Reactivos e instrumentos para inmunología, biología celular y biología molecular.

GANT 61 [500579-04-4]

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Referencia HY-13901-1mL

embalaje : 10mM/1mL

Marca : MedChemExpress

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Descripciòn

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

IC₅₀ & Target

Gli1/2^[1]

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

In Vitro

GANT61 (20 μM) induces greater cell death than targeting Smo (cyclopamine). GANT61 (0, 5, 10, 20 μM) inhibits clonogenic survival of human colon carcinoma cell lines. GANT61 (20 μM, 0-72 hr) down-regulates Gli1 and Gli2 expression in HT29 cells. GANT61 (0, 10 μM or 20 μM) differentially regulates genes involved in the balance between cell death and cell survival^[1].
GANT-61 inhibits cell viability and induces apoptosis in pancreatic CSCs. GANT-61 inhibits expression of downstream targets of Shh pathway, decreases Gli-DNA interaction, Gli transcriptional activity and Gli nuclear translocation in pancreatic CSCs. GANT-61 differentially regulates genes involved in cell survival, cell death and pluripotency. GANT-61 inhibits motility, invasion and migration of CSCs^[2].
GANT61 sensitivity positively correlates to GLI1 and negatively to MYCN expression in the neuroblastoma cell lines tested. GANT61 downregulates GLI1, c-MYC, MYCN and Cyclin D1 expression and induces apoptosis of neuroblastoma cells^[3].

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

Solvente y solubilidad

In Vitro:

Ethanol : 66.67 mg/mL (155.19 mM; Need ultrasonic)

DMSO : 25 mg/mL (58.19 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	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

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% EtOH 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 5 mg/mL (11.64 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL EtOH stock solution (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% EtOH 90% (20% SBE-β-CD in Saline)
Solubility: 5 mg/mL (11.64 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL EtOH stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% EtOH 90% Corn Oil
Solubility: ≥ 5 mg/mL (11.64 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL EtOH stock solution (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.
Protocol 4

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.82 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 5

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (5.82 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 6

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (5.82 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.
Protocol 7

Add each solvent one by one: 5% DMSO 40% PEG300 5% Tween-80 50% Saline
Solubility: ≥ 2.5 mg/mL (5.82 mM); Clear solution
Protocol 8

Add each solvent one by one: 5% DMSO 95% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (5.82 mM); Suspended solution; Need ultrasonic

Pureza y Documentación

Purity: 99.80%

Ficha de datos (286 KB) SDS (393 KB)

COA (256 KB) HNMR (272 KB) RP-HPLC (254 KB) MS (68 KB)

Instrucciones de manejo (2659 KB)

Referencias

[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]

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GANT 61 [500579-04-4]

Referencia HY-13901-1mL

Marca : MedChemExpress

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