GSK-547 free base · Synonyms: GSK'547

GSK547 is a highly selective and potent inhibitor of RIP1.

For research use only. Not for human or veterinary use.

Target RIP kinase

Research area Cancer

Purity >98% Stock Inquire

Data Sheet SDS COA

GSK-547 structure

CAS No.: 2226735-55-1

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
250 mg	USD 545.00	BP-01990-250mg	In stock	Get quote
500 mg	USD 872.00	BP-01990-500mg	In stock	Get quote
1 g	USD 1,395.00	BP-01990-1g	In stock	Get quote
5 g	Inquire	BP-01990-5g	Inquire	Inquire

Need another size or custom synthesis? Request a quote.

Description

GSK547 is a highly selective and potent inhibitor of RIP1.

Biological activity

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. ? GSK547 up-regulates STAT1 signaling in bone marrow-derived macrophages (BMDM). 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). ? 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.

Identifiers

SMILES: FC1=CC(=CC(F)=C1)[C@@H]1CC=NN1C(=O)C1CCN(CC1)C1=CC(=NC=N1)C#N
InChIKey: SJVGFKBLUYAEOK-SFHVURJKSA-N

Specifications

MW (average): 396.3933
Formula: C₂₀H₁₈F₂N₆O
CAS No.: 2226735-55-1
Physical state: Solid
Color: White to off-white
Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage: Powder -20℃ 2 years; In solvent -20℃ 1 month;

Solubility

Soluble in DMSO >100 mg/mL

Documents

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.

Same target

Search RIP kinase

Same research area

Search Cancer