GANT 61

SKU: orb1304571

Description

GANT61 is a small molecule inhibitor that selectively targets the Gli1 and Gli2 transcription factors within the Hedgehog signaling pathway. It is widely used in both in vitro and in vivo research to study cancers and developmental disorders associated with aberrant Hedgehog signaling.

Research Area

Cell Biology, Pharmacology & Drug Discovery, Stem Cell & Developmental Biology

Key Properties

• CAS Number: 500579-04-4
• MW: 429.6
• Purity: 97.59%
• Formula: C₂₇H₃₅N₅
• SMILES: CN(C)c1ccccc1CN1CCCN(Cc2ccccc2N(C)C)C1c1ccncc1
• Target: Autophagy,Hedgehog/Smoothened
• Solubility: Ethanol:43 mg/mL (100.09 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:1 mg/mL (2.33 mM);DMSO:25 mg/mL (58.19 mM)

Bioactivity

• Target IC50:
  GLI1:5 μM
• In Vivo:
  GANT61 effectively inhibits tumor cell proliferation in vitro through a GLI-dependent mechanism. At a concentration of 30μM, GANT61 halts growth and induces apoptosis in acute myeloid leukemia cells. It exhibits potent cytotoxicity towards human colon cancer cell lines, eradicating colony formation. GANT61 specifically targets chronic lymphocytic leukemia cells over normal B lymphocytes, triggering apoptosis. In the early S phase of human colon cancer cell lines, GANT61 induces DNA replication inhibition leading to DNA damage signaling through the ATM-Chk2 axis and consequent cell death. Furthermore, GANT61 inhibits GLI1's DNA binding capability and suppresses the hedgehog signaling pathway with an IC50 of 5μM, displaying higher selectivity over other pathways (such as TNF signaling/NFκB activation, glucocorticoid receptor gene transcription, and the Ras-Raf-Mek-Mapk cascade).
• In Vitro:
  Nude mice bearing SK-N-AS neuroblastoma xenografts administered orally with 50 mg/kg GANT61 exhibited significant tumor growth inhibition on day 12 of the experiment, achieving a 63% reduction in tumor volume compared to the control group. Additionally, in nude mice injected with GLI1-positive 22Rv1 prostate cancer cells, GANT61 induced tumor regression to the point where no discernible tumors were observed.
• Cell Research:
  BrdU Incorporation Assay. 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.(Only for Reference)

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

Autophagy, inhibit, NSC136476, NSC-136476, NSC 136476, Gli, GLI1, Hedgehog, GANT 61, GANT61, GANT-61, Inhibitor, Smoothened

Compound Identifiers

PubChem CID

421610