2. MAPK/ERK Pathway Metabolic Enzyme/Protease
  3. p38 MAPK Mitochondrial Metabolism
  4. Arvenin I

Arvenin I is a natural cucurbitacin glucoside that activates T cells within the cancer-competitive environment. Arvenin I covalently reacts with and hyperactivates MKK3, thereby reviving the mitochondrial fitness of exhausted T cells through the activation of the p38MAPK pathway. Arvenin I exhibits broad-spectrum antiproliferative against cancer cells. Arvenin I enhances antitumor effects both as a monotherapy and in combination with immune checkpoint inhibitors in mice. Arvenin I can be used for cancer research, such as colon cancer, breast cancer, lung cancer, and ovarian cancer[1][2].

For research use only. We do not sell to patients.

Arvenin I

Arvenin I Chemical Structure

CAS No. : 65247-27-0

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Description

Arvenin I is a natural cucurbitacin glucoside that activates T cells within the cancer-competitive environment. Arvenin I covalently reacts with and hyperactivates MKK3, thereby reviving the mitochondrial fitness of exhausted T cells through the activation of the p38MAPK pathway[1]. Arvenin I exhibits broad-spectrum antiproliferative against cancer cells[2]. Arvenin I enhances antitumor effects both as a monotherapy and in combination with immune checkpoint inhibitors in mice[1]. Arvenin I can be used for cancer research, such as colon cancer, breast cancer, lung cancer, and ovarian cancer[1][2].

In Vitro

Arvenin I (0.5-4 μM, 48 h) displays no detectable induction of IL-2 in Jurkat PD-1 cells in the absence of PHA and PMA (HY-18739) and exhibits no significant cytotoxicity in Jurkat PD-1 cells at 4 μM, suggesting that it does not independently activate T cells but rather augments the PHA/PMA-induced activation of T cells[1].
Arvenin I (0-30 μM, 24-48 h) forms a covalent bond with specific cysteine residues in AKT (Cys310) and MKK3 (Cys227) through its Michael acceptor moiety to activate the MKK3-p38MAPK signaling pathway, leading to increased IL-2 production[1].
Arvenin I (250 nM, 2 h) enhances the mitochondrial bioenergetics in primary CD8+ T cells by increasing basal and maximal respiration as well as spare respiratory capacity through the p38MAPK pathway[1].
Arvenin I (1-100 μM, 3 days) exhibits broad-spectrum antiproliferative activity against a panel of human cancer cell lines, with IC50 values of 17.0, 49.4, 14.7 and 42.8 μM in A-549, HT-29, OVCAR, and MCF-7 cells, respectively[2].

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

Arvenin I Related Antibodies

Western Blot Analysis[1]

Cell Line: HEK293 and Jurkat PD-1 cells
Concentration: 0, 3, 10, and 30 μM for HEK293 cells; 0, 2, and 4 μM for Jurkat PD-1 cells
Incubation Time: 24 h
Result: Caused slightly slower electrophoretic migration of the Western-blotted bands of Flag-AKT wt and Flag-MKK3 wt on SDS-PAGE gels at concentrations as low as 3 μM.
Failed to induce a band shift in mutants where each corresponding cysteine residue was substituted with a serine residue (Flag-AKT C310S and Flag-MKK3 C227S), even at a high concentration of 30 μM.
Markedly increased the phosphorylation of p38MAPK Thr180/Tyr182 in Jurkat hPD-1 cells either in the presence or absence of PHA and PMA.
Had no detectable effects on the phosphorylation of FOXO1 Ser256.
Increased the phosphorylation of MKK3 in Jurkat hPD-1 cells.

Cell Viability Assay[1]

Cell Line: Jurkat PD-1 cells
Concentration: 0.5, 1, 2, and 4 μM
Incubation Time: 48 h
Result: Exhibited no significant cytotoxicity in Jurkat PD-1 cells at 4 μM.

ELISA Assay[1]

Cell Line: Jurkat PD-1, Jurkat MKK3 wild-type and C227S cells
Concentration: 4 μM
Incubation Time: 48 h
Result: Its ability to restore IL-2 production (suppressed by MDA-MB-231 conditioned medium) was dose-dependently canceled by SB203580 (HY-10256).
Potentiated the augmentation of IL-2 production resulting from the overexpression of wild-type MKK3.
In Vivo

Arvenin I (6 mg/kg, i.p., every 3 days from day 10 to day 22) suppresses tumor growth in immunocompetent but not Rag2KO MC38 tumor-bearing mice, demonstrating adaptive immune-dependent efficacy[1]

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

Animal Model: WT C57BL/6N mice (6 weeks old) Subcutaneously injected with MC38 colon cancer cells[1]
Dosage: 6 mg/kg
Administration: i.p., every 3 days from day 10 to day 22
Result: Caused a 40 % inhibition of tumor growth in comparison to the control group, comparable to the efficacy of the PD-L1 antibody (30 μg every 6 day from day 10 to day 22).
Produced approximately 70 % inhibition of tumor growth with a combination with PD-L1 antibody.
Did not lead to significant reductions in body weight or differences in liver toxicity markers, including AST, ALT, and LDH.
Significantly enhanced mitochondrial respiration and upregulated proliferation markers (Ki67) in DLN CD8+ T cells in combination with the PD-L1 antibody.
Increased TNF-α levels but reduced IFN-γ levels in combination with the PD-L1 antibody.
Showed a trend toward decreasing the population of terminally exhausted CD8+ T cells (PD1+ Tim3+) and increasing the proportion of less exhausted CD8+ T cells in the combination group.
Animal Model: Rag2KO C57BL/6N mice (6 weeks old) Subcutaneously injected with MC38 colon cancer cells[1]
Dosage: 6 mg/kg
Administration: i.p., every 3 days from day 10 to day 22
Result: Failed to suppress tumors in immunodeficient mice, thereby demonstrating that its antitumor efficacy is depends on the adaptive immune system.
Molecular Weight

720.84

Formula

C38H56O13
CAS No.
SMILES

CC(OC(C)(/C=C/C([C@@]([C@H]1[C@H](O)C[C@]2(C)[C@]1(C)CC([C@]3(C)[C@H]2CC=C4[C@H]3C[C@H](O[C@H]5[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O5)C(C4(C)C)=O)=O)(O)C)=O)C)=O
Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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Arvenin I 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:

Arvenin I65247-27-0p38 MAPKMitochondrial Metabolismanticancer effectscucurbitacin glucosideT cellscancer-competitiveMKK3mitochondrialp38MAPKMC38Rag2KO miceInhibitorinhibitorinhibit

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