For research use only.

Catalog No.S7092

9 publications

SANT-1 Chemical Structure

CAS No. 304909-07-7

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

Selleck's SANT-1 has been cited by 9 publications

1 Customer Review

  • (D) Percentage cell death of OCI-AML3 cells was measured using the CellTiter-Glo® viability assay following 24 hours treatment with either sequential treatment of 1 μM Vorinostat with low (0.1 μM) or high dose (2.5 μM) SANT-1, or single agents. Data represents a biological replicate of 3, with data presented relative to the DMSO control (0% cell death). (E) Protein expression of SHH was measured following 24 hours treated with the four treatment strategies in OCI-AML3 cells. Equal loading was confirmed with β-Actin

    Oncotarget, 2017, 8(40): 67891-67903. SANT-1 purchased from Selleck.

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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 ; 

PubMed: 26943330     

Western blot analysis of the Hh signaling pathway activity and its target genes E-Cadherin, Snail and ABCG2 in EGFR-resistant cells A549 after SANT-1 treatment for 0, 24, and 48 h.



Solubility (25°C)

In vitro DMSO 21 mg/mL (56.22 mM)
Ethanol 20 mg/mL (53.54 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 373.49


CAS No. 304909-07-7
Storage powder
in solvent
Synonyms N/A
Smiles CC1=C(C(=NN1C2=CC=CC=C2)C)C=NN3CCN(CC3)CC4=CC=CC=C4

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Hedgehog/Smoothened Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID