A RIPK1 inhibitor
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GSK963

Item No. 39900

Technical Information
Formal Name
1-[(5S)-4,5-dihydro-5-phenyl-1H-pyrazol-1-yl]-2,2-dimethyl-1-propanone
CAS Number
2049868-46-2
Molecular Formula
C14H18N2O
Formula Weight
Purity
≥95%
A solid
Acetonitrile: SolubleDMSO: Soluble
SMILES
CC(C)(C)C(N1[C@H](C2=CC=CC=C2)CC=N1)=O
InChi Code
InChI=1S/C14H18N2O/c1-14(2,3)13(17)16-12(9-10-15-16)11-7-5-4-6-8-11/h4-8,10,12H,9H2,1-3H3/t12-/m0/s1
InChi Key
NJQVSLWJBLPTMD-LBPRGKRZSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    GSK963 is an inhibitor of receptor-interacting serine/threonine kinase 1 (RIPK1).1 It is selective for RIPK1 with less than 50% inhibition of 339 kinases in a panel at 10 µM. Unlike the RIPK1 inhibitor necrostatin-1 (Item No. 11658), GSK963 is inactive against indolamine-2,3-dioxygenase (IDO). GSK963 inhibits necroptosis induced by TNF in the presence of the caspase inhibitor zVAD in L-929 mouse and U937 human cells (IC50s = 1 and 4 nM, respectively). It also inhibits RIPK1-mediated lethal hypothermia induced by TNF with zVAD in mice when administered at a dose of 2 mg/kg in a model of sterile shock.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Berger, S.B., Harris, P., Nagilla, R., et alCharacterization of GSK'963: A structurally distinct, potent and selective inhibitor of RIP1 kinase. Cell Death Discov. 1, 15009 (2015).