GSK547 (GSK'547) 是受体相互作用的丝氨酸/苏氨酸蛋白激酶 1 (RIPK1) 的高选择性和强效抑制剂，可抑制巨噬细胞介导的胰腺癌适应性免疫耐受。
| Cas No. | 2226735-55-1 |
| 别名 | GSK'547 |
| Canonical SMILES | N#CC1=NC=NC(N2CCC(C(N3N=CC[C@H]3C4=CC(F)=CC(F)=C4)=O)CC2)=C1 |
| 分子式 | C20H18F2N6O |
| 分子量 | 396.39 |
| 溶解度 | Soluble in DMSO |
| 储存条件 | Store at -20℃ |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | GSK547, a highly selective and potent RIP1 inhibitor, inhibits macrophage-mediated adaptive immune tolerance in pancreatic cancer[1].
GSK547 (0.1-100000 nM; 24 hours) pretreats L929 cells with recombinant TNFα and zVAD at various doses for 30 min, then cell death is induced with an IC50 of 32 nM after 24 hours[1].
GSK547 up-regulates STAT1 signaling in bone marrow-derived macrophages (BMDM)[1].
GSK547 (GSK′547; RIP1i) robustly targets RIP1 in vivo. RIP1 inhibition results in immunogenic macrophage differentiation in pancreatic cancer, leading to adaptive immune activation and tumor protection for pancreatic ductal adenocarcinoma (PDA)[1].
GSK547 (100 mg/kg/day; fed via food-based dosing; 15-50 days) reduces tumor burden and extends survival compared with mice treated with controls or Nec-1s[1].
Reference：
[1]. Wang W, et al. RIP1 Kinase Drives Macrophage-Mediated Adaptive Immune Tolerance in Pancreatic Cancer. Cancer Cell. 2018 Nov 12;34(5):757-774.e7. |
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