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| Product Name: | SANT-1 | | Synonyms: | N-[(3,5-DIMETHYL-1-PHENYL-1H-PYRAZOL-4-YL)METHYLENE]-4-(PHENYLMETHYL)-1-PIPERAZINAMINE;SANT-1;(4-Benzyl-piperazin-1-yl)-(3,5-dimethyl-1-phenyl-1H-pyrazol-4-ylmethylene)-amine;1-Piperazinamine, N-[(3,5-dimethyl-1-phenyl-1H-pyrazol-4-yl)methylene]-4-(phenylmethyl)-;(E)-N-(4-benzylpiperazin-1-yl)-1-(3,5-dimethyl-1-phenylpyrazol-4-yl)methanimine;SANT1 10MG;SANT1;SANT 1;SANT-1 - CAS 304909-07-7 - Calbiochem | | CAS: | 304909-07-7 | | MF: | C23H27N5 | | MW: | 373.49 | | EINECS: | | | Product Categories: | Lipid signaling;Inhibitors;All Inhibitors;API | | Mol File: | 304909-07-7.mol |  |
| | SANT-1 Chemical Properties |
| Melting point | 104-106°C | | Boiling point | 547.4±50.0 °C(Predicted) | | density | 1.13±0.1 g/cm3(Predicted) | | storage temp. | -20°C | | solubility | Soluble in DMSO with warming | | form | White solid | | pka | 7.35±0.10(Predicted) | | Sensitive | Moisture & Light Sensitive | | CAS DataBase Reference | 304909-07-7 |
| | SANT-1 Usage And Synthesis |
| Description | Smoothened (SMO) is a GPCR-like receptor which, with Patched, mediates hedgehog signaling to regulate gene expression through the Gli transcription factors. SANT 1 is a potent inhibitor of hedgehog signaling that acts by directly antagonizing SMO (IC50 = 20 nM). It counteracts SMO activation by the SMO agonist SAG but only partially competes with SAG binding to SMO. SANT 1 targets inactive SMO while it is in the cytoplasm, before it relocates to the primary cilium and is activated. Through antagonism of SMO, SANT 1 represses Gli-mediated transcription in a variety of cell types. | | Chemical Properties | Pale Yellow Solid | | Uses | Treatment of Anaplastic lymphoma kinase (ALK)-positive anaplastic large cell lymphoma cells2 and chronic lymphocytic leukemia cells3 with SANT-1 induced cell death. | | Uses | A potent antagonist of the sonic hedgehog (Shh) signaling pathway (IC50=20nm inShh-LIGHT2 assay an d in Ptch1-/- cells) that acts by binding to smoothened (Smo: KD=1.2 nM), a distant relative of G protein-coupled receptors. In contrast to cyclopamine, SNAT-1 inhibits the activities of both wild type and oncogenic Smo with equal potency (IC50=30nm in SmoA1-LIGHT2 assay). | | Definition | ChEBI: 1-(3,5-dimethyl-1-phenyl-4-pyrazolyl)-N-[4-(phenylmethyl)-1-piperazinyl]methanimine is a ring assembly and a member of pyrazoles. | | Biological Activity | Potent, cell-permeable inhibitor of Sonic hedgehog (Shh) signaling; high affinity antagonist of smoothened activity (K D = 1.2 nM). Inhibits smoothened agonist effects with an IC 50 of 20 nM (in Shh-LIGHT2 cells). | | Biochem/physiol Actions | SANT-1 is a potent sonic hedgehog pathway (Shh) antagonist that directly inhibits by binding to the smoothened (Smo) receptor. SANT-1 inhibits wild type and oncogenic Smo with equal potency. | | storage | Desiccate at +4°C | | references | [1]. chen j k., taipale j, young k e,. small molecule modulation of smoothened activity. proc natl acad sci u s a, 2002, 99: 14071-6.
[2]. chun sg, zhou w & yee n s. combined targeting of histone deacetylases and hedgehog signaling enhances cytoxicity in pancreatic cancer. cancer biol ther, 2009, 8: 1328-39. |
| | SANT-1 Preparation Products And Raw materials |
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