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Description: Inhibitor of hedgehog (Hh) signaling; antagonizes smoothened activity
Chemical Name: N-[(3,5-dimethyl-1-phenyl-1H-pyrazol-4-yl)methylene]-4-(phenylmethyl)-1-piperazinamine
Purity: ≥98% (HPLC)
Biological Activity for SANT-1
SANT-1 is a potent, cell-permeable inhibitor of Sonic hedgehog (Shh) signaling; high affinity antagonist of smoothened activity (KD = 1.2 nM). Inhibits smoothened agonist effects with an IC50 of 20 nM (in Shh-LIGHT2 cells). Has been used in protocols to generate pancreatic β cells from hPSCs.
For more information about how SANT-1 may be used, see our protocol: Generation of β cells from hPSCs
Compound Libraries for SANT-1
SANT-1 is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Stem Cell Library. Find out more about compound libraries available from Tocris.
Technical Data for SANT-1
| M. Wt | 373.5 |
| Formula | C23H27N5 |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 304909-07-7 |
| PubChem ID | 6878030 |
| InChI Key | FOORCIAZMIWALX-JJIBRWJFSA-N |
| Smiles | CC1=NN(C(C)=C1\C=N\N1CCN(CC2=CC=CC=C2)CC1)C1=CC=CC=C1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for SANT-1
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 18.68 | 50 |
Preparing Stock Solutions for SANT-1
The following data is based on the product molecular weight 373.5. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.5 mM | 5.35 mL | 26.77 mL | 53.55 mL |
| 2.5 mM | 1.07 mL | 5.35 mL | 10.71 mL |
| 5 mM | 0.54 mL | 2.68 mL | 5.35 mL |
| 25 mM | 0.11 mL | 0.54 mL | 1.07 mL |
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Product Datasheets for SANT-1
References for SANT-1
References are publications that support the biological activity of the product.
Chen et al (2002) Small molecule modulation of smoothened activity. Proc.Natl.Acad.Sci.USA. 99 1407
If you know of a relevant reference for SANT-1, please let us know.
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Keywords: SANT-1, SANT-1 supplier, inhibitors, inhibits, hedgehog, Hh, signaling, antagonizes, smoothened, activity, Signaling, Signalling, Smo, Receptors, antagonist, Hedgehog, Smoothened, Organoids, 1974, Tocris Bioscience
10 Citations for SANT-1
Citations are publications that use Tocris products. Selected citations for SANT-1 include:
Hoch et al (2015) MRT-92 inhibits Hedgehog signaling by blocking overlapping binding sites in the transmembrane domain of the Smoothened receptor. FASEB J 29 1817 PMID: 25636740
Atwood et al (2013) GLI activation by atypical protein kinase C Ι/λ regulates the growth of basal cell carcinomas. Stem Cell Reports 494 484 PMID: 23446420
Strating et al (2015) Itraconazole inhibits enterovirus replication by targeting the oxysterol-binding protein. Cell Rep 10 600 PMID: 25640182
Fleury et al (2016) Hedgehog associated to microparticles inhibits adipocyte differentiation via a non-canonical pathway. Sci Rep 6 23479 PMID: 27010359
Wang et al (2012) Glucocorticoid compounds modify smoothened localization and hedgehog pathway activity. Chem Biol 19 972 PMID: 22921064
Yung et al (2019) Sufu- And Spop-mediated downregulation of Hedgehog signaling promotes beta cell differentiation through organ-specific niche signals. Nat.Commun. 10 4647 PMID: 31604927
Yuan et al (2016) Ciliary IFT80 balances canonical versus non-canonical hedgehog signalling for osteoblast differentiation. Nat Commun 21 11024 PMID: 26996322
Nostro et al (2015) Efficient generation of NKX6-1+ pancreatic progenitors from multiple human pluripotent stem cell lines. Neuropsychopharmacology 4 591 PMID: 25843049
Sambathkumar et al (2018) Generation of hepatocyte- and endocrine pancreatic-like cells from human induced endodermal progenitor cells. PLoS One 13 e0197046 PMID: 29750821
Krentz et al (2017) Phosphorylation of NEUROG3 Links Endocrine Differentiation to the Cell Cycle in Pancreatic Progenitors. Dev Cell 41 129 PMID: 28441528
Do you know of a great paper that uses SANT-1 from Tocris? Please let us know.
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Protocols for SANT-1
The following protocol features additional information for the use of SANT-1 (Cat. No. 1974).
Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
Stem Cell Research Product Guide
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