Antibodies
SANT-1
- 貨號 Cat. No.
- S7092
- 規格 Size
- 10mgã€50mg
- 品牌 Brand
- Selleckchem
Description
SANT-1
Catalog No.S7092
SANT-1 directly binds to Smoothened (Smo) receptor with Kd of 1.2 nM and inhibits Smo agonist effects with IC50 of 20 nM.
| Size | Price | Stock | Quantity | ||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|
| |||||||||||
Distributor Tel: +886-2-2827-1197jimmy@new.abscience.com.tw
Biological Activity
| Description | SANT-1 directly binds to Smoothened (Smo) receptor with Kd of 1.2 nM and inhibits Smo agonist effects withIC50 of 20 nM. | |||||
|---|---|---|---|---|---|---|
| Targets | Smoothened receptor | |||||
| IC50 | 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] | |||||
| In vivo | ||||||
| Features | Attenuates SAG stimulation of Shh-LIGHT2 cells to a greater extent relative to other antagonists. | |||||
Protocol(Only for Reference)
Kinase Assay: [1]
| Small Molecule Screens for Hh Pathway Modulators | Shh-N (N-terminal fragment of Shh without cholesterol modification)-conditioned medium is obtained from an HEK 293 cell line stably transfected with Shh-N expression and neomycin resistance constructs. The Shh-N-producing HEK 293 cells are grown to 80% confluency in DMEM containing 10% (vol/vol) FBS and 400 μg/ml G418. The medium then is replaced with DMEM containing 2% (vol/vol) FBS, and after 1 day of growth, the medium is collected and filtered through a 0.22-μm membrane. Control medium is obtained from HEK 293 cells. Shh-LIGHT2 cells are then cultured to confluency in 96-well plates and treated with the small molecules (0.714 μg/mL; ≈2 μM compound in each well) in the presence of either Shh-N-conditioned medium or HEK 293 control medium (1:25 dilution into DMEM containing 0.5% bovine calf serum). After incubating the treated cells for 30 h at 37°C, cellular firefly and Renilla luciferase activities are measured. |
|---|
References
Chemical Information
| Molecular Weight (MW) | 373.49 |
|---|---|
| Formula | C23H27N5 |
| CAS No. | 304909-07-7 |
| Storage | 3 years -20℃Powder |
|---|---|
| 6 months-80℃in DMSO | |
| Syonnyms | N/A |
| Solubility (25°C) * | In vitro | DMSO | 21 mg/mL (56 mM) |
|---|---|---|---|
| Water | <1 mg/mL (<1 mM) | ||
| Ethanol | 20 mg/mL (53 mM) | ||
| * <1 mg/ml means slightly soluble or 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 Name | 1-Piperazinamine, N-[(3,5-dimethyl-1-phenyl-1H-pyrazol-4-yl)methylene]-4-(phenylmethyl)- |
|---|
Preparing Stock Solutions
| Stock Solution (1ml DMSO) | 1mM | 10mM | 20mM | 30mM |
|---|---|---|---|---|
| Mass(mg) | 0.37349 | 3.7349 | 7.4698 | 11.2047 |
