| 货号 | 14933-1mg |
| 描述 | Smoothened (SMO) is a GPCR-like receptor which, with Patched, mediates hedgehog signaling to regulate gene expression through the Gli transcription factors.1 SANT 1 is a potent inhibitor of hedgehog signaling that acts by directly antagonizing SMO (IC50 = 20 nM).2 It counteracts SMO activation by the SMO agonist SAG but only partially competes with SAG binding to SMO.2,3 SANT 1 targets inactive SMO while it is in the cytoplasm, before it relocates to the primary cilium and is activated.4 Through antagonism of SMO, SANT 1 represses Gli-mediated transcription in a variety of cell types.4,5 |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Ruiz-Gómez, A.,Molnar, C.,Holguín, H., et al. The cell biology of Smo signalling and its relationships with GPCRs. Biochimica et Biophysica Acta 1768(4), 901-912 (2007). 2.Chen, J.K.,Taipale, J.,Young, K.E., et al. Small molecule modulation of smoothened activity. Proceedings of the National Academy of Sciences of the United States of America 99(22), 14071-14076 (2002). 3.Rominger, C.M.,Bee, W.L.T.,Copeland, R.A., et al. Evidence for allosteric interactions of antagonist binding to the smoothened receptor. Journal of Pharmacology and Experimental Therapeutics 329(3), 995-1005 (2009). 4.Stanton, B.Z. and Peng, L.F. Small-molecule modulators of the Sonic Hedgehog signaling pathway. Molecular BioSystems 6(1), 44-54 (2010). 5.Scales, S.J. and de Sauvage, F.J. Mechanisms of hedgehog pathway activation in cancer and implications for therapy. Trends in Pharamacological Sciences 30(6), 303-312 (2009). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 373.5 |
| 分子式 | C23H27N5 |
| CAS号 | 304909-07-7 |
| 稳定性 | ≥ 2 years |
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