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SKI-178 是一种鞘氨醇激酶-1(SphK1)和 SphK2抑制剂,以 CDK1 依赖性方式诱导人急性髓性白血病细胞凋亡。
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SKI-178 是一种鞘氨醇激酶-1(SphK1)和 SphK2抑制剂,以 CDK1 依赖性方式诱导人急性髓性白血病细胞凋亡。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 247 | 现货 | |
2 mg | ¥ 359 | 现货 | |
5 mg | ¥ 622 | 现货 | |
10 mg | ¥ 1,080 | 现货 | |
25 mg | ¥ 1,980 | 现货 | |
50 mg | ¥ 3,320 | 现货 | |
100 mg | ¥ 4,880 | 现货 | |
500 mg | ¥ 9,870 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 688 | 现货 |
产品描述 | SKI-178 is a sphingosine kinase 1 (SphK1) inhibitor with IC50 of 0.1-1.8 μM. It induces prolonged mitosis followed by apoptotic cell death through the intrinsic apoptotic cascade. The sustained activation of CDK1 during prolonged mitosis, mediated by SKI-178 leads to the simultaneous phosphorylation of the prosurvival Bcl-2 family members, Bcl-2 and Bcl-xl, as well as the phosphorylation and subsequent degradation of Mcl-1. |
靶点活性 | SPHK1:0.1-1.8 μM |
体外活性 | SKI-178是一种多靶向药物,既能抑制SphKs也能破坏微管网络。由于这两种活动的协同作用,SKI-178能引起细胞凋亡。在小鼠的AML模型中,SKI-178表现出安全性和有效性,支持其作为多靶向抗癌治疗药物的进一步开发[1]。 |
分子量 | 394.42 |
分子式 | C21H22N4O4 |
CAS No. | 1259484-97-3 |
Smiles | COc1ccc(cc1)-c1cc([nH]n1)C(=O)N\N=C(/C)c1ccc(OC)c(OC)c1 |
密度 | 1.24 g/cm3 (Predicted) |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
溶解度信息 | DMSO: 50 mg/mL (126.77 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
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