SANT-2 |
Catalog No.GC11193 |
SANT-2 is a potent antagonist of Hh-signaling pathway. Hedgehog (Hh) signaling plays an important role in cell signaling of embryonic development and adult tissue homeostasis. SANT-2 has the potential for the research of several malignancies including Gorlin syndrome (a disorder predisposing to basal cell carcinoma, medulloblastoma and rhabdomyosarcoma), prostate, pancreatic and breast cancers.
Products are for research use only. Not for human use. We do not sell to patients.
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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