SANT-1 Chemische Eigenschaften,Einsatz,Produktion Methoden
Beschreibung
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 (IC
50 = 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.
Chemische Eigenschaften
Pale Yellow Solid
Verwenden
Treatment of Anaplastic lymphoma kinase (ALK)-positive anaplastic large cell lymphoma cells
2 and chronic lymphocytic leukemia cells
3 with SANT-1 induced cell death.
Biologische Aktivität
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).
SANT-1 Upstream-Materialien And Downstream Produkte
Upstream-Materialien
Downstream Produkte
