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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, CAS 304909-07-7

Pack Size	Availability	Price/USD
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%

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)

References 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：

Inhibitor Library GPCR Compound Library Osteogenesis Compound Library Neuronal Differentiation Compound Library Wnt/Hedgehog/Notch Compound Library Anti-Obesity Compound Library Bioactive Compounds Library Max Stem Cell Differentiation Compound Library Anti-Prostate Cancer Compound Library Target-Focused Phenotypic Screening Library

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MK-4101 Triparanol BMS-833923 Naftifine hydrochloride RU-SKI 43 GANT 58 Ellagic acid GANT 61

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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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