Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C23H27N5 |
| Molecular Weight | 373.494 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 1 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
CC1=NN(C(C)=C1\C=N\N2CCN(CC3=CC=CC=C3)CC2)C4=CC=CC=C4
InChI
InChIKey=FOORCIAZMIWALX-JJIBRWJFSA-N
InChI=1S/C23H27N5/c1-19-23(20(2)28(25-19)22-11-7-4-8-12-22)17-24-27-15-13-26(14-16-27)18-21-9-5-3-6-10-21/h3-12,17H,13-16,18H2,1-2H3/b24-17+
DescriptionSources: https://www.ncbi.nlm.nih.gov/pubmed/12391318Curator's Comment: Description was created based on several sources, including https://www.ncbi.nlm.nih.gov/pubmed/19421011 | https://www.ncbi.nlm.nih.gov/pubmed/26943330 | https://www.ncbi.nlm.nih.gov/pubmed/26781311 | https://www.ncbi.nlm.nih.gov/pubmed/23548480
Sources: https://www.ncbi.nlm.nih.gov/pubmed/12391318
Curator's Comment: Description was created based on several sources, including https://www.ncbi.nlm.nih.gov/pubmed/19421011 | https://www.ncbi.nlm.nih.gov/pubmed/26943330 | https://www.ncbi.nlm.nih.gov/pubmed/26781311 | https://www.ncbi.nlm.nih.gov/pubmed/23548480
SANT-1 is antagonist of Smoothened (Smo), a distant relative of G protein-coupled receptors, mediates Hedgehog (Hh) signaling during embryonic development and can initiate or transmit ligand-independent pathway activation in tumorigenesis. It suppressed cancer cell viability, proliferation and colony formation.
Originator
Sources: https://www.ncbi.nlm.nih.gov/pubmed/12391318
Curator's Comment: 2002
Approval Year
PubMed
| Title | Date | PubMed |
|---|---|---|
| Silibinin Treatment Inhibits the Growth of Hedgehog Inhibitor-Resistant Basal Cell Carcinoma Cells via Targeting EGFR-MAPK-Akt and Hedgehog Signaling. | 2017-07 |
|
| Targeting hedgehog signaling pathway in pediatric tumors: in vitro evaluation of SMO and GLI inhibitors. | 2016-03 |
|
| Blockade of Hedgehog Signaling Synergistically Increases Sensitivity to Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitors in Non-Small-Cell Lung Cancer Cell Lines. | 2016 |
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| The presence of primary cilia in cancer cells does not predict responsiveness to modulation of smoothened activity. | 2015-07 |
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| Structural basis for Smoothened receptor modulation and chemoresistance to anticancer drugs. | 2014-07-10 |
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| CDO, an Hh-coreceptor, mediates lung cancer cell proliferation and tumorigenicity through Hedgehog signaling. | 2014 |
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| Guggulsterone sensitizes glioblastoma cells to Sonic hedgehog inhibitor SANT-1 induced apoptosis in a Ras/NFκB dependent manner. | 2013-08-19 |
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| Sonic hedgehog antagonists induce cell death in acute myeloid leukemia cells with the presence of lipopolysaccharides, tumor necrosis factor-α, or interferons. | 2013-08 |
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| Pituitary adenylyl cyclase activating polypeptide inhibits gli1 gene expression and proliferation in primary medulloblastoma derived tumorsphere cultures. | 2010-12-09 |
|
| Small-molecule modulators of the Sonic Hedgehog signaling pathway. | 2010-01 |
|
| Combined targeting of histone deacetylases and hedgehog signaling enhances cytoxicity in pancreatic cancer. | 2009-07 |
|
| Evidence for allosteric interactions of antagonist binding to the smoothened receptor. | 2009-06 |
|
| Smoothened adopts multiple active and inactive conformations capable of trafficking to the primary cilium. | 2009 |
|
| Identification and characterization of Hedgehog modulator properties after functional coupling of Smoothened to G15. | 2006-10-20 |
|
| Small molecule modulation of Smoothened activity. | 2002-10-29 |
Sample Use Guides
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/26781311
SMO inhibition in a panel of 18 tumor cell lines by SANT1 moderately decreased cell viability with GI50s between 28 and 93 uM
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GYK6BKF2M2
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304909-07-7
Created by
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6878030
Created by
admin on Wed Apr 02 18:07:32 GMT 2025 , Edited by admin on Wed Apr 02 18:07:32 GMT 2025
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SUBSTANCE RECORD