SANT-2 |
Katalog-Nr.GC11193 |
SANT-2 ist ein potenter Antagonist des Hh-Signalwegs. Die Hedgehog (Hh)-Signalgebung spielt eine wichtige Rolle bei der Zellsignalisierung der embryonalen Entwicklung und der HomÖostase des adulten Gewebes. SANT-2 hat das Potenzial fÜr die Erforschung mehrerer bÖsartiger Erkrankungen, darunter das Gorlin-Syndrom (eine Erkrankung, die fÜr Basalzellkarzinom, Medulloblastom und Rhabdomyosarkom prÄdisponiert), Prostata-, BauchspeicheldrÜsen- und Brustkrebs.
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Cas No.: 329196-48-7
Sample solution is provided at 25 µL, 10mM.
SANT-2 is a Smoothened (Smo) receptor antagonist.[1],[2] It binds to the Smo receptor (Kd = 12 nM) and inhibits binding of the Smo receptor agonist SAG-1.3 and antagonist cyclopamine(Kis = 7.8 and 8.4 nM, respectively). SANT-2 inhibits hedgehog signaling induced by an N-terminal fragment of sonic hedgehog (Shh) in an Shh-LIGHT2 cellular assay (IC50 = 30 nM).[1]
Reference:
[1]. Chen, J.K., Taipale, J., Young, K.E., et al. Small molecule modulation of smoothened activity. Proc. Natl. Acad. Sci. USA 99(22), 14071-14076 (2002).
[2]. Rominger, C.M., Bee, W.L.T., Copeland, R.A., et al. Evidence for allosteric interactions of antagonist binding to the smoothened receptor. J. Pharmacol. Exp. Ther. 329(3), 995-1005 (2009).
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