MYCi975
规格
Cas Number | 2289691-01-4 |
规格或纯度 | 10mM in DMSO |
包装 | 1ml |
产品信息
品牌 | 阿拉丁 |
浓度 | 10mM in DMSO |
简短描述 | Myc 抑制剂 |
英文简短描述 | Myc Inhibitors |
过滤标签 | Compound libraries |
储存温度 | -80℃储存 |
运输条件 | 超低温冰袋运输 |
生化和生理学机理 | MYCi975(NUCC-0200975)是一种强效、选择性和口服活性的 MYC 抑制剂,它能破坏 MYC/MAX 相互作用,促进 MYC T58 磷酸化和 MYC 降解,并损害 MYC 驱动的基因表达。MYCi975 具有很强的抗肿瘤活性。 |
英文描述 |
Information MYCi975 MYCi975 is an orally active inhibitor of MYC that disrupts MYC/MAX interaction, promotes MYC T58 phosphorylation and MYC degradation, and impairs MYC driven gene expression. MYCi975 exhibits potent anti-tumor activities. Targets MYC In vitro MYCi975 localizes to the same region of the MYC protei. Treatment of cells with MYCi975 enhances MYC degradation and phosphorylation on T58. MYCi975 also directly increases GSK3b-mediated MYC pT58 in the in vitro kinase assay. In vivo MYCi975 suppresses in vivo tumor growth in mice, increases tumor immune cell infiltration, upregulates PD-L1 on tumors, and sensitizes tumors to anti-PD1 immunotherapy with good tolerability. Cell Research(from reference) Cell lines:MycCaP, PC3, LNCaP, PC12, MV411, SK-N-BE (2), 293T, P493-6 B cells, LLC1 cells, TGR-1, HO15.19 Rat-1 cells Concentrations:3-25 μM, 8 μM, 6 μM Incubation Time:24 h |