SANT-1

SKU: orb1305467

Description

SANT-1 is a potent and selective small molecule antagonist of the Smoothened (Smo) receptor, binding with high affinity (Kd: 1.2 nM) and effectively blocking agonist activity (IC50: 20 nM). This inhibitor is a valuable chemical tool for investigating Hedgehog signaling pathway mechanisms in both cellular and animal models of cancer and developmental biology.

Research Area

Pharmacology & Drug Discovery, Stem Cell & Developmental Biology

Key Properties

• CAS Number: 304909-07-7
• MW: 373.49
• Purity: >99.99% (May vary between batches)
• Formula: C₂₃H₂₇N₅
• SMILES: Cc1nn(c(C)c1C=NN1CCN(Cc2ccccc2)CC1)-c1ccccc1
• Target: Hedgehog/Smoothened,Smo
• Solubility: DMSO:18.7 mg/mL (50.07 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (5.35 mM);Ethanol:9.3 mg/mL (24.9 mM)

Bioactivity

• Target IC50:
  Smo receptor:1.2 Nm
• In Vivo:
  SANT-1 inhibits the transportation of Smo (stimulated by PKA) to the proximal cilia. It equally suppresses both the wild-type and oncogenic forms of Smo. In SmoA1-LIGHT2 cells, SANT-1 impedes pathway activation, displaying similar efficacy to that observed in the Shh-LIGHT2 experiments. Distinct inhibitory activities of SANT-1 are evident in both Shh-LIGHT2 and BODIPY-Cyclopamine studies, where it notably blocks the SAG-modulated pathway activation. Additionally, when used in combination with SAHA, SANT-1 curtails cell proliferation and effectively inhibits colony formation in the pancreatic cancer cell lines Panc-1 and BxPC-3, offering a counteraction to gemcitabine resistance.

Storage & Handling

• Storage: store at low temperature | 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

inhibit, Inhibitor, Hedgehog, Smo, Smoothened, SANT1, SANT-1, SANT 1

Compound Identifiers

PubChem CID

1356208