SANT-1Shh inhibitor,potent and cell-permeable CAS# 304909-07-7 |
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Quality Control & MSDS
Number of papers citing our products
Chemical structure
3D structure
| Cas No. | 304909-07-7 | SDF | Download SDF |
| PubChem ID | 6878030 | Appearance | Powder |
| Formula | C23H27N5 | M.Wt | 373.5 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | DMSO : 62.5 mg/mL (167.34 mM; Need ultrasonic) | ||
| Chemical Name | (E)-N-(4-benzylpiperazin-1-yl)-1-(3,5-dimethyl-1-phenylpyrazol-4-yl)methanimine | ||
| SMILES | CC1=C(C(=NN1C2=CC=CC=C2)C)C=NN3CCN(CC3)CC4=CC=CC=C4 | ||
| Standard InChIKey | FOORCIAZMIWALX-JJIBRWJFSA-N | ||
| Standard InChI | 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+ | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | 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). |
SANT-1 Dilution Calculator
SANT-1 Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.6774 mL | 13.3869 mL | 26.7738 mL | 53.5475 mL | 66.9344 mL |
| 5 mM | 0.5355 mL | 2.6774 mL | 5.3548 mL | 10.7095 mL | 13.3869 mL |
| 10 mM | 0.2677 mL | 1.3387 mL | 2.6774 mL | 5.3548 mL | 6.6934 mL |
| 50 mM | 0.0535 mL | 0.2677 mL | 0.5355 mL | 1.071 mL | 1.3387 mL |
| 100 mM | 0.0268 mL | 0.1339 mL | 0.2677 mL | 0.5355 mL | 0.6693 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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SANT-1 is a novel molecule that has anti-tumour effect through its ability to bind to smoothened protein [1] .
Smoothened is one of the two types of two integral membrane proteins that regulate the activation of Hh pathway, a process that direct cellular differentiation and proliferation[1]. In addition, abnormities function of Smoothened was linked to occurrence of tumor genesis in human[1].
SANT-1 is one of the 4 Smoothened antagonists during high-throughput assay and is the molecules that have the highest antagonist effect to Smoothened protein[1]. In two healthy cell lines (Shh-LIGHT2 nM and SmoA1-LIGHT2 cell lines) , SANT-1 was able to inhibited both cells after 30 hrs of incubation with a IC50 value of 20 and 30 nM, respectively[1]. In addition, SANT-1 has the highest affinity toward Smoothened among 4 molecules, having an apparent KDs of 1.2 nM[1]. In tumor pancreas cancer cell line, SANT-1 inhibited Panc-1 cell lines with an IC50 value of 100 µM after incubation. In addition, a combination application of SANT-1 and SAHA (histone deacetylase inhibitor) enhancement the anti-tumor effectives of treatment as a result of their cooperative suppression of the Hh pathway activity[2].
No in vivo test has been carried out on SANT-1.
References:
[1]. Chen J K., Taipale J, Young K E,. Small molecule modulation of Smoothened activity. Proc Natl Acad Sci U S A, 2002, 99: 14071-6.
[2]. Chun SG, Zhou W & Yee N S. Combined targeting of histone deacetylases and hedgehog signaling enhances cytoxicity in pancreatic cancer. Cancer Biol Ther, 2009, 8: 1328-39.
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Guggulsterone sensitizes glioblastoma cells to Sonic hedgehog inhibitor SANT-1 induced apoptosis in a Ras/NFkappaB dependent manner.[Pubmed:23548480]
Cancer Lett. 2013 Aug 19;336(2):347-58.
Since Shh pathway effector, Gli1, is overexpressed in gliomas, we investigated the effect of novel Shh inhibitor SANT-1 on glioma cell viability. Though SANT-1 failed to induce apoptosis, it reduced proliferation of glioma stem-like cells. Apart from canonical Shh cascade, Gli1 is also induced by non-canonical pathways including NFkappaB. Therefore, a combinatorial strategy with Ras/NFkappaB inhibitor, Guggulsterone, was employed to enhance effectiveness of SANT-1. Guggulsterone inhibited Ras and NFkappaB activity and sensitized cells to SANT-1 induced apoptosis via intrinsic apoptotic mechanism. Inhibition of either Ras or NFkappaB activity was sufficient to sensitize cells to SANT-1. Guggulsterone induced ERK activation also contributed to Caspase-9 activation. Since SANT-1 and Guggulsterone differentially target stem-like and non-stem glioma cells respectively, this combination warrants investigation as an effective anti-glioma therapy.
Synthesis and cytotoxicity studies of Hedgehog enzyme inhibitors SANT-1 and GANT-61 as anticancer agents.[Pubmed:24521409]
J Environ Sci Health A Tox Hazard Subst Environ Eng. 2014;49(6):641-7.
Cancer-related death is one of the most common causes of mortality in society. Small molecules have the capability to disrupt aberrant signaling pathways in tumors, leading to anticancer activities. Therefore the search for new molecules for cancer treatment continues to draw attention to the scientific research community. Synthesis and biological evaluation of hedgehog (Hh) pathway inhibitors SANT-1 and GANT-61 are disclosed. These molecules have been synthesized from common precursors using simple conversions, our synthesis features Vils-Meier-Haack reaction, imine formation reaction and N-arylation reaction. These drugs were evaluated using a Hh reporter assay to confirm pathway inhibitory activity, and tested for cell viability against pancreatic and prostate cancer cells. These methodologies can be applied to make potent analogs of both inhibitors.
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.[Pubmed:15716051]
Biochim Biophys Acta. 2005 Feb 14;1727(2):81-6.
While screening for plant homologs of telomeric-complex proteins, we isolated a cDNA for the Terminal acidic SANT 1 (Tacs1) gene of maize, encoding a 45-kDa protein with a C-terminal Myb/SANT-like domain. Gene expression and protein modeling data indicate that the TACS1 protein may function in chromatin remodeling within shoot primordia or other meristem-containing tissues.
