GANT 58

SKU: orb1308281

Description

GANT 58 (NSC-75503) is a small molecule inhibitor that potently antagonizes the Gli transcription factor, specifically blocking GLI1-mediated transcriptional activity with an IC50 of 5 μM. This compound is a valuable research tool for studying Hedgehog signaling in cancer biology and has been utilized in both in vitro and in vivo experimental models.

Research Area

Pharmacology & Drug Discovery, Stem Cell & Developmental Biology

Key Properties

• CAS Number: 64048-12-0
• MW: 392.48
• Purity: 99.88%
• Formula: C₂₄H₁₆N₄S
• SMILES: c1cc(ccn1)-c1sc(c(c1-c1ccncc1)-c1ccncc1)-c1ccncc1
• Target: Hedgehog/Smoothened
• Solubility: 10% DMSO+40% PEG300+5% Tween-80+45% Saline:0.5 mg/mL (1.27 mM);DMSO:9.09 mg/mL (23.16 mM)

Bioactivity

• Target IC50:
  GLI:5 μM
• 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.
• 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. 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. GANT58 mainly acts at the nuclear level because transcription induced by GLI1 with a mutated nuclear export signal is still blocked.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Smoothened, Gli, Inhibitor, Hedgehog, GANT 58, GANT58, GANT-58, inhibit, NSC 75503, NSC75503, NSC-75503

Compound Identifiers

PubChem CID

253078