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SANT-1
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
SANT-1图片
CAS NO:304909-07-7
规格:98%
分子量:373.5
包装与价格:
包装价格(元)
10mg电议
50mg电议

产品介绍
Shh inhibitor,potent and cell-permeable
CAS:304909-07-7
分子式:C23H27N5
分子量:373.5
纯度:98%
存储:Store at -20°C

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.


参考文献:
[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.