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MedChemExpressModel GSK547 - 2226735-55-1

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GSK547 (GSK'547) is a highly selective and potent inhibitor of receptor-interacting serine/threonine protein kinase 1 (RIPK1), inhibits macrophage-mediated adaptive immune tolerance in pancreatic cancer[1].
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GSK547

MCE China:GSK547

Brand:MedChemExpress (MCE)

Cat. No.HY-114492

CAS:2226735-55-1

Synonyms:GSK'547

Purity:99.92%

Storage:-20°C, stored under nitrogen *In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Shipping:Room temperature in continental US; may vary elsewhere.

Description:GSK547 (GSK'547) is a highly selective and potent inhibitor of receptor-interacting serine/threonine protein kinase 1 (RIPK1), inhibits macrophage-mediated adaptive immune tolerance in pancreatic cancer.

In Vitro: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].

In Vivo: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].

IC50 & Target:RIP1[1] Cellular Effect Cell Line Type Value Description References

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References:

[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.  [Content Brief]

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