GSK547 (Synonyms: GSK'547) |
Catalog No.GC19503 |
GSK547(GSK'547)은 수용체-상호작용 세린/트레오닌 단백질 키나제 1(RIPK1)의 고도로 선택적이고 강력한 억제제로, 췌장암에서 대식세포 매개 적응 면역 관용을 억제합니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2226735-55-1
Sample solution is provided at 25 µL, 10mM.
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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