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.
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]

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


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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Handling Instructions

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