GANT 58
Based on 9 publication(s) in Google Scholar
GANT 58 (NSC 75503) is a potent GLI antagonist that inhibits GLI1-induced transcription with IC50 of 5 μM.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.37%
- CAS. Nr.: 64048-12-0
- Formel: C24H16N4S
- Molecular Weight:392.48
-
Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biologische Aktivität
-
Chemical Information
-
Lösungsmittel & Löslichkeit
- Protokoll
- Reinheit & Dokumentation
- Verweise
-
Help & FAQs
-
Stem Cell Signaling Compound Library
HY-L017
-
Wnt/Hedgehog/Notch Compound Library
HY-L020
-
Anti-Cancer Compound Library
HY-L025
-
Anti-Aging Compound Library
HY-L034
-
Transcription Factor-Targeted Library
HY-L090
-
Targeted Diversity Library
HY-L099
-
Anti-Liver Cancer Compound Library
HY-L101
-
Anti-Colorectal Cancer Compound Library
HY-L103
-
Cancer Stem Cells Compound Library
HY-L135
-
Heterocyclic Compound Library
HY-L138
-
Bioactive Compound Library Max
HY-L181
-
MCE Bioactive Compound Library
HY-L001V
-
Bioactive Compound Library
HY-L001
-
High-Throughput Bioactive Compound Library
HY-L205
Publications Citing Use of MedChemExpress (MCE) GANT 58
More- MedComm. 2024 May 13;5(5):e535. [Abstract]
- Cell Death Dis. 2018 May 29;9(6):639. [Abstract]
- Acta Pharmacol Sin. 2026 Mar 11. [Abstract]
- Int J Oncol. 2023 Mar;62(3):43. [Abstract]
- Arthritis Res Ther. 2024 Jan 25;26(1):36. [Abstract]
- J Mol Cell Cardiol. 2022 Oct:171:16-29. [Abstract]
- Biochem Bioph Res Co. 2020 Dec 17;533(4):770-778. [Abstract]
- Elife. 2023 Nov 6:12:e92142. [Abstract]
- bioRxiv. 2023 Feb 7.
Customer Validation & Images
-
IF
Biologische Aktivität
IC50: 5 μM (Gli)[1]
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| Shh Light II | IC50 |
5 μM
Compound: 129, GANT58
|
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] |
GANT58 is a downstream inhibitor of Hh signaling. GANT58 is an indeed inhibitor of Hh signaling downstream of Smo and Sufu. GANT58 mainly acts at the nuclear level because transcription induced by GLI1 with a mutated nuclear export signal is still blocked. GANT58 efficiently inhibits in vitro tumor cell proliferation in a GLI-dependent manner and successfully blocks cell growth using human prostate cancer cells harboring downstream activation of the Hh pathway[1].
GANT58 (NSC75503) has been shown to inhibit transcriptional activation by GLI1 (as well as by the other GLI species). GANT58 has been shown to inhibit GLI transactivation[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
-
CAS. Nr. 64048-12-0
-
Appearance Solid
-
Molecular Weight 392.48
-
Formel C24H16N4S
-
Color Light yellow to yellow
-
SMILES
C1(C2=C(C(C3=CC=NC=C3)=C(S2)C4=CC=NC=C4)C5=CC=NC=C5)=CC=NC=C1
-
Synonyms
NSC 75503
-
Versand
Room temperature in continental US; may vary elsewhere.
-
Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (9)
-
Journal Impact Factor
-
Most Recent
-
MedComm
Transcription factor EHF drives cholangiocarcinoma development through transcriptional activation of glioma-associated oncogene homolog 1 and chemokine CCL2. [Abstract]2024 May 13;5(5):e535. PMID: 38741887 -
Cell Death Dis
The hedgehog and Wnt/β-catenin system machinery mediate myofibroblast differentiation of LR-MSCs in pulmonary fibrogenesis. [Abstract]2018 May 29;9(6):639. PMID: 29844390
GANT 58 purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2018 May 29;9(6):639. [Abstract]
The expression of α-SMA and Collagen I is determined by immunofluorescence staining. Lung-resident mesenchymal stem cells (LR-MSCs) are cultured with TGF-β1 for 7 days, along with or without the treatment of GANT58 (10 μM).
-
Acta Pharmacol Sin
2026 Mar 11. PMID: 41813972 -
Int J Oncol
Keratin19 promotes pancreatic cancer progression and poor prognosis via activating the Hedgehog pathway. [Abstract]2023 Mar;62(3):43. PMID: 36825581 -
Arthritis Res Ther
Endoplasmic reticulum aminopeptidase 2 regulates CD4+ T cells pyroptosis in rheumatoid arthritis. [Abstract]2024 Jan 25;26(1):36. PMID: 38273310 -
J Mol Cell Cardiol
Induction of GLI1 by miR-27b-3p/FBXW7/KLF5 pathway contributes to pulmonary arterial hypertension. [Abstract]2022 Oct:171:16-29. PMID: 35810662 -
Biochem Bioph Res Co
Microcystin-leucine-arginine induces liver fibrosis by activating the Hedgehog pathway in hepatic stellate cells. [Abstract]2020 Dec 17;533(4):770-778. PMID: 32988585 -
Elife
GLI1 facilitates collagen-induced arthritis in mice by collaborative regulation of DNA methyltransferases. [Abstract]2023 Nov 6:12:e92142. PMID: 37929702 -
Lösungsmittel & Löslichkeit
Ethanol : 20 mg/mL (50.96 mM; Need ultrasonic)
DMSO : 9.09 mg/mL (23.16 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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.
Add each solvent one by one: 10% EtOH 40% PEG300 5% Tween-80 45% Saline
Solubility: 2 mg/mL (5.10 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2 mg/mL.
Taking 1 mL working solution as an example, add 100 μL EtOH stock solution (20.0 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.
Add each solvent one by one: 10% EtOH 90% (20% SBE-β-CD in Saline)
Solubility: 2 mg/mL (5.10 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2 mg/mL.
Taking 1 mL working solution as an example, add 100 μL EtOH stock solution (20.0 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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 0.91 mg/mL (2.32 mM); Clear solution
This protocol yields a clear solution of ≥ 0.91 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (9.1 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 0.91 mg/mL (2.32 mM); Clear solution
This protocol yields a clear solution of ≥ 0.91 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (9.1 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.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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.
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protokoll
HEK293 cells are transfected with GLI1 expression plasmid, together with the reporter plasmids 12× GliBS-Luc and R-Luc on 10 cm plates (day 0). Twenty-four hours later, cells are seeded in white 96 well plates with clear bottom at a density of 15,000 cells per well. Cells are allowed to attach, and compounds are added at a final concentration of 10 μM in DMSO (0.5% final DMSO concentration) (day 1.5). Cells are grown for another 24 h, subsequently lysed, and then analyzed by using the Dual Luciferase kit. Plates are read on a Berthold Technologies microplate luminometer. Subconfluent cells are grown in reduced FBS (2.5%) for 48 h in the presence of 5 μM test compound (or DMSO) on white 96 well plates with clear bottom. Subsequently, cells are labeled for 2 h with BrdU, fixed, and analyzed. Samples are read on a Molecular Devices SpectraMax Gemini EM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice[1]
5×106 22Rv1 cells are suspended in a total volume of 100 μL of a 1:1 mixture of RPMI medium 1640:Matrigel (E1270). The cell suspension is injected s.c. at the posterior flank of female BALB/c nude mice (nu/nu). Tumors are grown until they reached a median size of ≈250 mm3 (5-6 days). Animals are randomly divided into four groups (n=4-5) and treated with solvent only (corn oil:ethanol, 4:1) or compounds in solvent (50 mg/kg) for 16 days s.c. injections of compounds are performed several centimeters away from the tumor. Tumor volumes are calculated by the formula length×width×0.5×(length+width). At the end of the treatment period, animals are given a BrdU pulse (50 mg/kg) for 30 min, and tumors are removed. All animal experiments are approved by local ethics authorities.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Reinheit & Dokumentation
-
Data Sheet (287 KB)
-
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
-
Handling Instructions (2659 KB)
Verweise
[1]. Lauth M, et al. Inhibition of GLI-mediated transcription and tumor cell growth by small-molecule antagonists. Proc Natl Acad Sci U S A. 2007 May 15;104(20):8455-60. [Content Brief]
[2]. Joo J, et al. GLI1 is a central mediator of EWS/FLI1 signaling in Ewing tumors. PLoS One. 2009 Oct 27;4(10):e7608. [Content Brief]
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO / Ethanol | 1 mM | 2.5479 mL | 12.7395 mL | 25.4790 mL | 63.6975 mL |
| 5 mM | 0.5096 mL | 2.5479 mL | 5.0958 mL | 12.7395 mL | |
| 10 mM | 0.2548 mL | 1.2740 mL | 2.5479 mL | 6.3698 mL | |
| 15 mM | 0.1699 mL | 0.8493 mL | 1.6986 mL | 4.2465 mL | |
| 20 mM | 0.1274 mL | 0.6370 mL | 1.2740 mL | 3.1849 mL | |
| Ethanol | 25 mM | 0.1019 mL | 0.5096 mL | 1.0192 mL | 2.5479 mL |
| 30 mM | 0.0849 mL | 0.4247 mL | 0.8493 mL | 2.1233 mL | |
| 40 mM | 0.0637 mL | 0.3185 mL | 0.6370 mL | 1.5924 mL | |
| 50 mM | 0.0510 mL | 0.2548 mL | 0.5096 mL | 1.2740 mL |
GANT 58 Related Classifications
HY-13282 Related Classifications
Powered by Bioz