2. Epigenetics Apoptosis Neuronal Signaling Membrane Transporter/Ion Channel
  3. Epigenetic Reader Domain Necroptosis TRP Channel
  4. 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.

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Artepillin C Chemical Structure

Artepillin C Chemical Structure

CAS No. : 72944-19-5

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Based on 1 publication(s) in Google Scholar

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Artepillin C Related Antibodies

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Description

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].

IC50 & Target[3]

CREB/CRTC2

 

TRPA1

1.8 μM ()

Cellular Effect
Cell Line Type Value Description References
DU-145 IC50
179 μM
Compound: 1
Antiproliferative activity against human DU-145 cells assessed as cell viability for 72 hrs by MTT assay
Antiproliferative activity against human DU-145 cells assessed as cell viability for 72 hrs by MTT assay
[PMID: 34454129]
HeLa IC50
7 μg/mL
Compound: 1
Antiallergic activity in Ca(2+)-stimulated differentiated human HeLa cells assessed as inhibition of cys-leukotriene release after 6 days by ELISA
Antiallergic activity in Ca(2+)-stimulated differentiated human HeLa cells assessed as inhibition of cys-leukotriene release after 6 days by ELISA
[PMID: 19942440]
HT-1080 ED50
45.47 μg/mL
Compound: 5
Cytotoxicity against human HT1080 cells after 24 hrs by MTT assay
Cytotoxicity against human HT1080 cells after 24 hrs by MTT assay
[PMID: 9677271]
MCF-10A CC50
> 200 μM
Compound: 1
Cytotoxicity against human MCF-10A cells assessed as cell viability for 72 hrs by MTT assay
Cytotoxicity against human MCF-10A cells assessed as cell viability for 72 hrs by MTT assay
[PMID: 34454129]
MCF7 IC50
162.3 μM
Compound: 1
Antiproliferative activity against human MCF7 cells assessed as cell viability for 72 hrs by MTT assay
Antiproliferative activity against human MCF7 cells assessed as cell viability for 72 hrs by MTT assay
[PMID: 34454129]
MDA-MB-231 IC50
172.7 μM
Compound: 1
Antiproliferative activity against human MDA-MB-231 cells assessed as cell viability for 72 hrs by MTT assay
Antiproliferative activity against human MDA-MB-231 cells assessed as cell viability for 72 hrs by MTT assay
[PMID: 34454129]
PC-3 IC50
178.9 μM
Compound: 1
Antiproliferative activity against human PC-3 cells assessed as cell viability for 72 hrs by MTT assay
Antiproliferative activity against human PC-3 cells assessed as cell viability for 72 hrs by MTT assay
[PMID: 34454129]
PNT2 CC50
187.6 μM
Compound: 1
Cytotoxicity against human PNT2 cells assessed as cell viability for 72 hrs by MTT assay
Cytotoxicity against human PNT2 cells assessed as cell viability for 72 hrs by MTT assay
[PMID: 34454129]
In Vitro

Artepillin C (1 μM-1 mM; 12-48 h) inhibits the viability of HEp-2 tumor cells in a concentration- and time-dependent manner, with a CC50 of 4.07 μM-0.9 μM[1].
Artepillin C (1-0.5 μM; 24 h) induces HEp-2 cell necrosis and significantly increases cell membrane permeability[1].
Artepillin C (1 μM; 30 min; pH 3.2) enhances the membrane permeability of DPPS-containing macropinosomes (GUVs) and significantly accelerates the efflux of fluorescent probes[1].
Artepillin C (3.13-50 μg/mL; 36 h) inhibits HUVEC cell tube formation in a concentration-dependent manner, and completely inhibits it at 50 μg/mL[2].
Artepillin C (3.13-50 μg/mL; 3 d) inhibits HUVEC cell proliferation with an IC50 of approximately 37.2 μg/mL[2].

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

Artepillin C Related Antibodies

Apoptosis Analysis[1]

Cell Line: HEp-2 cells
Concentration: 0.01 mM, 0.05 mM, 0.1 mM, 0.5 mM
Incubation Time: 24 h
Result: Increased propidium iodide (PI)-positive cells, indicating membrane permeabilization and necrosis.
Morphological changes included cell swelling and granular nuclei, characteristic of necrotic cell death, without significant apoptosis induction.
In Vivo

Artepillin C (0.125%-0.5% diet; po; once a day; 6 days) inhibits tumor-induced angiogenesis in the mouse dorsal air sac tumor model and reduces the number of blood vessels in a dose-dependent manner[2].
Artepillin C (20 mg/kg; intraperitoneal injection; once a day; 1-3 weeks) significantly improves glucose homeostasis, reduces fasting blood glucose and insulin resistance, inhibits hepatic BMAL1 expression and lipid synthesis-related genes, and reduces hepatic lipid accumulation in db/db obese mice[4].
Artepillin C (20 mg/kg; intraperitoneal injection; once a day; 3 weeks) improves insulin sensitivity, reduces hepatic gluconeogenesis and lipid synthesis, and regulates the expression of the circadian rhythm-related gene Bmal1 in DIO mice fed a high-fat diet[4].

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

Animal Model: ICR mice (female, 30±5 g, 7-week-old), dorsal air sac (DAS) tumor angiogenesis model[2]
Dosage: 0.125%, 0.25%, 0.5% (w/w in diet)
Administration: Oral administration via diet, once daily, 6 days starting from chamber implantation
Result: Significantly reduced tumor-induced angiogenesis in a dose-dependent manner.
No signs of toxicity were observed, with stable body weight throughout the treatment period.
Histological analysis confirmed reduced vascular density in the treated groups, indicating anti-angiogenic activity without systemic toxicity.
Molecular Weight

300.39

Formula

C19H24O3
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

C/C(C)=C\CC1=C(C(C/C=C(C)\C)=CC(/C=C/C(O)=O)=C1)O
Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Purity & Documentation
References
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Artepillin C Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Artepillin C72944-19-5Epigenetic Reader DomainNecroptosisTRP ChannelTransient receptor potential channelsBile acidcholereticantitumorgastroprotectiveanti-inflammatoryantimicrobialantioxidantInhibitorinhibitorinhibit

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