| 货号 | 11914-10mg |
| 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 Smoothened agonist (SAG) is a chlorobenzothiophene-containing compound which acts as a SMO agonist (EC50 = 3 nM) but inhibits hedgehog signaling at high concentrations (>1 μM).2 It directly binds to SMO and can block SMO inhibition by cyclopamine.2 Binding of SAG alters the conformation of SMO, leading to its accumulation in cilia and activation of gene transcription.3,4,5 At 15-240 nM, SAG prevents the neurotoxic effects of glucocorticoids without interfering with the beneficial effects of glucocorticoids on lung maturation.6 At higher concentrations (0.4 mM), SAG improves the conversion of human induced pluripotent stem cells to the neural lineage.7 |
| 别名 | Smoothened Agonist; |
| 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.Frank-Kamenetsky, M.,Zhang, X.M.,Bottega, S., et al. Small-molecule modulators of Hedgehog signaling: Identification and characterization of smoothened agonists and antagonists. J.Biol. 1(2), (2002). 4.Yang, H.,Xiang, J.,Wang, N., et al. Converse conformational control of smoothened activity by structurally related small molecules. The Journal of Biological Chemisty 284(31), 20876-20884 (2009). 5.Rohatgi, R.,Milenkovic, L.,Corcoran, R.B., et al. Hedgehog signal transduction by smoothened: Pharmacologic evidence for a 2-step activation process. Proceedings of the National Academy of Sciences of the United States of America 106(9), 3196-3201 (2009). 6.Heine, V.M.,Griveau, A.,Chapin, C., et al. A small-molecule smoothened agonist prevents glucocorticoid-induced neonatal cerebellar injury. Sci.Transl.Med. 3(105), 1-9 (2011). 7.Mak, S.K.,Huang, Y.A.,Iranmanesh, S., et al. Small molecules greatly improve conversion of human-induced pluripotent stem cells to the neuronal lineage. Stem Cells Int. 2012, (2012). | |
| 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 | 490.1 |
| 分子式 | C28H28ClN3OS |
| CAS号 | 912545-86-9 |
| 稳定性 | ≥ 2 years |
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