Artepillin C

Artepillin C is an orally active CREB/CRTC2 inhibitor and TRPA1 covalent agonist (EC50=1.8 μM) . Artepillin C inhibits CREB/CRTC2-mediated gene transcription and downregulates BMAL1 expression to regulate glucose and lipid metabolism. Artepillin C can also activate TRPA1 channels to induce spicy taste signals. Artepillin C can inhibit tumor cell proliferation, induce necroptosis, improve insulin resistance and inhibit liver lipid synthesis. Artepillin C can be used in the study of metabolic syndrome, tumor prevention and treatment, and inflammation[1][2][3][4].

Product Specifications

CAS Number

[72944-19-5]

UNSPSC

12352005

Hazard Statement

H315, H319

Target

Epigenetic Reader Domain; Necroptosis; TRP Channel

Type

Natural Products

Related Pathways

Apoptosis; Epigenetics; Membrane Transporter/Ion Channel; Neuronal Signaling

Applications

Cancer-programmed cell death

Field of Research

Cancer; Metabolic Disease; Inflammation/Immunology

Assay Protocol

https://www.medchemexpress.com/artepillin-c.html

Purity

98.28

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

C/C(C)=C\CC1=C(C(C/C=C(C)\C)=CC(/C=C/C(O)=O)=C1)O

Molecular Formula

C19H24O3

Molecular Weight

300.39

Precautions

H315, H319

References & Citations

[1]Kobal MB, et al. Correlating Artepillin C cytotoxic activity on HEp-2 cells with bioinspired systems of plasma membranes. Mater Sci Eng C Mater Biol Appl. 2020 Jul;112:110943.|[2]Ahn MR, et al. Suppression of tumor-induced angiogenesis by Brazilian propolis: major component artepillin C inhibits in vitro tube formation and endothelial cell proliferation. Cancer Lett. 2007 Jul 18;252 (2) :235-43.|[3]Hata T, et al. Artepillin C, a major ingredient of Brazilian propolis, induces a pungent taste by activating TRPA1 channels. PLoS One. 2012;7 (11) :e48072.|[4]Wang L, et al. Artepillin C Time-Dependently Alleviates Metabolic Syndrome in Obese Mice by Regulating CREB/CRTC2-BMAL1 Signaling. Nutrients. 2023 Mar 28;15 (7) :1644.