Date published: 2026-5-13

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SANT-1 (CAS 304909-07-7)

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Alternate Names:
(4-Benzyl-piperazin-1-yl)-(3,5-dimethyl-1-phenyl-1H-pyrazol-4-ylmethylene)-amine
Application:
SANT-1 is a Smo inhibitor and Sonic Hedgehog signaling pathway antagonist
CAS Number:
304909-07-7
Purity:
>95%
Molecular Weight:
373.49
Molecular Formula:
C23H27N5
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.

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SANT-1, a member of the santacruz compound family, is a small molecule inhibitor that specifically targets protein kinase C (PKC), an enzyme involved in various cellular processes. This inhibitor has gained significant attention in scientific research due to its ability to selectively target and modulate specific proteins. One of SANT-1′s notable actions is its role as a membrane-permeable antagonist of the Shh (Sonic Hedgehog) signaling pathway. By directly binding to Smo (Smoothened), SANT-1 effectively inhibits Smo in both oncogenic and wild-type forms. Furthermore, when combined with the HDAC inhibitor SAHA, SANT-1 demonstrates promising suppression of cellular proliferation and colony formation in Gemcitabine-resistant pancreatic adenocarcinoma cell lines Panc-1 and BxPC-3. In addition to its impact on the Shh signaling pathway, SANT-1 may act to modulate the activity of various proteins involved in cellular processes like cell cycle regulation, apoptosis, and inflammation. It also influences the activity of enzymes participating in metabolic processes, including fatty acid oxidation and glycolysis. The mechanism of SANT-1 involves acting as a competitive inhibitor of SANT-1 itself. By binding to the active site of the enzyme, it effectively blocks the substrate from binding, leading to the inhibition of the enzyme′s activity.


SANT-1 (CAS 304909-07-7) References

  1. Small molecule modulation of Smoothened activity.  |  Chen, JK., et al. 2002. Proc Natl Acad Sci U S A. 99: 14071-6. PMID: 12391318
  2. Small-molecule modulators of Hedgehog signaling: identification and characterization of Smoothened agonists and antagonists.  |  Frank-Kamenetsky, M., et al. 2002. J Biol. 1: 10. PMID: 12437772
  3. The Terminal acidic SANT 1 (Tacs1) gene of maize is expressed in tissues containing meristems and encodes an acidic SANT domain similar to some chromatin-remodeling complex proteins.  |  Marian, CO. and Bass, HW. 2005. Biochim Biophys Acta. 1727: 81-6. PMID: 15716051
  4. Evidence for allosteric interactions of antagonist binding to the smoothened receptor.  |  Rominger, CM., et al. 2009. J Pharmacol Exp Ther. 329: 995-1005. PMID: 19304771
  5. Smoothened adopts multiple active and inactive conformations capable of trafficking to the primary cilium.  |  Wilson, CW., et al. 2009. PLoS One. 4: e5182. PMID: 19365551
  6. Combined targeting of histone deacetylases and hedgehog signaling enhances cytoxicity in pancreatic cancer.  |  Chun, SG., et al. 2009. Cancer Biol Ther. 8: 1328-39. PMID: 19421011
  7. Guggulsterone sensitizes glioblastoma cells to Sonic hedgehog inhibitor SANT-1 induced apoptosis in a Ras/NFκB dependent manner.  |  Dixit, D., et al. 2013. Cancer Lett. 336: 347-58. PMID: 23548480
  8. Synthesis and cytotoxicity studies of Hedgehog enzyme inhibitors SANT-1 and GANT-61 as anticancer agents.  |  Chenna, V., et al. 2014. J Environ Sci Health A Tox Hazard Subst Environ Eng. 49: 641-7. PMID: 24521409
  9. Silibinin Treatment Inhibits the Growth of Hedgehog Inhibitor-Resistant Basal Cell Carcinoma Cells via Targeting EGFR-MAPK-Akt and Hedgehog Signaling.  |  Dheeraj, A., et al. 2017. Photochem Photobiol. 93: 999-1007. PMID: 28120452
  10. Efficient Differentiation of Pluripotent Stem Cells to NKX6-1+ Pancreatic Progenitors.  |  McGaugh, EC. and Nostro, MC. 2017. J Vis Exp.. PMID: 28362406
  11. Protective effect of sonic hedgehog signaling pathway activation on acute myocardial infarction.  |  Li, SJ., et al. 2020. J Biol Regul Homeost Agents. 34: 367-378. PMID: 32515175
  12. Nanog promotes stem-like traits of glioblastoma cells.  |  Yuan, Y., et al. 2021. Front Biosci (Landmark Ed). 26: 552-565. PMID: 33049683
  13. Solubilization, purification, and ligand binding characterization of G protein-coupled receptor SMO in native membrane bilayer using styrene maleic acid copolymer.  |  Zhu, L., et al. 2022. PeerJ. 10: e13381. PMID: 35529497

Ordering Information

Product NameCatalog #UNITPriceQtyFAVORITES

SANT-1, 5 mg

sc-203253
5 mg
$135.00