1. Apoptosis NF-κB Metabolic Enzyme/Protease Immunology/Inflammation MAPK/ERK Pathway
  2. Ferroptosis Reactive Oxygen Species (ROS) p38 MAPK
  3. Talaroconvolutin A

Talaroconvolutin A is a ferroptosis inducer. Talaroconvolutin A induces ferroptosis by increasing reactive oxygen species (ROS) levels rather than the GPX4 pathway. Talaroconvolutin A downregulates the expression of the channel protein solute carrier family 7 member 11 (SLC7A11) and upregulates arachidonic acid lipoxygenase 3 (ALOXE3). Talaroconvolutin A inhibits the growth of colorectal cancer cells HCT116 and bladder cancer cells SW480 with IC50 values of 1.22 μM and 1.4 μM, respectively. Talaroconvolutin A can be used in the study of colorectal cancer and bladder cancer[1][2][3].

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Talaroconvolutin A

Talaroconvolutin A Chemical Structure

CAS No. : 273199-42-1

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Description

Talaroconvolutin A is a ferroptosis inducer. Talaroconvolutin A induces ferroptosis by increasing reactive oxygen species (ROS) levels rather than the GPX4 pathway. Talaroconvolutin A downregulates the expression of the channel protein solute carrier family 7 member 11 (SLC7A11) and upregulates arachidonic acid lipoxygenase 3 (ALOXE3). Talaroconvolutin A inhibits the growth of colorectal cancer cells HCT116 and bladder cancer cells SW480 with IC50 values of 1.22 μM and 1.4 μM, respectively. Talaroconvolutin A can be used in the study of colorectal cancer and bladder cancer[1][2][3].

In Vitro

Talaroconvolutin A (0-40 μM, 24 h) suppresses the growth of HCT116, SW480, and SW620 cells, with the IC50s of 9.23, 8.15, and 5.82 μM in 10% FBS medium, respectively, with the IC50s of 1.22, 1.40, and 1.27 μM in 1% FBS medium, correspondingly[1].

Talaroconvolutin A (0-40 μM, 48 h) decreases DNA synthesis in HCT116 cells and SW480 cells[1].

Talaroconvolutin A (0-10 μM, 12 days) suppresses cell growth and induces cell death in SW480 cells[1].

Talaroconvolutin A (0-10 μM, 24 h) kills CRC cells by increasing ROS levels, but does not induce apoptosis or cell cycle arrest in SW480 cells[1].

Talaroconvolutin A (5 μM, 24 h) induces ferroptosis and increases lipid peroxidation in SW480 cells[1].

Talaroconvolutin A (0-125 μM, 24 h) induces the death of colon cancer cells by the ferroptosis pathway[1].

Talaroconvolutin A (5 μM) enhances cell activity in overexpressed SLC7A11 SW480 cells, reduces cell activity in SLC7A11 knocked-down SW480 cells[1].

Talaroconvolutin A (0-10 μM) increases ALOXE3 mRNA and protein levels in SW480 cells[1].

Talaroconvolutin A (0-12 μM, 24 h) inhibits the proliferation of SW780 and UM-UC-3 cells, with IC50s of 5.7 and 8.2 μM, respectively, in 10% FBS medium, with the IC50s of 1.2 and 2.3 μM, respectively, in 1% FBS medium[2].

Talaroconvolutin A (0-12 μM, 24 h) slows DNA replication in SW780 cells[2].

Talaroconvolutin A (0-8 μM, 10 days) inhibits the clonogenic ability of SW780 cells[2].

Talaroconvolutin A (0-7.5 μM, 24 h) inhibits cell cycle in SW780 cells[2].

Talaroconvolutin A (0-15 μM, 24-48 h) induces cell death through ROS-induced ferroptosis in SW780 cells, but does not induce significant apoptosis in SW780 cells[2].

Talaroconvolutin A still exhibits anticancer activity in SW780 cells and UM-UC-3 cells after conjugation with biotin, indicating that biotin does not destroy the anticancer active site[2].

Talaroconvolutin A induces phosphoproteomic changes by pulling down MAPK1 and MAPK14 kinase activities in SW780 cells and UM-UC-3 cells[2].

Talaroconvolutin A inhibits Hela cells, BEL-7042 cells and α-glucosidase activity, with IC50s of 14.9 μM, 26.7 μM, and 78.2 μM, respectively[3].

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

Cell Cycle Analysis[1]

Cell Line: SW480 cells
Concentration: 0 μM, 5.0 μM, 10 μM
Incubation Time: 24 h
Result: Did not cause cell cycle arrest, but increased the subG1 peak.

Apoptosis Analysis[1]

Cell Line: SW480 cells
Concentration: 0 μM, 5.0 μM, 10 μM
Incubation Time: 24 h
Result: Induced cell death but did not induce early apoptosis.
Led to drastic changes in the morphology of the cell membrane: the membrane surface was no longer smooth and intact, but had multiple perforations.

Cell Cycle Analysis[2]

Cell Line: SW480 cells
Concentration: 0 μM, 2.5 μM, 5.0 μM, 7.5 μM
Incubation Time: 24 h
Result: Inhibited cell cycle, increased p21/CIP, but decreased CCNA2 and CCNB1 at the protein level.

Apoptosis Analysis[2]

Cell Line: SW480 cells
Concentration: 0 μM, 5 μM, 10 μM, 15 μM
Incubation Time: 48 h
Result: Did not induce significant apoptosis.
In Vivo

Talaroconvolutin A (6 mg/kg, i.p., every 2 days, 40 days) suppresses tumor growth in Balb/c nude mice bearing cancer HCT116 cells[1].

Talaroconvolutin A (6 mg/kg, i.p., every 2 days, 24 days) suppresses bladder tumor growth in vivo in a xenografted mouse model[2].

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

Animal Model: Balb/c nude mice (5-week old). bearing cancer HCT116 cells (5 × 106) [1]
Dosage: 6 mg/kg
Administration: i.p., every 2 days, 40 days
Result: Decreased tumor growth speed, did not affect body weight, routine blood index, histological morphology of liver and kidney.
Reduced Ki67 and ferroptosis-related molecule SLC7A11 levels but increased the level of HMOX1.
Animal Model: SW780 bladder cancer cells (107 cells) xenografted nude mice (female 6-week-old BALB/C-nude mice) model [2]
Dosage: 6 mg/kg
Administration: i.p., every 2 days, 24 days
Result: Reduced tumor growth rate and size.
Decreased the expression of the marker protein Ki67, repressed cell proliferation in transplanted tumors.
Had no serious toxicity in the liver and kidney
Molecular Weight

487.67

Formula

C32H41NO3

CAS No.
SMILES

O=C(C1=C/C(NC1=O)=C/C2=CC=C(C=C2)O)[C@H]3[C@@]4([H])[C@](C=C([C@H]3/C(C)=C/[C@@H](C)CC)C)(C[C@@H](CC4)C)C

Structure Classification
Initial Source

Cladosporium sp.

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Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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