Ingenol-3-angelate | PKC activator

Ingenol-3-angelate (75567-37-2) is a selective activator of protein kinase C which displays antileukemic activity mediated via PKCδ.¹ In contrast, it provides a strong survival signal to resting and activated human T cells via activation of PKC and downstream activation of NFκB.² Treatment of subcutaneous tumors results in anti-cancer CD8 T cells, also displays adjuvant activity and synergizes with cancer immunotherapies.³ Induces senescence-like growth arrest in solid tumor cells.⁴ Inhibits HIV-1 infection at an early pathway of viral entry.⁵

References/Citations

1) Hampson et al. (2005), PEP005, a selective small-molecule activator of protein kinase C, has potent antileukemic activity mediated via the delta isoform of PKC; Blood, 106 1362
2) Lee et al. (2010), Novel antileukemic compound ingenol 3-angelate inhibits T cell apoptosis by activating protein kinase Ctheta; J. Biol. Chem., 285 23889
3) Le et al. (2009), Immunostimulatory cancer chemotherapy using local ingenol-3-angelate and synergy with immunotherapies; Vaccine, 27 3053
4) Mason et al. (2010), The induction of senescence-like growth arrest by protein kinase C-activating diterpene esters in solid tumor cells; Invest. New Drugs, 28 575
5) Warrilow et al. (2006), HIV type 1 inhibition by protein kinase C modulatory compounds; AIDS Res. Hum. Retroviruses, 22 854