SANT-1

Catalog No.S7092

For research use only.

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

SANT-1 Chemical Structure

CAS No. 304909-07-7

Selleck's SANT-1 has been cited by 12 Publications

1 Customer Review

Purity & Quality Control

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Biological Activity

Description SANT-1 directly binds to Smoothened (Smo) receptor with Kd of 1.2 nM and inhibits Smo agonist effects with IC50 of 20 nM.
Features Attenuates SAG stimulation of Shh-LIGHT2 cells to a greater extent relative to other antagonists.
Targets
Smoothened receptor [1]
1.2 nM(Kd)
In vitro

SANT-1 inhibits wild type and oncogenic Smo with equal potency. SANT-1 counteracts SAG-induced pathway activation in Shh-LIGHT2 cells. SANT-1 is able to block BODIPY-cyclopamine binding to Smo-expressing cells, but SANT-1 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. SANT-1 blocks pathway activation in SmoA1-LIGHT2 cells with potencies similar to those observed in the Shh-LIGHT2 assay. SANT-1 has disparate inhibitory activities in the Shh-LIGHT2 and BODIPY-cyclopamine assays and is unusually potent at blocking SAG-mediated pathway activation.[1] SANT-1 efficiently inhibited cyclopamine- and jervine- induced translocation of Smo to the primary cilium. SANT-1 inhibits PKA stimulation of Smo trafficking to the proximal cilium.[2] When combined HDAC inhibitor SAHA, SANT-1 is able to suppress cellular proliferation and colony formation of Gemcitabine-resistant pancreatic adenocarcinoma cell lines Panc-1 and BxPC-3. [3]

Assay
Methods Test Index PMID
Western blot Gli1 / E-cadherin / Sanil / ABCG2 26943330

Protocol (from reference)

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 373.49
Formula

C23H27N5

CAS No. 304909-07-7
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1=C(C(=NN1C2=CC=CC=C2)C)C=NN3CCN(CC3)CC4=CC=CC=C4

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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