| 产品描述: | BAY-888 is a selective CK1α/CSNK1A1 (casein kinase 1α) ATP-competitive inhibitor (IC50: 4 nM@10 μM ATP; 63 nM@1 mM ATP). BAY-888 blocks the negative regulation of p53 and other signaling pathways by CK1α, induces apoptosis and inhibits proliferation of tumor cells. BAY-888 has shown inhibitory efficacy against cancers such as acute myeloid leukemia (AML) in PRISM barcoded cell line screening and can mimic the effects of shRNA-mediated CK1α knockdown. BAY-888 is primarily used for the development of anticancer drugs for p53 wild-type tumors and for the study of the mechanisms of CK1α-related signaling pathways. |
| 体外研究: |
BAY-888 在多种小鼠细胞系异种移植模型中具有体内抑制效力,对弥漫大 B 细胞淋巴瘤 (TMD8) 以及多种 FAM83 高表达实体瘤模型 (结直肠癌 (HCT116 和 HT29)、胃癌 (IM95) 和尿路上皮癌 (KU19-19)) 等。BAY-888 的体内抗癌机制可能与 RPS6 磷酸化有关[2]。 |
| 体内研究: |
BAY-888 (example 5) 抑制 WT EGFR 的 IC50 为 11.5-15.5 μM (@2 mM ATP)。 BAY-888 抑制 CSNK1A1 和 CSNK1D 的 IC50 分别为 3.62-6.34 μM 和 1.21 μM。 |
| 保存条件: |
-80°C 12个月; -20°C 6个月,干燥, 避光 |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
2.068 ml |
10.34 ml |
20.681 ml |
| 5 mM |
0.414 ml |
2.068 ml |
4.136 ml |
| 10 mM |
0.207 ml |
1.034 ml |
2.068 ml |
| 50 mM |
0.041 ml |
0.207 ml |
0.414 ml |
|
| 注意: |
部分产品我司仅能提供部分信息,我司不保证所提供信息的权威性,仅供客户参考交流研究之用。 |