JWG-045
JWG-045 is a selective ERK5 inhibitor. JWG-045 exhibits unique ferroptosis-resistant activity independent of ERK5 inhibition. JWG-045 can be used in breast cancer research.
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- CAS 番号: 1234480-61-5
- 分子式: C27H33N7O2
- 分子量:487.60
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
製品説明
IC50 & Target
[1]|
ERK5 |
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| HeLa | IC50 |
0.23 μM
Compound: 24
|
Inhibition of EGF-induced BMK1 autophosphorylation in human HeLa cells by SDS-PAGE analysis
Inhibition of EGF-induced BMK1 autophosphorylation in human HeLa cells by SDS-PAGE analysis
|
[PMID: 21412406] |
体外実験
JWG-045 (3 μM; 24 h) reduces cell density modestly in BT474 cells and protects both BT474 and MDA-MB-231 breast cancer cells from RSL3-induced ferroptotic cell death[1].
JWG-045 (3 μM; 24 h) protects ERK5-silenced MDA-MB-231 triple-negative breast cancer cells from RSL3-induced ferroptosis independently of ERK5 expression[1].
JWG-045 (3 μM; 6 days) reduces cell density in Trastuzumab (HY-P9907)-resistant BT474 breast cancer cells and restores sensitivity to Trastuzumab[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:BT474 luminal B breast cancer cells, MDA-MB-231 triple-negative breast cancer cells
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Concentration:3 μM (single treatment; pre-incubated then combined with RSL3)
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Incubation Time:24 h (single treatment; total incubation with RSL3); 20 h (live-cell imaging)
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Result:Caused a modest, statistically significant reduction in BT474 cell density.
Reduced RSL3-induced cytotoxicity in both BT474 and MDA-MB-231 cells, significantly increasing cell density compared to RSL3 alone.
Prevented the time-dependent decrease in BT474 cell confluency induced by RSL3 over 20 hours.
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Cell Line:ERK5-silenced MDA-MB-231 triple-negative breast cancer cells
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Concentration:3 μM (alone; combined with RSL3)
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Incubation Time:24 h
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Result:Blocked RSL3-induced ferroptotic death in both control and ERK5-silenced MDA-MB-231 cells, significantly increasing cell density compared to RSL3 alone.
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Cell Line:Trastuzumab-resistant BT474 breast cancer cells
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Concentration:3 μM (alone; combined with Trastuzumab)
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Incubation Time:6 days
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Result:Reduced BT474 cell density.
Restored the growth inhibitory effect of trastuzumab in Trastuzumab-resistant BT474 cells to the level achieved by Trastuzumab monotherapy in parental BT474 cells.
化学情報
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CAS 番号 1234480-61-5
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分子量 487.60
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分子式 C27H33N7O2
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SMILES
O=C(N(C1=CN=C(N=C12)NC3=CC=C(C=C3OC)N4CCN(CC4)C)C)C5=CC=CC=C5N2C(C)C
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
プロトコル
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Ferroptosis Solutions
Ferroptosis is an iron-dependent, non-apoptotic form of regulated cell death characterized by lethal lipid peroxidation and sensitivity to suppression by iron chelators or lipophilic radical-trapping antioxidants. The core pathway links cystine uptake through system Xc−, glutathione availability, GPX4-dependent detoxification of phospholipid hydroperoxides, iron-dependent oxidative reactions, and polyunsaturated-phospholipid metabolism into a cell-death program that is biochemically and morphologically distinct from apoptosis, necrosis, and autophagy. The ferroptosis pathway is experimentally linked to phenotype through chemical and genetic perturbation. Erastin induces ferroptosis by inhibiting cystine uptake through system Xc− and weakening antioxidant defenses, while GPX4 inhibition or depletion causes lipid peroxide accumulation and ferroptotic cancer-cell death. ACSL4 and oxidizable arachidonoyl- or adrenoyl-containing phosphatidylethanolamines shape ferroptosis sensitivity by con
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Breast Cancer Modeling
Breast cancer is a heterogeneous cancer, and it has been distinguished into four subtypes: luminal A, luminal B, HER2-positive and basal-like. Molecular mutations, epigenetic alterations, hormone exposure and immune microenvironment are related to the progression of breast cancer.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)