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GANT 58

GANT 58
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Purity:99.88%
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GANT 58

Catalog No. T15370Cas No. 64048-12-0
GANT 58 (NSC-75503) is a potent antagonist of Gli. Which inhibits GLI1-induced transcription (IC50: 5 μM).
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Pack SizePriceAvailabilityQuantity
5 mg$40In Stock
10 mg$64In Stock
25 mg$119In Stock
50 mg$197In Stock
100 mg$318In Stock
1 mL x 10 mM (in DMSO)$44In Stock
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Product Introduction

Bioactivity
Description
GANT 58 (NSC-75503) is a potent antagonist of Gli. Which inhibits GLI1-induced transcription (IC50: 5 μM).
In vitro
GANT58 is a downstream inhibitor of Hh signaling and it also is an indeed inhibitor of Hh signaling downstream of Smo and Sufu. GANT58 potently 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 has been shown to inhibit transcriptional activation by GLI1 (as well as by the other GLI species) and it has been shown to inhibit GLI transactivation[2]. GANT58 mainly acts at the nuclear level because transcription induced by GLI1 with a mutated nuclear export signal is still blocked.
In vivo
Nude mice are treated with every second-day s.c. injections at a concentration of 50 mg/kg of cyclopamine, GANT61, GANT58, or solvent only (n=4-5 for each group). Although mice treated with these compounds showed no such signs of toxicity, this protocol is also introduced for the GANTs to be able to compare all compounds. All injections are done 2-3 cm away from the tumors. Suppression of tumor cell growth is observed for all compounds, during an 18-day treatment period. Treatment with cyclopamine or GANT58 results in the inhibition of additional xenograft growth and limited the increase in tumor size[1].
AliasNSC 75503
Chemical Properties
Molecular Weight392.48
FormulaC24H16N4S
Cas No.64048-12-0
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 9.09 mg/mL (23.16 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.5479 mL12.7395 mL25.4790 mL127.3950 mL
5 mM0.5096 mL2.5479 mL5.0958 mL25.4790 mL
10 mM0.2548 mL1.2740 mL2.5479 mL12.7395 mL
20 mM0.1274 mL0.6370 mL1.2740 mL6.3698 mL

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