2. Apoptosis Metabolic Enzyme/Protease NF-κB Immunology/Inflammation
  3. Ferroptosis Apoptosis ACSL Family Glutathione Peroxidase Reactive Oxygen Species (ROS)
  4. Lepadin H

Lepadin H is a ferroptosis inducer and apoptosis inducer with in vitro cytotoxicity and in vivo antitumor efficacy against cancer cells. Lepadin H reduces GPX4 and SLC7A11 levels, increases p53 and ACSL4 expression, drives lipid hydroperoxide production, elevates reactive oxygen species (ROS) levels, reduces cellular glutathione (GSH) levels, induces lipid peroxidation and G2/M phase cell cycle arrest, and suppresses clonogenic growth and migration of cancer cells.Lepadin H can be used for the research of melanoma.

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Lepadin H

Lepadin H 構造式

CAS 番号 : 412328-25-7

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Lepadin H 関連抗体

Top Publications Citing Use of Products

ACSL Family アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
ACSL4 ACSL5

Glutathione Peroxidase アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
GPX1 GPX4

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製品説明

Lepadin H is a ferroptosis inducer and apoptosis inducer with in vitro cytotoxicity and in vivo antitumor efficacy against cancer cells. Lepadin H reduces GPX4 and SLC7A11 levels, increases p53 and ACSL4 expression, drives lipid hydroperoxide production, elevates reactive oxygen species (ROS) levels, reduces cellular glutathione (GSH) levels, induces lipid peroxidation and G2/M phase cell cycle arrest, and suppresses clonogenic growth and migration of cancer cells.Lepadin H can be used for the research of melanoma[1].

IC50 & Target[1]

ACSL4

 

GPX4

 

Cellular Effect
Cell Line Type Value Description References
A549 IC50
4.68 μM
Compound: Lepadin H
Cytotoxicity against human A549 cells incubated for 72 hrs by MTT assay
Cytotoxicity against human A549 cells incubated for 72 hrs by MTT assay
[PMID: 37578947]
B16-F10 IC50
3.14 μM
Compound: Lepadin H
Cytotoxicity against mouse B16-F10 cells incubated for 72 hrs by MTT assay
Cytotoxicity against mouse B16-F10 cells incubated for 72 hrs by MTT assay
[PMID: 37578947]
HeLa IC50
2.52 μM
Compound: Lepadin H
Cytotoxicity against human HeLa cells incubated for 72 hrs by MTT assay
Cytotoxicity against human HeLa cells incubated for 72 hrs by MTT assay
[PMID: 37578947]
HepG2 IC50
6.2 μM
Compound: Lepadin H
Cytotoxicity against human HepG2 cells incubated for 72 hrs by MTT assay
Cytotoxicity against human HepG2 cells incubated for 72 hrs by MTT assay
[PMID: 37578947]
L02 IC50
12.49 μM
Compound: Lepadin H
Cytotoxicity against human L02 cells incubated for 72 hrs by MTT assay
Cytotoxicity against human L02 cells incubated for 72 hrs by MTT assay
[PMID: 37578947]
MCF7 IC50
5.03 μM
Compound: Lepadin H
Cytotoxicity against human MCF7 cells incubated for 72 hrs by MTT assay
Cytotoxicity against human MCF7 cells incubated for 72 hrs by MTT assay
[PMID: 37578947]
MDA-MB-231 IC50
8.51 μM
Compound: Lepadin H
Cytotoxicity against human MDA-MB-231 cells incubated for 72 hrs by MTT assay
Cytotoxicity against human MDA-MB-231 cells incubated for 72 hrs by MTT assay
[PMID: 37578947]
NCI-H1155 IC50
7.06 μM
Compound: Lepadin H
Cytotoxicity against human NCI-H1155 cells incubated for 72 hrs by MTT assay
Cytotoxicity against human NCI-H1155 cells incubated for 72 hrs by MTT assay
[PMID: 37578947]
NCI-H1355 IC50
9.3 μM
Compound: Lepadin H
Cytotoxicity against human NCI-H1355 cells incubated for 72 hrs by MTT assay
Cytotoxicity against human NCI-H1355 cells incubated for 72 hrs by MTT assay
[PMID: 37578947]
SH-SY5Y IC50
5.8 μM
Compound: Lepadin H
Cytotoxicity against human SH-SY5Y cells incubated for 72 hrs by MTT assay
Cytotoxicity against human SH-SY5Y cells incubated for 72 hrs by MTT assay
[PMID: 37578947]
SK-OV-3 IC50
8.02 μM
Compound: Lepadin H
Cytotoxicity against human SK-OV-3 cells incubated for 72 hrs by MTT assay
Cytotoxicity against human SK-OV-3 cells incubated for 72 hrs by MTT assay
[PMID: 37578947]
SMMC-7721 IC50
4.09 μM
Compound: Lepadin H
Cytotoxicity against human SMMC-7721 cells incubated for 72 hrs by MTT assay
Cytotoxicity against human SMMC-7721 cells incubated for 72 hrs by MTT assay
[PMID: 37578947]
体外実験

Lepadin H (72 h) potently inhibits the viability of 10 human cancer cell lines and 1 normal human cell line (L02) with IC50 values ranging from 2.52 μM (HeLa) to 12.49 μM (L02) after 72 h incubation[1].
Lepadin H (5-9 μM; 24 h) inhibits clonogenic growth of HeLa cells in a dose-dependent manner, with complete inhibition at 8 and 9 μM after 24 h treatment[1].
Lepadin H (0.625-10 μM; 24 h) potently suppresses HeLa cell migration in a dose-dependent manner when treated for 24 h at concentrations from 0.625 to 10 μM[1].
Lepadin H (4-10 μM; 24 h) induces dose-dependent apoptosis in HeLa cells, with ~70% apoptotic cells at 10 μM after 24 h treatment, and upregulates cleaved-PARP expression[1].
Lepadin H (4-12 μM; 24 h) causes dose-dependent G2/M phase cell cycle arrest in HeLa cells and upregulates p53 and p21 protein expression after 24 h treatment[1].
Lepadin H (6-20 μM; 0.5-1 h) increases intracellular ROS levels in HeLa cells in a dose- and time-dependent manner[1].
Lepadin H (10-12 μM; 4 h) significantly increases lipid peroxidation in HeLa cells, with ~55% and ~73% lipid peroxidation observed at 10 and 12 μM after 4 h treatment, respectively[1].
Lepadin H (2.5-20 μM; 24 h) induces ferroptosis in HeLa cells via the p53-SLC7A11-GPX4 pathway, as evidenced by reduced GSH levels, characteristic mitochondrial ultrastructural changes, upregulated ACSL4 expression, downregulated SLC7A11 and GPX4 expression[1].
Lepadin H (6 μM; 24 h) alters the transcriptome and proteome of HeLa cells, with significant enrichment of ferroptosis-related pathways and downregulation of ferroptosis-associated gene SLC7A11[1].

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

Lepadin H 関連抗体

Cell Proliferation Assay[1]

Cell Line: HeLa
Concentration: 5 μM, 6 μM, 7 μM, 8 μM, 9 μM
Incubation Time: 24 h
Result: Completely eliminated colony formation at 8 and 9 μM.
Strongly reduced colony numbers at 7 μM.
Showed partial inhibition of colony growth at 5 and 6 μM compared to control.

Cell Migration Assay[1]

Cell Line: HeLa
Concentration: 0.625 μM, 1.25 μM, 2.5 μM, 5 μM, 10 μM
Incubation Time: 24 h
Result: Significantly inhibited cell migration at all tested concentrations in a dose-dependent manner.
Showed the strongest inhibition at 10 μM.

Apoptosis Analysis[1]

Cell Line: HeLa
Concentration: 4 μM, 6 μM, 8 μM, 10 μM
Incubation Time: 24 h
Result: Induced apoptosis in ~70% of cells at 10 μM.
Induced dose-dependent increase in apoptotic cell percentages at 4, 6, 8, and 10 μM.
Markedly increased cleaved-PARP protein levels at 10 μM.

Cell Cycle Analysis[1]

Cell Line: HeLa
Concentration: 4 μM, 6 μM, 8 μM, 10 μM, 12 μM
Incubation Time: 24 h
Result: Induced dose-dependent G2/M phase cell cycle arrest with increasing percentages of cells in G2/M phase at 4 to 12 μM.
Upregulated p53 and p21 protein levels in a dose-dependent manner at 4, 6, 8, and 10 μM.
体内実験

Lepadin H (30 mg/kg; i.p.; daily; 14 consecutive days) significantly suppresses B16F10 melanoma tumor growth in C57BL/6J mice by reducing tumor volume greater than three-fold, with no obvious toxicity to major organs[1].

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

Animal Model: C57BL/6J (female, 8 weeks old, subcutaneous injection of 1 × 107 B16F10 cells)[1]
Dosage: 30 mg/kg
Administration: i.p.; daily; 14 consecutive days
Result: Reduced tumor volume from ~1500 mm3 to <500 mm3 (a greater than three-fold reduction).
Significantly decreased tumor weight relative to controls.
Showed no significant changes in mouse body weight, organ indexes, or histologic tissue damage in heart, liver, spleen, lung, kidney, or thymus.
分子量

419.64

分子式

C26H45NO3
CAS 番号
SMILES

CCC[C@@H](O)CCCC[C@@H]1[C@@]2([H])[C@](CCC1)([H])N[C@H]([C@@H](C2)OC(/C=C/C=C/CCC)=O)C
Structure Classification
Initial Source

Tropical Marine Tunicate Didemnum sp.
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
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Lepadin H Related Classifications

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  • 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:

Lepadin H412328-25-7FerroptosisApoptosisACSL FamilyGlutathione PeroxidaseReactive Oxygen Species (ROS)ferroptosismelanomatumor protein p53apoptosisacyl-CoA synthetase long chain family member 4HeLareactive oxygen speciessolute carrier family 7 member 11glutathione peroxidase 4lipid peroxidationInhibitorinhibitorinhibit

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