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human IMR32 cells after 72 hrs by fluorometric microculture cytotoxicity assay, GI50 = 5.82 μM. | ChEMBL | |
| SK-N-BE(2) | Cytotoxicity assay | 72 hrs | Cytotoxicity against human SK-N-BE(2) cells after 72 hrs by fluorometric microculture cytotoxicity assay, GI50 = 5.82 μM. | ChEMBL | |
| SH-SY5Y | Cytotoxicity assay | 72 hrs | Cytotoxicity against human SH-SY5Y cells after 72 hrs by fluorometric microculture cytotoxicity assay, GI50 = 5.82 μM. | ChEMBL | |
| NIH 3T3 | Function assay | Inhibition of Hh signaling pathway in Shh-LIGHT2 incorporated mouse NIH 3T3 cells assessed as downregulation of Gli1 gene expression by luciferase reporter gene assay, EC50 = 5 μM. | 26976215 | ||
| Shh-L2 | Function assay | Inhibition of Hedgehog signaling in human Shh-L2 cells, IC50 = 5 μM. | 17494766 | ||
| Shh Light2 | Function assay | Inhibition of SHH in mouse Shh Light2 cells by GLI-responsive firefly luciferase reporter gene assay, IC50 = 5 μM. | 19309080 | ||
| HEK293 | Function assay | Reduction of GLI2 mediated transcription in HEK293 cells by luciferase reporter assay | 17494766 | ||
| NIH3T3 | Function assay | Inhibition of GLI1 induced hedgehog signaling in mouse NIH3T3 cells | 17494766 | ||
| HEK293 | Function assay | Inhibition of beta galactosidase in HEK293 cells | 17494766 | ||
| MEF | Function assay | Reduction in expression of Hedgehog target gene Hip1 in Sufu deficient mouse MEF cells | 17494766 | ||
| 22Rv | Function assay | Reduction of expression of PTCH mRNA in human 22Rv cells | 17494766 | ||
| HEK293 | Function assay | Inhibition of nuclear accumulation of GLI mutant in HEK293 cells | 17494766 | ||
| HEK293 | Function assay | Inhibition of nuclear accumulation of wild type GLI in HEK293 cells | 17494766 | ||
| HEK293 | Function assay | Reduction of GLI1 mediated transcription in HEK293 cells by luciferase reporter assay | 17494766 | ||
| 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 | ||
| NB-EBc1 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 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 | ||
| 點擊查看更多細胞系數(shù)據(jù) | |||||
生物活性
| 產(chǎn)品描述 | GANT61 (NSC 136476)是一種GLI1及GLI2誘導的轉(zhuǎn)錄抑制劑，抑制hedgehog，在表達GLI1的HEK293T細胞中IC50為5 μM，選擇性作用于其他通路，如TNF和糖皮質(zhì)激素受體基因的轉(zhuǎn)錄。GANT61在LX-2細胞中可誘導凋亡并激活保護性自噬。 | ||
|---|---|---|---|
| 靶點 |
|
| 體外研究(In Vitro) | ||||
| 體外研究活性 | GANT61抑制GLI1及GLI2誘導的轉(zhuǎn)錄。GANT61抑制GLI1的DNA結(jié)合能力。GANT61抑制hedgehog信號，IC50為5 μM，比作用于其他通路選擇性高，如TNF信號/NFκB激活，糖皮質(zhì)激素受體基因轉(zhuǎn)錄，及Ras-Raf-Mek-Mapk級聯(lián)。GANT61在體外有效抑制腫瘤細胞增殖，這種作用存在GLI依賴性。[1]GANT61作用于慢性淋巴細胞性白血病細胞（CLL），而非正常的B淋巴細胞，誘導細胞凋亡。[2]GANT61作用于人結(jié)腸癌細胞系，具有強大的細胞毒性，且廢除集落生成。[3]GANT61作用于人結(jié)腸癌細胞系的早S期階段，抑制DNA復制，產(chǎn)生涉及ATM-Chk2信號軸的DNA損傷信號，且誘導細胞死亡。[4] GANT61 (30 μM)作用于急性髓系白血病（AML）細胞，導致生長停滯和凋亡。[5] | |||
|---|---|---|---|---|
| 激酶實驗 | 雙熒光素酶含量 | |||
| 轉(zhuǎn)染GLI1表達質(zhì)粒的HEK293細胞與報告質(zhì)粒12×GliBSLuc 和R-Luc 一起置于10 cm板上（實驗第0天）。24小時后，細胞接種按每孔15,000個細胞的密度接種在白色透明底的96孔板中。細胞粘附，加入溶于DMSO(DMSO終濃度為0.5% ) 的終濃度為10 μM的化合物加（實驗第1.5天）。細胞再生長24小時，隨后裂解，然后使用雙熒光素酶試劑盒進行分析。 | ||||
| 細胞實驗 | 細胞系 | PANC1 或 22Rv1 | ||
| 濃度 | ~5 μM | |||
| 孵育時間 | 48 小時 | |||
| 方法 | 進行BrdU滲透實驗。在有5 μM 實驗化合物 (或 DMSO) 存在下，亞融合的細胞在含F(xiàn)BS(2.5%)的白色透明底的96孔板上生長48小時。隨后，使用BrdU對細胞進行標記2小時，混合，然后分析。 | |||
| 實驗圖片 | 檢測方法 | 檢測指標 | 實驗圖片 | PMID |
| Western blot | GLI1 / p-STAT3 / STAT3 / SOCS3 GLI2 / Bcl-2 |
|
27275540 | |
| Immunofluorescence | Gli2 |
|
24533083 | |
| Growth inhibition assay | Cell viability |
|
27275540 | |
| 體內(nèi)研究(In Vivo) | ||
| 體內(nèi)研究活性 | GANT61處理注射GLI1-陽性22Rv1前列腺癌細胞的裸鼠，誘導腫瘤生長衰退，直到觀察不到明顯的腫瘤。[1]GANT61按50 mg/kg劑量口服飼喂處理攜帶SK-N-AS神經(jīng)母細胞瘤移植瘤的裸鼠，在實驗第12天顯著抑制腫瘤生長，與對照組相比，腫瘤體積減少63％。[6] | |
|---|---|---|
| 動物實驗 | Animal Models | 攜帶22Rv1細胞移植瘤的BALB/c裸鼠 |
| Dosages | 50 mg/kg | |
| Administration | 皮下注射 | |
化學信息&溶解度
| 分子量 | 429.6 | 分子式 | C27H35N5 |
| CAS號 | 500579-04-4 | SDF | Download GANT61 SDF |
| Smiles | CN(C)C1=CC=CC=C1CN2CCCN(C2C3=CC=NC=C3)CC4=CC=CC=C4N(C)C | ||
| 儲存條件(自收到貨起) | |||
|
體外溶解度 |
Ethanol : 85 mg/mL (197.85 mM) DMSO : Insoluble ( ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO) Water : Insoluble |
摩爾濃度計算器 |
|
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 | |||||
實驗計算
動物體內(nèi)配方計算器（澄清溶液）
第一步：請輸入基本實驗信息（考慮到實驗過程中的損耗，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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