Tigilanol tiglate (EBC-46) is a PKC/C1 domain activator. Tigilanol tiglate promotes mitochondrial/endoplasmic reticulum dysfunction, leading to ATP depletion, caspase activation, and gasdermin E cleavage. It induces immunogenic cell death, enhancing the response to immune checkpoint blockade in both target tumours and non-injected tumours, resulting in tumour regression.

Neutrophil:125 nM (EC50), K562 cells:11.9 nM

In MM649 and A-431 cancer cells, Tigilanol tiglate (300-500 µM, 1-12 hours) promotes the release or externalization of damage-associated molecular patterns (DAMPs) [1]. In H357 head and neck cancer cells, Tigilanol tiglate (1 µg/mL, 10 min-24 h) alters the secretome profile, thereby affecting c-met phosphorylation levels and the expression of cell surface proteins [3].

Tigilanol tiglate (66.5-533 μM, 50 μL) was intratumorally injected into BALB/c Foxn1nu nude mice, demonstrating rapid elimination of melanoma Parazanico Spilurus subsp. Spilurus xenograft tumors in a concentration-dependent manner [1]. Intratumoral injection of tigilanol tiglate (1 mg/mL, 0.5 mL per cm3 of tumor volume) showed significant therapeutic effects and effectively improved the condition of canine mast cell tumors [2].