Name: SANT-1
Brand: Selleck Chemicals
SKU: S7092
Availability: InStock
Rating: 5 (17 reviews)

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Quality Control

Batch: Purity: 99.03%

99.03

Related Targets	JAK TGF-beta/Smad Wnt/beta-catenin ERK GSK-3 ROCK PKA Secretase STAT Casein Kinase
Other Hedgehog/Smoothened Inhibitors	SAG (Smoothened Agonist) Hydrochloride Purmorphamine Cyclopamine (11-Deoxojervine) GANT61 SAG (Smoothened Agonist) HPI-4 (Ciliobrevin A) BMS-833923 Taladegib (LY2940680) Ciliobrevin D Jervine

Solubility

In vitro
Batch:

DMSO : 75 mg/mL (200.8 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 18 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	1.050mg/ml (2.81mM)	Taking the 1 mL working solution as an example, add 50 μL of 21 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	1.050mg/ml (2.81mM)	Taking the 1 mL working solution as an example, add 50 μL of 21 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

%

% Tween 80

% ddH₂O

% DMSO

+

%

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	373.49	Formula	C₂₃H₂₇N₅	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	304909-07-7	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	CC1=C(C(=NN1C2=CC=CC=C2)C)C=NN3CCN(CC3)CC4=CC=CC=C4

Mechanism of Action

Features	Attenuates SAG stimulation of Shh-LIGHT2 cells to a greater extent relative to other antagonists.
Targets/IC₅₀/Ki	Smoothened receptor 1.2 nM(Kd)
In vitro	SANT-1 inhibits wild type and oncogenic Smo with equal potency. This compound counteracts SAG-induced pathway activation in Shh-LIGHT2 cells. It is able to block BODIPY-cyclopamine binding to Smo-expressing cells, but this chemical is unable to inhibit completely this association to background levels. This suggests that their interactions with Smo may alter its affinity for cyclopamine rather than compete directly for cyclopamine binding. The compound blocks pathway activation in SmoA1-LIGHT2 cells with potencies similar to those observed in the Shh-LIGHT2 assay. It has disparate inhibitory activities in the Shh-LIGHT2 and BODIPY-cyclopamine assays and is unusually potent at blocking SAG-mediated pathway activation. This compound efficiently inhibited cyclopamine- and jervine- induced translocation of Smo to the primary cilium. It inhibits PKA stimulation of Smo trafficking to the proximal cilium.
Kinase Assay	Small Molecule Screens for Hh Pathway Modulators
Kinase Assay	Shh-N (N-terminal fragment of Shh without cholesterol modification)-conditioned medium is obtained from an HEK 293 cell line stably transfected with Shh-N expression and neomycin resistance constructs. The Shh-N-producing HEK 293 cells are grown to 80% confluency in DMEM containing 10% (vol/vol) FBS and 400 μg/ml G418. The medium then is replaced with DMEM containing 2% (vol/vol) FBS, and after 1 day of growth, the medium is collected and filtered through a 0.22-μm membrane. Control medium is obtained from HEK 293 cells. Shh-LIGHT2 cells are then cultured to confluency in 96-well plates and treated with this compound (0.714 μg/mL; ≈2 μM compound in each well) in the presence of either Shh-N-conditioned medium or HEK 293 control medium (1:25 dilution into DMEM containing 0.5% bovine calf serum). After incubating the treated cells for 30 h at 37°C, cellular firefly and Renilla luciferase activities are measured.
References	[1] https://pubmed.ncbi.nlm.nih.gov/12391318/ [2] https://pubmed.ncbi.nlm.nih.gov/19365551/ [3] https://pubmed.ncbi.nlm.nih.gov/19421011/

Applications

Methods	Biomarkers	Images	PMID
Western blot	Gli1 / E-cadherin / Sanil / ABCG2		26943330

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SANT-1 Smoothened Receptor Antagonist

Chemical Structure

Molecular Weight: 373.49