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SANT-1

🥰Excellent
Catalog No. T2450Cas No. 304909-07-7
Alias SANT 1

SANT-1 directly binds to Smoothened (Smo) receptor (Kd: 1.2 nM) and inhibits Smo agonist effects (IC50: 20 nM).

SANT-1

SANT-1

🥰Excellent
Purity: 100%
Catalog No. T2450Alias SANT 1Cas No. 304909-07-7
SANT-1 directly binds to Smoothened (Smo) receptor (Kd: 1.2 nM) and inhibits Smo agonist effects (IC50: 20 nM).
Pack SizePriceAvailabilityQuantity
2 mg$30In Stock
5 mg$48In Stock
10 mg$77In Stock
25 mg$128In Stock
50 mg$207In Stock
100 mg$369In Stock
1 mL x 10 mM (in DMSO)$52In Stock
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Purity:100%
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Product Introduction

Bioactivity
Description
SANT-1 directly binds to Smoothened (Smo) receptor (Kd: 1.2 nM) and inhibits Smo agonist effects (IC50: 20 nM).
Targets&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.
Kinase Assay
CK1 kinase assay: All protein kinase assays (25 μL) are carried out at room temperature (21℃). Assays are performed for 40 min using a Biomek 2000 Laboratory Automation Workstation in a 96-well format. The concentrations of magnesium acetate and [γ-33P]ATP (800 cpm/pmol) in the assays are 10 mM and 0.1 mM, respectively. Assays are initiated with MgATP and stopped by the addition of 5 μL of 0.5 M orthophosphoric acid. Aliquots are then spotted on to P30 ?ltermats, washed four times in 75 mM phosphoric acid to remove ATP, once in methanol, then dried and counted for radioactivity. CK1 δ (5-20 m-units), diluted in 20 mM Hepes, pH 7.5, 0.15 M NaCl, 0.1 mM EGTA, 0.1% (v/v) Triton X-100, 5 mM dithiothreitol, 50% (v/v) glycerol, is assayed against the peptide RRKDLHDDEEDEAMSITA in an incubation containing 20 mM Hepes, pH 7.5, 0.15 M NaCl, 0.1 mM EDTA, 5 mM DTT, 0.1% (v/v) Triton X-100 and 0.5 mM substrate peptide.
AliasSANT 1
Chemical Properties
Molecular Weight373.49
FormulaC23H27N5
Cas No.304909-07-7
SmilesCc1nn(c(C)c1C=NN1CCN(Cc2ccccc2)CC1)-c1ccccc1
Relative Density.1.13 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 18.7 mg/mL (50 mM)
Ethanol: 9.3 mg/mL (25 mM)
Solution Preparation Table
Ethanol/DMSO
1mg5mg10mg50mg
1 mM2.6774 mL13.3872 mL26.7745 mL133.8724 mL
5 mM0.5355 mL2.6774 mL5.3549 mL26.7745 mL
10 mM0.2677 mL1.3387 mL2.6774 mL13.3872 mL
20 mM0.1339 mL0.6694 mL1.3387 mL6.6936 mL
DMSO
1mg5mg10mg50mg
50 mM0.0535 mL0.2677 mL0.5355 mL2.6774 mL

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