SANT-2 |
カタログ番号GC11193 |
SANT-2 は、Hh シグナル伝達経路の強力なアンタゴニストです。ヘッジホッグ (Hh) シグナル伝達は、胚発生および成体組織の恒常性の細胞シグナル伝達において重要な役割を果たします。 SANT-2 は、ゴーリン症候群 (基底細胞癌、髄芽腫、横紋筋肉腫の素因となる疾患)、前立腺癌、膵臓癌、乳癌など、いくつかの悪性腫瘍の研究に役立つ可能性があります。
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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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