GANT 58 是GLI拮抗剂，能够抑制 GLI1 诱导的转录，其IC50=5 μM。

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

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.

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].

64048-12-0

C24H16N4S

392.48

NSC 75503;4,44乔,4乔(2,3,4,5-Thiophentetrayl)tetrakis-pyridine

DMSO:9.09 mg/mL (23.16 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years