GPCR/G Protein Hedgehog/Smoothened GANT 58


Catalog No. T15370   CAS 64048-12-0
Synonyms: NSC 75503

GANT 58 is a potent antagonist of Gli. Which inhibits GLI1-induced transcription (IC50: 5 μM).

GANT 58, CAS 64048-12-0
Pack Size Availability Price/USD Quantity
5 mg In stock 55.00
10 mg In stock 85.00
25 mg In stock 186.00
50 mg In stock 295.00
100 mg In stock 473.00
1 mL * 10 mM (in DMSO) In stock 66.00
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Purity 99.88%
Biological Description
Chemical Properties
Storage & Solubility Information
Description GANT 58 is a potent antagonist of Gli. Which inhibits GLI1-induced transcription (IC50: 5 μM).
Targets&IC50 Gli : 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].
Synonyms NSC 75503
Purity 99.88%
Molecular Weight 392.48
Formula C24H16N4S
CAS No. 64048-12-0


0-4℃ for short term (days to weeks), or -20℃ for long term (months).

Solubility Information

DMSO: 9.09 mg/mL (23.16 mM), Need ultrasonic

( < 1 mg/ml refers to the product slightly soluble or insoluble )


References and Literature
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. 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.

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