GANT61
别名: NSC 136476
GANT61 (NSC 136476)是一种GLI1及GLI2诱导的转录抑制剂，抑制hedgehog，在表达GLI1的HEK293T细胞中IC50为5 μM，选择性作用于其他通路，如TNF和糖皮质激素受体基因的转录。GANT61在LX-2细胞中可诱导凋亡并激活保护性自噬。
GANT61 Chemical Structure
CAS: 500579-04-4
产品质控
批次：
纯度：
99.91%
99.91
GANT61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 |
|---|---|---|---|---|---|
| 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 | ||
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | GANT61 (NSC 136476)是一种GLI1及GLI2诱导的转录抑制剂，抑制hedgehog，在表达GLI1的HEK293T细胞中IC50为5 μM，选择性作用于其他通路，如TNF和糖皮质激素受体基因的转录。GANT61在LX-2细胞中可诱导凋亡并激活保护性自噬。 | ||
|---|---|---|---|
| 靶点 |
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| 体外研究(In Vitro) | ||||
| 体外研究活性 | GANT61抑制GLI1及GLI2诱导的转录。GANT61抑制GLI1的DNA结合能力。GANT61抑制hedgehog信号，IC50为5 μM，比作用于其他通路选择性高，如TNF信号/NFκB激活，糖皮质激素受体基因转录，及Ras-Raf-Mek-Mapk级联。GANT61在体外有效抑制肿瘤细胞增殖，这种作用存在GLI依赖性。[1]GANT61作用于慢性淋巴细胞性白血病细胞（CLL），而非正常的B淋巴细胞，诱导细胞凋亡。[2]GANT61作用于人结肠癌细胞系，具有强大的细胞毒性，且废除集落生成。[3]GANT61作用于人结肠癌细胞系的早S期阶段，抑制DNA复制，产生涉及ATM-Chk2信号轴的DNA损伤信号，且诱导细胞死亡。[4] GANT61 (30 μM)作用于急性髓系白血病（AML）细胞，导致生长停滞和凋亡。[5] | |||
|---|---|---|---|---|
| 激酶实验 | 双荧光素酶含量 | |||
| 转染GLI1表达质粒的HEK293细胞与报告质粒12×GliBSLuc 和R-Luc 一起置于10 cm板上（实验第0天）。24小时后，细胞接种按每孔15,000个细胞的密度接种在白色透明底的96孔板中。细胞粘附，加入溶于DMSO(DMSO终浓度为0.5% ) 的终浓度为10 μM的化合物加（实验第1.5天）。细胞再生长24小时，随后裂解，然后使用双荧光素酶试剂盒进行分析。 | ||||
| 细胞实验 | 细胞系 | PANC1 或 22Rv1 | ||
| 浓度 | ~5 μM | |||
| 孵育时间 | 48 小时 | |||
| 方法 | 进行BrdU渗透实验。在有5 μM 实验化合物 (或 DMSO) 存在下，亚融合的细胞在含FBS(2.5%)的白色透明底的96孔板上生长48小时。随后，使用BrdU对细胞进行标记2小时，混合，然后分析。 | |||
| 实验图片 | 检测方法 | 检测指标 | 实验图片 | PMID |
| Western blot | GLI1 / p-STAT3 / STAT3 / SOCS3 GLI2 / Bcl-2 |
|
27275540 | |
| Immunofluorescence | Gli2 |
|
24533083 | |
| Growth inhibition assay | Cell viability |
|
27275540 | |
| 体内研究(In Vivo) | ||
| 体内研究活性 | GANT61处理注射GLI1-阳性22Rv1前列腺癌细胞的裸鼠，诱导肿瘤生长衰退，直到观察不到明显的肿瘤。[1]GANT61按50 mg/kg剂量口服饲喂处理携带SK-N-AS神经母细胞瘤移植瘤的裸鼠，在实验第12天显著抑制肿瘤生长，与对照组相比，肿瘤体积减少63％。[6] | |
|---|---|---|
| 动物实验 | Animal Models | 携带22Rv1细胞移植瘤的BALB/c裸鼠 |
| Dosages | 50 mg/kg | |
| Administration | 皮下注射 | |
化学信息&溶解度
| 分子量 | 429.6 | 分子式 | C27H35N5 |
| CAS号 | 500579-04-4 | SDF | Download GANT61 SDF |
| Smiles | CN(C)C1=CC=CC=C1CN2CCCN(C2C3=CC=NC=C3)CC4=CC=CC=C4N(C)C | ||
| 储存条件(自收到货起) | |||
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体外溶解度 |
Ethanol : 85 mg/mL (197.85 mM) DMSO : Insoluble ( ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Water : Insoluble |
摩尔浓度计算器 |
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体内溶解配方 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）
mg/kg
g
μL
只
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，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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