SANT-2

Inhibitor of Hedgehog (Hh) signaling; antagonizes smoothened activity CAS# 329196-48-7

SANT-2

Catalog No. BCC3937----Order now to get a substantial discount!

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Chemical structure

SANT-2

3D structure

Chemical Properties of SANT-2

Cas No. 329196-48-7 SDF Download SDF
PubChem ID 1367095 Appearance Powder
Formula C26H26ClN3O4 M.Wt 479.96
Type of Compound N/A Storage Desiccate at -20°C
Solubility Soluble to 100 mM in DMSO and to 100 mM in ethanol
Chemical Name N-[3-(1H-benzimidazol-2-yl)-4-chlorophenyl]-3,4,5-triethoxybenzamide
SMILES CCOC1=CC(=CC(=C1OCC)OCC)C(=O)NC2=CC(=C(C=C2)Cl)C3=NC4=CC=CC=C4N3
Standard InChIKey VQOJFGFKIVFMDH-UHFFFAOYSA-N
Standard InChI InChI=1S/C26H26ClN3O4/c1-4-32-22-13-16(14-23(33-5-2)24(22)34-6-3)26(31)28-17-11-12-19(27)18(15-17)25-29-20-9-7-8-10-21(20)30-25/h7-15H,4-6H2,1-3H3,(H,28,31)(H,29,30)
General tips For 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.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of SANT-2

DescriptionInhibitor of Sonic hedgehog (Shh) signaling; antagonizes smoothened receptor activity (KD = 12 nM). Displays allosteric binding characteristics similar to SANT-1. Displaces smo-[3H]SAG-1.3 and -[3H]Cyclopamine binding (Ki values are 7.8 nM and 8.4 nM respectively).

SANT-2 Dilution Calculator

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SANT-2 Molarity Calculator

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Preparing Stock Solutions of SANT-2

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.0835 mL 10.4175 mL 20.8351 mL 41.6701 mL 52.0877 mL
5 mM 0.4167 mL 2.0835 mL 4.167 mL 8.334 mL 10.4175 mL
10 mM 0.2084 mL 1.0418 mL 2.0835 mL 4.167 mL 5.2088 mL
50 mM 0.0417 mL 0.2084 mL 0.4167 mL 0.8334 mL 1.0418 mL
100 mM 0.0208 mL 0.1042 mL 0.2084 mL 0.4167 mL 0.5209 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on SANT-2

Inhibitor of Sonic hedgehog (Shh) signaling; antagonizes smoothened receptor activity (KD = 12 nM).

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References on SANT-2

Synthesis and biological evaluation of SANT-2 and analogues as inhibitors of the hedgehog signaling pathway.[Pubmed:19541490]

Bioorg Med Chem. 2009 Jul 15;17(14):4943-54.

Hedgehog (Hh) signaling plays an important role in cell signaling of embryonic development and adult tissue homeostasis. In vertebrates, the hh gene encodes three different unique proteins: sonic hedgehog (Shh), desert hedgehog (Dhh) and indian hedgehog (Ihh). Disruption of the Hh signaling pathway leads to severe disorders in the development of vertebrates whereas aberrant activation of the Hh pathway has been associated with several malignancies including Gorlin syndrome (a disorder predisposing to basal cell carcinoma, medulloblastoma and rhabdomyosarcoma), prostate, pancreatic and breast cancers. In vivo evidence suggests the antagonism of excessive Hh signaling provides a route to unique mechanism-based anti-cancer therapies. Recently the small molecule SANT-2 was identified as a potent antagonist of Hh-signaling pathway. Here, we describe the synthesis, SAR studies as well as biological evaluation of SANT-2 and its analogues. Fifteen SANT-2 derivatives were synthesized and analyzed for their interference with the expression of the Hh target gene Gli1 in a reporter gene assay. By comparison of structure and activity important molecular descriptors for Gli inhibition could be identified. Furthermore we identified derivative TC-132 that was slightly more potent than the parent compound SANT-2. Selected compounds were tested for Hh related teratogenic effects in the small teleost model medaka. Albeit Gli expression has indicated a 16-fold higher Hh-inhibiting activity than observed for the plant alkaloid cyclopamine, none of the tested compounds were able to induce the cyclopamine-specific phenotype in the medaka assay.

Evidence for allosteric interactions of antagonist binding to the smoothened receptor.[Pubmed:19304771]

J Pharmacol Exp Ther. 2009 Jun;329(3):995-1005.

The Smoothened receptor (Smo) mediates hedgehog (Hh) signaling critical for development, cell growth, and migration, as well as stem cell maintenance. Aberrant Hh signaling pathway activation has been implicated in a variety of cancers, and small-molecule antagonists of Smo have entered human clinical trials for the treatment of cancer. Here, we report the biochemical characterization of allosteric interactions of agonists and antagonists for Smo. Binding of two radioligands, [(3)H]3-chloro-N-[trans-4-(methylamino)cyclohexyl]-N-{[3-(4-pyridinyl)-phenyl]met hyl}-1-benzothiophene-2-carboxamide (SAG-1.3) (agonist) and [(3)H]cyclopamine (antagonist), was characterized using human Smo expressed in human embryonic kidney 293F membranes. We observed full displacement of [(3)H]cyclopamine by all Smo agonist and antagonist ligands examined. N-[(1E)-(3,5-Dimethyl-1-phenyl-1H-pyrazol-4-yl)methylidene]-4-(phenylmethyl)-1-pi perazinamine (SANT-1), an antagonist, did not fully inhibit the binding of [(3)H]SAG-1.3. In a functional cell-based beta-lactamase reporter gene assay, SANT-1 and N-[3-(1H-benzimidazol-2-yl)-4-chlorophenyl]-3,4,5-tris(ethyloxy)-benzamide (SANT-2) fully inhibited 3-chloro-4,7-difluoro-N-[trans-4-(methylamino)cyclohexyl]-N-{[3-(4-pyridinyl)phen yl]methyl}-1-benzothiophene-2-carboxamide (SAG-1.5)-induced Hh pathway activation. Detailed "Schild-type" radioligand binding analysis with [(3)H]SAG-1.3 revealed that two structurally distinct Smoothened receptor antagonists, SANT-1 and SANT-2, bound in a manner consistent with that of allosteric modulation. Our mechanism of action characterization of radioligand binding to Smo combined with functional data provides a better understanding of small-molecule interactions with Smo and their influence on the Hh pathway.

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