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SANT-1

Catalog No.
A8659
Shh inhibitor,potent and cell-permeable
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$80.00
In stock
10mg
$103.00
In stock
50mg
$399.00
In stock

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

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.

Product Citation

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt373.5
Cas No.304909-07-7
FormulaC23H27N5
Solubility≥18.75mg/mL in DMSO
Chemical Name(E)-N-(4-benzylpiperazin-1-yl)-1-(3,5-dimethyl-1-phenylpyrazol-4-yl)methanimine
SDFDownload SDF
Canonical SMILESCC1=C(C(=NN1C2=CC=CC=C2)C)C=NN3CCN(CC3)CC4=CC=CC=C4
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor 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.

Biological Activity

Description SANT-1 is a inhibitor of Smoothened (Smo) with Kd of 1.2 nM and IC50 of 20 nM.
Targets Smoothened          
IC50 20 nM (Kd=1.2 nM)          

Quality Control

Chemical structure

SANT-1