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MedChemExpress - Model Tigilanol ...

MedChemExpress - Model Tigilanol tiglate - 943001-56-7

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

MCE China：Tigilanol tiglate

Brand：MedChemExpress (MCE)

Cat. No.HY-109076

CAS：943001-56-7

Synonyms：EBC-46

Purity：95.89%

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

Shipping：Room temperature in continental US; may vary elsewhere.

Description：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.

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 Foxn1nu 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].

References：

[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]

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