PK68

PK68 is an inhibitor of receptor-interacting serine/threonine kinase 1 (RIPK1; IC₅₀ = 90 nM).¹ It is selective for RIPK1 over RIPK3 and a panel of 369 kinases at 1,000 nM. PK68 inhibits necroptosis induced by TNF-α, a Smac mimetic, and z-VAD in HT-29 colon cancer cells (EC₅₀ = 23 nM). It reduces the number of lung metastases in a B16/F10 murine melanoma model when administered at a dose of 5 mg/kg. PK68 (1 mg/kg) increases survival and prevents decreases in body temperature and increases in serum Il-1β levels in a mouse model of Tnf-α-induced systemic inflammatory response syndrome (SIRS).

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1. Hou, J., Ju, J., Zhang, Z., et al. Discovery of potent necroptosis inhibitors targeting RIPK1 kinase activity for the treatment of inflammatory disorder and cancer metastasis. Cell Death Dis. 10(7), 493 (2019).