A potent inhibitor of hedgehog signaling that acts by directly antagonizing SMO (IC50 = 20 nM); counteracts SMO activation by the SMO agonist SAG but only partially competes with SAG binding to SMO

SANT 1 – 1 mg

Brand:
Cayman
CAS:
304909-07-7
Storage:
-20
UN-No:
Non-Hazardous - /

Smoothened (SMO) is a GPCR-like receptor which, with Patched, mediates hedgehog signaling to regulate gene expression through the Gli transcription factors.{21774} SANT 1 is a potent inhibitor of hedgehog signaling that acts by directly antagonizing SMO (IC50 = 20 nM).{21771} It counteracts SMO activation by the SMO agonist SAG but only partially competes with SAG binding to SMO.{21771,24191} SANT 1 targets inactive SMO while it is in the cytoplasm, before it relocates to the primary cilium and is activated.{22122} Through antagonism of SMO, SANT 1 represses Gli-mediated transcription in a variety of cell types.{22122,24193}  

 

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Description

A potent inhibitor of hedgehog signaling that acts by directly antagonizing SMO (IC50 = 20 nM); counteracts SMO activation by the SMO agonist SAG but only partially competes with SAG binding to SMO

Formal name: N-[(3,5-dimethyl-1-phenyl-1H-pyrazol-4-yl)methylene]-4-(phenylmethyl)-1-piperazinamine

Synonyms: 

Molecular weight: 373.5

CAS: 304909-07-7

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Cell Biology|Cell Signaling|Hedgehog Signaling||Research Area|Neuroscience

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