Tigilanol tiglate

Tigilanol tiglate (EBC-46) is a protein kinase C (PKC)/C1 domain activator. Tigilanol tiglate is associated with mitochondrial/endoplasmic reticulum (ER) dysfunction, leading to activation of the unfolded protein response (UPRmt/ER) and subsequent induction of ATP depletion, organelles expansion, Caspase activation, gasdermin E cleavage, and terminal necrosis. Tigilanol tiglate, as a small anti-tumor molecule with immunomodulatory effects, can be used in the study of head and neck squamous cell carcinoma and soft tissue sarcoma^[1][2][3]. In Vitro:Tigilanol tiglate (300-500  µM, 1-12 h) promotes the release/externalization of damage associated molecular patterns from cancer cells MM649 and A-431^[1].
Tigilanol tiglate (1 µg/mL, 10 min-24 h) induces changes in secretome profiles, which altering c-met phosphorylation and cell surface protein expression in H357 head and neck cancer cells^[3].
In Vivo:Tigilanol tiglate (66.5-533 μM, 50 μL, intratumorally) rapidly ablates melanoma xenograft tumors in a concentration dependent manner in BALB/c Foxn1^nu nude mice^[1].
Tigilanol tiglate (1 mg/mL, 0.5 mL per cm³ of tumor volume, intratumoral) is highly efficacious for the improvement of mast cell tumors in dogs^[2].