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GSK547

Chemical Structure : GSK547

CAS No.: 2226735-55-1

GSK547 (GSK'547; RIP1i; GSK 547; GSK-547)

Catalog No.: PC-35793Not For Human Use, Lab Use Only.

GSK547 (RIP1i, GSK'547, GSK 547) is a highly selective and potent inhibitor of RIP1 kinase that robustly targets RIP1 in vivo.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

GSK547 (RIP1i, GSK'547) is a highly selective and potent inhibitor of RIP1 kinase that robustly targets RIP1 in vivo.
GSK547 exhibited a 400-fold improvement in mouse pharmacokinetic oral exposure compared with GSK'963.
GSK547 reprogrammed TAMs toward an MHCIIhiTNFα+IFNγ+ immunogenic phenotype in a STAT1-dependent manner.
RIP1 inhibition in TAMs resulted in cytotoxic T cell activation and T helper cell differentiation toward a mixed Th1/Th17 phenotype, leading to tumor immunity in mice and in organotypic models of human Pancreatic ductal adenocarcinoma (PDA).

Physicochemical Properties

M.Wt 396.402
Formula C20H18F2N6O
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(S)-6-(4-(5-(3,5-difluorophenyl)-4,5-dihydro-1H-pyrazole-1-carbonyl)piperidin-1-yl)pyrimidine-4-carbonitrile

References

1. Wang W, et al. Cancer Cell. 2018 Nov 12;34(5):757-774.e7.

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