- 抑制劑
- 化合物庫
- 抗體
- 生物試劑
- qPCR
- 2x SYBR Green qPCR Master Mix
- 2x SYBR Green qPCR Master Mix(Low ROX)
- 2x SYBR Green qPCR Master Mix(High ROX)
- 蛋白實(shí)驗(yàn)
- Protein A/G免疫沉淀磁珠
- Anti-DYKDDDDK Tag免疫磁珠
- Anti-DYKDDDDK Tag親和凝膠
- Anti-Myc免疫磁珠
- Anti-HA免疫磁珠
- 磁力架
- Poly DYKDDDDK Tag多肽
- 細(xì)胞核與細(xì)胞漿蛋白抽提試劑盒
- 免疫磁珠
- 蛋白酶抑制劑Cocktail
- 蛋白酶抑制劑Cocktail(DMSO儲液)
- 磷酸酶抑制劑Cocktail
- 細(xì)胞實(shí)驗(yàn)
- Cell Counting Kit-8 (CCK-8)
- 動(dòng)物實(shí)驗(yàn)
- 鼠尾直接PCR試劑盒(快速基因型鑒定)
- 小鼠CD3+ T細(xì)胞分選試劑盒
- 小鼠CD4+ T細(xì)胞分選試劑盒
- 小鼠CD8+ T細(xì)胞分選試劑盒
- 新產(chǎn)品
- 聯(lián)系我們
Home
Stem Cells & Wnt
Hedgehog/Smoothened inhibitor
-
Apoptosis related activator
-
Autophagy activator
GANT61
僅限科研使用
GANT61
別名: NSC 136476
GANT61 (NSC 136476)是一種GLI1及GLI2誘導(dǎo)的轉(zhuǎn)錄抑制劑，抑制hedgehog，在表達(dá)GLI1的HEK293T細(xì)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(xì)胞中可誘導(dǎo)凋亡并激活保護(hù)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(guān)產(chǎn)品
| 相關(guān)靶點(diǎn) | Hedgehog Smoothened GLI | 點(diǎn)擊展開 |
|---|---|---|
| 相關(guān)產(chǎn)品 | Cyclopamine SAG Hydrochloride Purmorphamine SANT-1 SAG (Smoothened Agonist) BMS-833923 Taladegib (LY2940680) HPI-4 (Ciliobrevin A) PF-5274857 Jervine Ciliobrevin D MK-4101 JK184 | 點(diǎn)擊展開 |
| 相關(guān)化合物庫 | 激酶抑制劑庫 FDA藥物庫 干細(xì)胞小分子化合物庫 GPCR小分子化合物庫 干細(xì)胞分化化合物庫 | 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(shí)間 | 活性描述 | 文獻(xiàn)信息(PMID) |
|---|---|---|---|---|---|
| 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(diǎn)擊查看更多細(xì)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(dǎo)的轉(zhuǎn)錄抑制劑，抑制hedgehog，在表達(dá)GLI1的HEK293T細(xì)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(xì)胞中可誘導(dǎo)凋亡并激活保護(hù)性自噬。 | ||
|---|---|---|---|
| 靶點(diǎn) |
|
| 體外研究(In Vitro) | ||||
| 體外研究活性 | GANT61抑制GLI1及GLI2誘導(dǎo)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(xì)胞增殖，這種作用存在GLI依賴性。[1]GANT61作用于慢性淋巴細(xì)胞性白血病細(xì)胞（CLL），而非正常的B淋巴細(xì)胞，誘導(dǎo)細(xì)胞凋亡。[2]GANT61作用于人結(jié)腸癌細(xì)胞系，具有強(qiáng)大的細(xì)胞毒性，且廢除集落生成。[3]GANT61作用于人結(jié)腸癌細(xì)胞系的早S期階段，抑制DNA復(fù)制，產(chǎn)生涉及ATM-Chk2信號軸的DNA損傷信號，且誘導(dǎo)細(xì)胞死亡。[4] GANT61 (30 μM)作用于急性髓系白血病（AML）細(xì)胞，導(dǎo)致生長停滯和凋亡。[5] | |||
|---|---|---|---|---|
| 激酶實(shí)驗(yàn) | 雙熒光素酶含量 | |||
| 轉(zhuǎn)染GLI1表達(dá)質(zhì)粒的HEK293細(xì)胞與報(bào)告質(zhì)粒12×GliBSLuc 和R-Luc 一起置于10 cm板上（實(shí)驗(yàn)第0天）。24小時(shí)后，細(xì)胞接種按每孔15,000個(gè)細(xì)胞的密度接種在白色透明底的96孔板中。細(xì)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(shí)驗(yàn)第1.5天）。細(xì)胞再生長24小時(shí)，隨后裂解，然后使用雙熒光素酶試劑盒進(jìn)行分析。 | ||||
| 細(xì)胞實(shí)驗(yàn) | 細(xì)胞系 | PANC1 或 22Rv1 | ||
| 濃度 | ~5 μM | |||
| 孵育時(shí)間 | 48 小時(shí) | |||
| 方法 | 進(jìn)行BrdU滲透實(shí)驗(yàn)。在有5 μM 實(shí)驗(yàn)化合物 (或 DMSO) 存在下，亞融合的細(xì)胞在含F(xiàn)BS(2.5%)的白色透明底的96孔板上生長48小時(shí)。隨后，使用BrdU對細(xì)胞進(jìn)行標(biāo)記2小時(shí)，混合，然后分析。 | |||
| 實(shí)驗(yàn)圖片 | 檢測方法 | 檢測指標(biāo) | 實(shí)驗(yàn)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(xì)胞的裸鼠，誘導(dǎo)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(xì)胞瘤移植瘤的裸鼠，在實(shí)驗(yàn)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(dòng)物實(shí)驗(yàn) | Animal Models | 攜帶22Rv1細(xì)胞移植瘤的BALB/c裸鼠 |
| Dosages | 50 mg/kg | |
| Administration | 皮下注射 | |
|
化學(xué)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(jì)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(dòng)物體內(nèi)配方計(jì)算器 | |||||
實(shí)驗(yàn)計(jì)算
摩爾濃度計(jì)算器
動(dòng)物體內(nèi)配方計(jì)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(dòng)物的藥量）
mg/kg
g
μL
只
第二步：請輸入動(dòng)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(jì)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。
技術(shù)支持
在訂購、運(yùn)輸、儲存和使用我們的產(chǎn)品的任何階段，您遇到的任何問題，均可以通過撥打我們的熱線電話400-668-6834，或者技術(shù)支持郵箱[email protected]，直接聯(lián)系到我們。我們會在24小時(shí)內(nèi)盡快聯(lián)系您。
如果有其他問題，請給我們留言。
* 必填項(xiàng)
