A RIPK1 inhibitor
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GSK547

Item No. 37347

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
6-[4-[[(5S)-5-(3,5-difluorophenyl)-4,5-dihydro-1H-pyrazol-1-yl]carbonyl]-1-piperidinyl]-4-pyrimidinecarbonitrile
CAS Number
2226735-55-1
Synonyms
  • RIP1i
Molecular Formula
C20H18F2N6O
Formula Weight
396.4
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMF: 1 mg/mlDMSO: Slightly solubleEthanol: Slightly soluble
λmax
256 nm
SMILES
N#CC1=CC(N2CCC(C(N3N=CC[C@@]3([H])C4=CC(F)=CC(F)=C4)=O)CC2)=NC=N1
InChi Code
InChI=1S/C20H18F2N6O/c21-15-7-14(8-16(22)9-15)18-1-4-26-28(18)20(29)13-2-5-27(6-3-13)19-10-17(11-23)24-12-25-19/h4,7-10,12-13,18H,1-3,5-6H2/t18-/m0/s1
InChi Key
SJVGFKBLUYAEOK-SFHVURJKSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $33

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    5 mg

    $139

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    10 mg

    $196

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    25 mg

    $367

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    Product Description

    GSK547 is an inhibitor of receptor-interacting serine/threonine kinase 1 (RIPK1; IC50 = 31 nM).1 It is selective for RIPK1 over a panel of 371 kinases, including RIPK2, -3, -4, and -5, at 10 µM. In vivo, GSK547 (100 mg/kg) increases survival and reduces tumor volume and the number of liver metastases in a P48Cre KrasG12D orthotopic mouse model of progressive pancreatic ductal adenocarcinoma (PDA). Adoptive transfer of tumor-infiltrating T cells isolated from GSK547-treated mice protects against orthotopic PDA tumor growth in mice. GSK547 also reduces plasma levels of TNF-α and IL-1β and decreases macrophage infiltration in aortic sinus lesions in an ApoESA/SA mouse model of early-phase atherogenesis.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Wang, W., Marinis, J.M., Beal, A.M., et al. RIP1 kinase drives macrophage-mediated adaptive immune tolerance in pancreatic cancer. Cancer Cell 34(5), 757-774 (2018).

    2. Zhang, Y., Li, H., Huang, Y., et al. Stage-dependent impact of RIPK1 inhibition on atherogenesis: Dual effects on inflammation and foam cell dynamics. Front. Cardiovasc. Med. 8:715337, (2021).