货号 | 15781-1mg |
描述 | The receptor tyrosine kinase c-kit, activated by its ligand stem-cell factor (SCF), modulates diverse cellular processes, including cell proliferation, differentiation, and survival.1,2 ISCK03 is a cell-permeable inhibitor of SCF-mediated c-kit activation, completely blocking phosphorylation of c-kit in human melanoma cells at a concentration between 1 and 5 µM.3 These concentrations also prevent SCF-mediated downstream phosphorylation of p44/p42 ERK but does not prevent phosphorylation of p44/p42 ERK induced by hepatocyte growth factor.3 Oral administration of ISCK03 in mice induces hair depigmentation, whereas topical application decreases epidermal melanin in guinea pig skin darkened by UV irradiation.3 ISCK03 has also been used to elucidate the role of SCF/c-kit signaling in cell viability, radiation-induced angiogenesis, and melanocortin receptor action.4,5,6 |
别名 | c-Kit Inhibitor II;Stem-Cell Factor/c-Kit Inhibitor; |
供应商 | Cayman |
应用文献 | |
1.Griswold, I.J.,Shen, L.J.,La Rosée, P., et al. Effects of MLN518, a dual FLT3 and KIT inhibitor, on normal and malignant hematopoiesis. Blood 104(9), 2912-2918 (2004). 2.Wisniewski, D.,Lambek, C.L.,Liu, C., et al. Characterization of potent inhibitors of the Bcr-Abl and the c-kit receptor tyrosine kinases. Cancer Research 62(15), 4244-4255 (2002). 3.Na, Y.J.,Baek, H.S.,Ahn, S.M., et al. [4-t-Butylphenyl]-N-(4-imidazol-1-yl phenyl)sulfonamide (ISCK03) inhibits SCF/c-kit signaling in 501mel human melanoma cells and abolishes melanin production in mice and brownish guinea pigs. Biochemical Pharmacology 74(5), 780-786 (2007). 4.Kamlah, F.,Hänze, J.,Arenz, A., et al. Comparison of the effects of carbon ion and photon irradiation on the angiogenic response in human lung adenocarcinoma cells. Int.J.Radiat.Oncol.Biol.Phys. 80(5), 1541-1549 (2011). 5.Kon, S.,Minegishi, N.,Tanabe, K., et al. Smap1 deficiency perturbs receptor trafficking and predisposes mice to myelodysplasia. Journal of Clinical Investigation 123(3), 1123-1137 (2013). 6.Herraiz, C.,Journé, F.,Abdel-Malek, Z., et al. Signaling from the human melanocortin 1 receptor to ERK1 and ERK2 mitogen-activated protein kinases involves transactivation of cKIT. Molecular Endocrinology 25(1), 138-156 (2011). | |
运输条件 | Room temperature in continental US; may vary elsewhere |
存放说明 | -20 |
纯度 | ≥95% |
计算分子量 | 355.5 |
分子式 | C19H21N3O2S |
CAS号 | 945526-43-2 |
稳定性 | ≥ 2 years |
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