GANT 61 (Synonyms: NSC 136476)

目录号: HY-13901 纯度: ≥98.0%: FAQs
Data Sheet SDS COA 产品使用指南

摩尔计算器

GANT 61 是靶向 Hedgehog /GLi 通路的 Gli1 和 Gli2 抑制剂。

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GANT 61 Chemical Structure

CAS No. : 500579-04-4

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规格	价格	是否有货
10 mM * 1 mL in DMSO	￥767	In-stock
1 mg	￥316	In-stock
5 mg	￥697	In-stock
10 mg	￥1083	In-stock
50 mg	￥4201	In-stock
100 mg		询价
200 mg		询价

or 大包装询价

* Please select Quantity before adding items.

Customer Review

MCE 顾客使用本产品发表的 54 篇科研文献

Proliferation Assay

: GANT 61 purchased from MCE. Usage Cited in: Cancer Lett. 2018 Apr 28;420:195-207. [Abstract]; Shh-Light 2 cells are transfected with Gli1 or Gli2 plasmids and the expression of proteins are analyzed by Western blot. Positive control JQ1, CBC and CBD inhibit Gli1 and Gli2 overexpression induced Gli luciferase activity, GDC-0499 and GANT61 have no effects.

: GANT 61 purchased from MCE. Usage Cited in: Front Pharmacol. 2018 Jun 26;9:674. [Abstract]; Cyclopamine and GANT61 decrease the level of Gli1 as evidenced by western blot.

: GANT 61 purchased from MCE. Usage Cited in: Cancer Med. 2018 Nov;7(11):5704-5715. [Abstract]; The Hh signaling pathway is involved in DHA induced inhibition of cell proliferation. A and B, CCK8 assay of SKOV3 and SKOV3-IP cells is conducted following treatment with purmorphamine, DHA or a combination of DHA and purmorphamine for 48 h. C and D, SKOV3 and SKOV3‐IP cells are treated with GANT61, DHA, or a combination of DHA and GATN61 for 48 h, while controls are treated with DMSO. CCK8 assay is used to analyze cell viability of SKOV3 and SKOV3-IP cells.

: GANT 61 purchased from MCE. Usage Cited in: Chinese Pharmacological Bulletin. 2018, 34(9): 1235-1242.; Expression of Gli1/2 (A) and DNA damage proteins (B) at OGD 6 h detected by Western blot.

: GANT 61 purchased from MCE. Usage Cited in: Cancer Lett. 2017 Jan 28;385:128-136. [Abstract]; GANT61 or SHH siRNA treatment alone moderately increases LC3-II, and LC3-II increased in cells co-treated with R51211 and GANT61 or SHH siRNA.

: GANT 61 purchased from MCE. Usage Cited in: ACS Appl Mater Interfaces. 2017 Dec 13;9(49):42544-42555. [Abstract]; ATG101 cross-talk with the hedgehog pathway modulates hypoxia-induced HPAEC cell proliferation and apoptosis. Effects of ssATG101-TNP on the hedgehog pathway. HPAECs are pretreated with ssATG101-TNP and GANT61; then, they are under hypoxia for 24 h.

: GANT 61 purchased from MCE. Usage Cited in: Life Sci. 2017 Dec 15;191:82-89. [Abstract]; ORS cells are exposed to 3% oxygen for 48 h in presence or absence of Shh pathway inhibitor cyclopamine (5 μM) or GANT61 (10 μM). Immunofluorescence assay using anti-PCNA antibody is performed to detect the proliferative ORS cells (red). Cell nuclei are counterstained with DAPI (blue).

: GANT 61 purchased from MCE. Usage Cited in: Cancer Sci. 2017 May;108(5):918-930. [Abstract]; Effects of E2 and GANT61 on the protein expression levels of GLI1 and GLI2 in MCF-7 cells. The expression levels are measured with a western blotting as described in the Materials and Methods.

: GANT 61 purchased from MCE. Usage Cited in: Breast Cancer. 2017 Sep;24(5):683-693. [Abstract]; Effects of GANT61 (0-20μM) on the expression levels of survivin in MDA-MB-231 cells. The cells are treated with the indicated concentrations of GANT61 for two days. The expression levels are tested using western blotting. The deduced molecular weight of surviving is approximately 16 kDa.

: GANT 61 purchased from MCE. Usage Cited in: Birla Institute of Technology, University of Colorado. 2016 Aug.; Western blot analyses of whole cell lysates (WCLs) collected from MCF7-Ctrl cells cultured in MCF7-Ctrl and Six1 CM for 48 hrs treated with GANT61 or vehicle.

: GANT 61 purchased from MCE. Usage Cited in: Oncotarget. 2015 Nov 3;6(34):36700-12. [Abstract]; BE2-M17 NB cells are incubated with GANT-61 (0–40 μM) for 3 days. The cell viability is monitored using an MTS assay. The expression levels of N-myc and INSM1 in the cells treated with 20 μM of GANT-61 is determined by Western blot analysis. Actin is used as a loading control.

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生物活性
实验参考方法
纯度 & 产品资料
参考文献

生物活性

GANT 61 is an inhibitor of Gli1 and Gli2 targeting the Hedgehog/GLI pathway.

IC₅₀ & Target

Gli1/2^[1]

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
HeLa	IC₅₀	6.83 μM Compound: GANT61	Inhibition of Ebolavirus glycoprotein/matrix protein VP40 entry in human HeLa cells after 4.5 hrs beta-lactamase reporter assay Inhibition of Ebolavirus glycoprotein/matrix protein VP40 entry in human HeLa cells after 4.5 hrs beta-lactamase reporter assay	[PMID: 29624387]
IMR-32	GI₅₀	5.82 μM Compound: 32, GANT-61	Cytotoxicity against human IMR32 cells after 72 hrs by fluorometric microculture cytotoxicity assay Cytotoxicity against human IMR32 cells after 72 hrs by fluorometric microculture cytotoxicity assay	10.1039/C3MD00334E
NIH3T3	EC₅₀	5 μM Compound: 4; GANT-61	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 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	[PMID: 26976215]
Shh Light II	IC₅₀	5 μM Compound: 128, GANT61	Inhibition of SHH in mouse Shh Light2 cells by GLI-responsive firefly luciferase reporter gene assay Inhibition of SHH in mouse Shh Light2 cells by GLI-responsive firefly luciferase reporter gene assay	[PMID: 19309080]
SH-SY5Y	GI₅₀	5.82 μM Compound: 32, GANT-61	Cytotoxicity against human SH-SY5Y cells after 72 hrs by fluorometric microculture cytotoxicity assay Cytotoxicity against human SH-SY5Y cells after 72 hrs by fluorometric microculture cytotoxicity assay	10.1039/C3MD00334E
SK-N-AS	GI₅₀	5.82 μM Compound: 32, GANT-61	Cytotoxicity against human SK-N-AS cells after 72 hrs by fluorometric microculture cytotoxicity assay Cytotoxicity against human SK-N-AS cells after 72 hrs by fluorometric microculture cytotoxicity assay	10.1039/C3MD00334E
SK-N-DZ	GI₅₀	5.82 μM Compound: 32, GANT-61	Cytotoxicity against human SK-N-DZ cells after 72 hrs by fluorometric microculture cytotoxicity assay Cytotoxicity against human SK-N-DZ cells after 72 hrs by fluorometric microculture cytotoxicity assay	10.1039/C3MD00334E
SK-N-FI	GI₅₀	5.82 μM Compound: 32, GANT-61	Cytotoxicity against human SK-N-FI cells after 72 hrs by fluorometric microculture cytotoxicity assay Cytotoxicity against human SK-N-FI cells after 72 hrs by fluorometric microculture cytotoxicity assay	10.1039/C3MD00334E
SK-N-SH	GI₅₀	5.82 μM Compound: 32, GANT-61	Cytotoxicity against human SK-N-SH cells after 72 hrs by fluorometric microculture cytotoxicity assay Cytotoxicity against human SK-N-SH cells after 72 hrs by fluorometric microculture cytotoxicity assay	10.1039/C3MD00334E

体外研究
(In Vitro)

GANT61 (20 μM) 比靶向 Smo (环巴胺) 诱导更多的细胞死亡。GANT61 (0，5，10，20 μM) 抑制人结肠癌细胞系的克隆形成存活。GANT61 (20 μM，0-72 小时) 下调 HT29 细胞中的 Gli1 和 Gli2 表达。GANT61 (0、10 μM 或 20 μM) 差异调节参与细胞死亡和细胞存活之间平衡的基因^[1]。
GANT-61 抑制细胞活力并诱导胰腺 CSC 细胞凋亡。GANT-61 抑制 Shh 通路下游靶标的表达，降低胰腺 CSC 中的 Gli-DNA 相互作用、Gli 转录活性和 Gli 核转位。GANT-61 差异调节参与细胞存活、细胞死亡和多能性的基因。GANT-61 抑制 CSCs 的运动、侵袭和迁移^[2]。
在测试的神经母细胞瘤细胞系中，GANT61 敏感性与 GLI1 呈正相关，与 MYCN 表达呈负相关。GANT61 下调 GLI1、c-MYC、MYCN 和 Cyclin D1 的表达并诱导神经母细胞瘤细胞凋亡^[3]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

GANT-61 (40 mg/kg，腹腔注射，每周三天) 抑制 NOD/SCID IL2Rγ 缺失小鼠的 CSC 肿瘤生长^[2]。
GANT61 (50 mg/kg，口服) 以相加或协同的方式增强用于处理神经母细胞瘤的化疗药物的作用，并减少裸鼠体内已建立的神经母细胞瘤异种移植物的生长^[3]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

429.60

Formula

C₂₇H₃₅N₅

CAS 号

500579-04-4

性状

固体

颜色

White to light yellow

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

细胞实验：

Ethanol 中的溶解度 : 66.67 mg/mL (155.19 mM; 超声助溶)

DMSO 中的溶解度 : 25 mg/mL (58.19 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.3277 mL	11.6387 mL	23.2775 mL
5 mM	0.4655 mL	2.3277 mL	4.6555 mL
10 mM	0.2328 mL	1.1639 mL	2.3277 mL

查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

摩尔计算器
稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

浓度 _(start)

体积 _(start)

浓度 _(final)

体积 _(final)

动物实验：

请根据您的实验动物和给药方式选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

方案一

请依序添加每种溶剂： 10% EtOH 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 5 mg/mL (11.64 mM); 澄清溶液

此方案可获得 ≥ 5 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 50.0 mg/mL 的澄清 EtOH 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水定容至 1 mL。
生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
方案二

请依序添加每种溶剂： 10% EtOH 90% (20% SBE-β-CD in Saline)
Solubility: 5 mg/mL (11.64 mM); 悬浊液; 超声助溶

此方案可获得 5 mg/mL的均匀悬浊液，悬浊液可用于口服和腹腔注射。
以 1 mL 工作液为例，取 100 μL 50.0 mg/mL 的澄清 EtOH 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。
方案三

请依序添加每种溶剂： 10% EtOH 90% Corn Oil
Solubility: ≥ 5 mg/mL (11.64 mM); 澄清溶液

此方案可获得 ≥ 5 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。
以 1 mL 工作液为例，取 100 μL 50.0 mg/mL 的澄清 EtOH 储备液加到 900 μL 玉米油中，混合均匀。
方案四

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.82 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水定容至 1 mL。
生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
方案五

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (5.82 mM); 悬浊液; 超声助溶

此方案可获得 2.5 mg/mL的均匀悬浊液，悬浊液可用于口服和腹腔注射。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。
方案六

请依序添加每种溶剂： 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (5.82 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。
方案七

请依序添加每种溶剂： 5% DMSO 40% PEG300 5% Tween-80 50% Saline
Solubility: ≥ 2.5 mg/mL (5.82 mM); 澄清溶液
方案八

请依序添加每种溶剂： 5% DMSO 95% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (5.82 mM); 悬浊液; 超声助溶

动物溶解方案计算器

请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

每只动物的给药体积

μL

动物数量

只

由于实验过程有损耗，建议您多配一只动物的量

请输入您的动物体内配方组成：

DMSO +

Tween-80 +

Saline

如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。

方案所需 助溶剂 包括：DMSO，，均可在 MCE 网站选购。，Tween 80，均可在 MCE 网站选购。

计算结果

工作液所需浓度 : mg/mL

储备液配制方法 : mg 药物溶于 μL DMSO（母液浓度为 mg/mL）。

您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。

动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。

连续给药周期超过半月以上，请谨慎选择该方案。

请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热（超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。

纯度 & 产品资料

纯度: ≥98.0%

选择批次：

Data Sheet (657 KB) SDS (393 KB)

COA (294 KB) HNMR (270 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Mazumdar T, et al. Hedgehog signaling drives cellular survival in human colon carcinoma cells. Cancer Res. 2011 Feb 1;71(3):1092-102. [Content Brief]

[2]. Fu J, et al. GANT-61 inhibits pancreatic cancer stem cell growth in vitro and in NOD/SCID/IL2R gamma null mice xenograft. Cancer Lett. 2013 Mar 1;330(1):22-32. [Content Brief]

[3]. Wickstrom M, et al. Targeting the hedgehog signal transduction pathway at the level of GLI inhibits neuroblastoma cell growth in vitro and in vivo. Int J Cancer. 2013 Apr 1;132(7):1516-24. [Content Brief]

Cell Assay ^[2]	Cells (1.5×10⁴) are incubated with 0, 1, 5 and 10 μM of GANT-61 in 250 μL of culture medium in 96-well plate for 48 and 72 h. Cell viability is determined by the XTT assay. In brief, a freshly prepared XTT-PMS labeling mixture (50 μL) is added to the cell culture. The absorbance is measured at 450 nm with λ correction at 650 nm. The cell viability is expressed as ΔOD (OD450 − OD650). The apoptosis is determined by FACS analysis of propidium iodide (PI)-stained cells. In brief, cells are trypsinized, washed with PBS and resuspended in 200 μL PBS with 10 μL RNAase (10 mg/mL) and incubated at 37°C for 30 min. After incubation, 50 μL PI solution is added and cells are analyzed for apoptosis using a flow cytometry. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[2]	Humanized NOD/SCID/IL2Rgammanull mice are used for the assay. Before CSC’s injection, mice are humanized with tail vein injection of human normal CD34⁺ peripheral blood stem/progenitor cells. CD34⁺peripheral blood stem/progenitor cells (500 cells/mouse, 50-75 μL volume) are injected through tail vein. After 3 days, human pancreatic CSCs (1×10³ cells mixed with Matrigel, Becton Dickinson, Bedford, MA, in 75 μL total volume, 50:50 ratio) are injected subcutaneously into the flanks of NOD/SCID IL2Rγnull mice (4–6 weeks old). After two weeks of CSC implantation, mice (10 mice per group) are treated with GANT-61(0 and 40 mg/kg body weight) ip three times per week for 6 weeks. At the end of the experiment, mice are euthanized, and tumors are isolated for biochemical analysis. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[1]. Mazumdar T, et al. Hedgehog signaling drives cellular survival in human colon carcinoma cells. Cancer Res. 2011 Feb 1;71(3):1092-102. [Content Brief] [2]. Fu J, et al. GANT-61 inhibits pancreatic cancer stem cell growth in vitro and in NOD/SCID/IL2R gamma null mice xenograft. Cancer Lett. 2013 Mar 1;330(1):22-32. [Content Brief] [3]. Wickstrom M, et al. Targeting the hedgehog signal transduction pathway at the level of GLI inhibits neuroblastoma cell growth in vitro and in vivo. Int J Cancer. 2013 Apr 1;132(7):1516-24. [Content Brief]

GANT 61 相关分类

完整储备液配制表

可选溶剂	浓度溶剂体积质量	1 mg	5 mg	10 mg	25 mg

DMSO / Ethanol	1 mM	2.3277 mL	11.6387 mL	23.2775 mL	58.1937 mL
	5 mM	0.4655 mL	2.3277 mL	4.6555 mL	11.6387 mL
	10 mM	0.2328 mL	1.1639 mL	2.3277 mL	5.8194 mL
	15 mM	0.1552 mL	0.7759 mL	1.5518 mL	3.8796 mL
	20 mM	0.1164 mL	0.5819 mL	1.1639 mL	2.9097 mL
	25 mM	0.0931 mL	0.4655 mL	0.9311 mL	2.3277 mL
	30 mM	0.0776 mL	0.3880 mL	0.7759 mL	1.9398 mL
	40 mM	0.0582 mL	0.2910 mL	0.5819 mL	1.4548 mL
	50 mM	0.0466 mL	0.2328 mL	0.4655 mL	1.1639 mL
Ethanol	60 mM	0.0388 mL	0.1940 mL	0.3880 mL	0.9699 mL
	80 mM	0.0291 mL	0.1455 mL	0.2910 mL	0.7274 mL
	100 mM	0.0233 mL	0.1164 mL	0.2328 mL	0.5819 mL

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

GANT 61500579-04-4NSC 136476GANT61GANT-61NSC136476NSC-136476GliAutophagyInhibitorinhibitorinhibit

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GANT 61 (Synonyms: NSC 136476)

Customer Review

MCE 顾客使用本产品发表的 54 篇科研文献

GANT 61 相关产品

•相关化合物库:

•同靶点产品:

•同靶点蛋白产品:

生物活性

实验参考方法

纯度 & 产品资料

参考文献

摩尔计算器

稀释计算器

GANT 61 相关分类

完整储备液配制表

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GANT 61 (Synonyms: NSC 136476)

Customer Review

GANT 61 相关抗体

MCE 顾客使用本产品发表的 54 篇科研文献

GANT 61 相关产品

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生物活性

实验参考方法

纯度 & 产品资料

参考文献

GANT 61 相关抗体:

摩尔计算器

稀释计算器

GANT 61 相关分类

完整储备液配制表

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