| 货号 | 17776-1mg |
| 描述 | Hedgehog (Hh) proteins, important regulators of development, bind the cell-surface protein Patched, allowing activation of the GPCR-like receptor, Smoothened (SMO).1 In vertebrates, this ultimately leads to the activation of the zinc-finger transcription factors of the Gli family. Overactivation of this pathway contributes to certain cancers.2 ALLO-1 is a SMO antagonist that inhibits both wild-type (IC50 = 50 nM) and mutant SMO, including the D473H SMO mutant (IC50s = 300-1000 nM).3 This compound binds to the SMO cysteine-rich domain, which is a different mechanism of interaction compared to other known SMO ligands that bind the transmembrane pocket.3,4 |
| 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.Rubin, L.L. and de Sauvage, F.J. Targeting the Hedgehog pathway in cancer. Nature Reviews.Drug Discovery 5(12), 1026-1033 (2006). 3.Tao, H.,Jin, Q.,koo, D.I., et al. Small molecule antagonists in distinct binding modes inhibit drug-resistant mutant of smoothened. Chemistry & Biology 18, 432-437 (2011). 4.Sharpe, H.J.,Wang, W.,Hannoush, R.N., et al. Regulation of the oncoprotein Smoothened by small molecules. Nature Chemical Biology 11, 246-255 (2015). | |
| 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 | 314.8 |
| 分子式 | C17H15ClN2O2 |
| CAS号 | 37468-32-9 |
| 稳定性 | ≥ 2 years |
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