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

GANT61 Chemical Structure

CAS: 500579-04-4

规格 价格 库存 购买数量
10mg 1215.87 现货
50mg 4661.51 现货
1g 24488.1 现货
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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
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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
GLI1 [1]
(HEK293T cells expressing GLI1)
5 μM
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)

体外溶解度
批次:

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

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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