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SANT-1

Catalog No. T2450   CAS 304909-07-7
Synonyms: SANT 1

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

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SANT-1 Chemical Structure
SANT-1, CAS 304909-07-7
Pack Size Availability Price/USD Quantity
2 mg In stock $ 30.00
5 mg In stock $ 48.00
10 mg In stock $ 77.00
25 mg In stock $ 128.00
50 mg In stock $ 207.00
100 mg In stock $ 369.00
1 mL * 10 mM (in DMSO) In stock $ 52.00
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Purity: 100%
Purity: 99.84%
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Biological Description
Chemical Properties
Storage & Solubility Information
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.
Synonyms SANT 1
Molecular Weight 373.49
Formula C23H27N5
CAS No. 304909-07-7

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 18.7 mg/mL (50 mM)

Ethanol: 9.3 mg/mL (25 mM)

TargetMolReferences and Literature

1. James K. Chen, et al. Proc Natl Acad Sci U S A, 2002, 99(22), 14071-14076. 2. Wilson CW, et al. PLoS One. 2009;4(4):e5182. 3. Chun SG, et al. Cancer Biol Ther, 2009, 8(14), 1328-1339.

Related compound libraries

This product is contained In the following compound libraries:
Membrane Protein-targeted Compound Library GPCR Compound Library Inhibitor Library Target-Focused Phenotypic Screening Library Bioactive Compounds Library Max Anti-Obesity Compound Library Wnt/Hedgehog/Notch Compound Library Anti-Aging Compound Library Stem Cell Differentiation Compound Library Anti-Prostate Cancer Compound Library

Related Products

Related compounds with same targets
MK-4101 Ciliobrevin A BMS-833923 GANT 58 Cyclopamine JK184 Tolnaftate Vismodegib

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Keywords

SANT-1 304909-07-7 GPCR/G Protein Stem Cells Hedgehog/Smoothened Smo Smoothened Hedgehog Inhibitor SANT1 inhibit SANT 1 inhibitor

 

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