CPS-021
CPS-021 is a selective PAK4 PROTAC degrader with a DC50 of 50 nM. CPS-021 degrades PAK4 via the ubiquitin-proteasome system. CPS-021 inhibits the migration and invasion of tumor cells, suppresses TGFβ-induced epithelial-mesenchymal transition (EMT) in tumor cells, and can be used in studies related to lung cancer metastasis.
(Pink: PAK4 ligand (HY-174822); Blue: Cereblon ligand (HY-10984); Black: linker).
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 分子式: C52H63N11O7
- 分子量:954.13
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
PROTACs アイソフォーム固有の製品をすべて表示
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生物活性
製品説明
IC50 & Target
[1]|
PAK4 50 nM (DC50) |
LIMK1 |
体外実験
CPS-021 (0.05-15.0 μM; 2-24 h) induces concentration-dependent and time-dependent degradation of PAK4 protein in A549 and MDA-MB-231 cells, without altering the phosphorylation level of PAK5[1].
CPS-021 inhibits PAK4 kinase activity in a cell-free system, with an IC50 value of 382.7 nM[1].
CPS-021 (0.6-10 µM) significantly reduces the protein and phosphorylation levels of PAK4 and its downstream target LIMK1 in H1299 cells[1].
CPS-021 (0.32-20 µM; 72 h) exhibits minimal cytotoxicity and weak antiproliferative activity in A549, MDA-MB-231 and H1299 cells[1].
CPS-021 (1-10 µM; 24-48 h) inhibits cell wound healing, migration and invasion in a concentration-dependent manner in A549, MDA-MB-231 and H1299 cells[1].
CPS-021 (0.01-0.64 μM) combined with TGF-β1 (HY-P78213) (5 ng/mL) blocks TGF-β-induced epithelial-mesenchymal transition (EMT) and alters the expression of related markers in A549 cells[1].
CPS-021 (5 μM; 14 h) exerts significant effects on altering the global proteome profile and regulating signaling pathways such as NOD-like receptors in A549 cells[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:A549 and MDA-MB-231
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Concentration:0.05, 0.15, 0.50, 1.50, 5.00, 15.0 µM
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Incubation Time:2, 4, 8, 12, 14, 24 h
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Result:Degraded PAK4 protein in a concentration-dependent manner.
Reduced PAK4 protein levels in a time-dependent manner, reaching maximum degradation at 24 hours.
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Cell Line:A549, MDA-MB-231, and H1299
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Concentration:0.32, 0.63, 1.25, 2.50, 5.00, 10.00, 20.00 µM
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Incubation Time:72 h
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Result:Exhibited low cytotoxicity at the tested concentrations and showed weak antiproliferative effects.
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Cell Line:A549, MDA-MB-231, and H1299
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Concentration:1.0, 5.0, 10.0 µM
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Incubation Time:24 h, 48 h
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Result:Effectively inhibited the wound healing and migration processes of the cells.
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Cell Line:A549, MDA-MB-231, and H1299
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Concentration:1.0, 5.0, 10.0 µM
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Incubation Time:48 h
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Result:Inhibited the migration and invasion capabilities of the cells in a concentration-dependent manner.
Parmacokinetics
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Balb/c-nu nude mice (lung cancer metastasis model via A549-luc luciferase-expressing lung cancer cell challenge)[1]
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Dosage:5 mg/kg; 10 mg/kg; 20 mg/kg
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Administration:once daily; 14 days
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Result:Inhibited the in vivo migration of lung cancer cells.
Was well tolerated.
Inhibited tumor cell metastasis in vivo in a dose-dependent manner.
化学情報
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分子量 954.13
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分子式 C52H63N11O7
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SMILES
O=C(N1CCN(CC1)CCCCCCCC(N2CCN(CC2)CCNC3=CC=CC4=C3C(N(C4=O)C5CCC(NC5=O)=O)=O)=O)C(C6=CC=C(C#CC7(O)CCCCC7)C=C86)=CN8C9=NC(N)=NC=C9
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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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Cell migration
Cell migration is a method that plays an important role in wound healing, cell differentiation, embryonic development, etc.
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Cell invasion
Cell invasion is the ability of cells to migrate from one area to another via the extracellular matrix. Cell invasion is the response of normal and cancer cells to chemical and mechanical stimuli. Before migrating to a new region, the extracellular matrix is degraded by proteases within the cell. Cell invasion often occurs during wound repair, vascularization and inflammation, abnormal tissue invasion, and tumor cell metastasis.
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Orthotopic Cell-Line Xenograft
Orthotopic cell-line xenograft models involve implantation of human cancer cell lines into the anatomically corresponding organ of immunodeficient mice to reproduce tumor growth within a native microenvironment, enabling more clinically relevant tumor behavior compared with subcutaneous models. These models are widely used because orthotopic placement better recapitulates tumor progression, including invasion and metastatic spread, which are often underrepresented in heterotopic implantation systems. Compared with conventional xenografts, orthotopic implantation is described as more technically complex but provides improved simulation of tumor-microenvironment interactions and metastatic behavior, making it particularly valuable for translational oncology research. Surgical orthotopic implantation approaches have been emphasized as enabling faithful reproduction of clinical cancer features, including metastasis and disease progression patterns that align with the tumor’s organ of origi
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)