Tigilanol tiglate  (Synonyms: EBC-46)

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].

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

562.65

C₃₀H₄₂O₁₀

943001-56-7

Solid

White to off-white

CC[C@H](C)C(O[C@@]12[C@@]([C@]3([H])[C@@]4([H])[C@](O4)([C@H]([C@]5([C@](C=C(C5=O)C)([H])[C@]3([C@@H]([C@H]2OC(/C(C)=C/C)=O)C)O)O)O)CO)([H])C1(C)C)=O

Room temperature in continental US; may vary elsewhere.

-20°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

• [1]. Cullen J K, et al. Tigilanol tiglate is an oncolytic small molecule that induces immunogenic cell death and enhances the response of both target and non-injected tumors to immune checkpoint blockade[J]. Journal for ImmunoTherapy of Cancer, 2024, 12(4).  [Content Brief]

  [2]. Miller J, et al. Dose Characterization of the Investigational Anticancer Drug Tigilanol Tiglate (EBC-46) in the Local Treatment of Canine Mast Cell Tumors. Front Vet Sci. 2019 Apr 9;6:106.  [Content Brief]

  [3]. Antwi FD, et al. Tigilanol Tiglate-Induced Changes in Secretome Profiles Alter C-Met Phosphorylation and Cell Surface Protein Expression in H357 Head and Neck Cancer Cells. Cells. 2024 Jun 5;13(11):982.  [Content Brief]